- Synthesis, characterization and in vitro antiproliferative activities of new 13-cis-retinoyl ferrocene derivatives
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In order to improve biological behavior of the retinoyl derivatives, monoarylferrocenyl alcohols 9a and 9b were synthesized by an improved Suzuki cross-coupling method and their 13-cis-retinoic acid analogues were prepared in moderate to good yields via t
- Long, Bohua,Liang, Shengzong,Xin, Dingcheng,Yang, Yingbin,Xiang, Jiannan
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Read Online
- Xylochemical synthesis and biological evaluation of shancigusin c and bletistrin g
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The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regiose-lective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.
- Efferth, Thomas,Geske, Leander,Kauhl, Ulrich,Opatz, Till,Saeed, Mohamed E. M.,Schüffler, Anja,Thines, Eckhard
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supporting information
(2021/06/16)
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- Palladium-Catalyzed Synthesis of N, N-Dimethylanilines via Buchwald-Hartwig Amination of (Hetero)aryl Triflates
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This work delineates the synthesis of N,N-dimethylaniline derivatives from dimethylamines and aryl triflates. The palladium-catalyzed C-N bond formation proceeds in excellent yields, using an unsophisticated catalytic system, a mild base, and triflates as electrophiles, which are readily available from inexpensive phenols. N,N-Dimethylanilines are multifunctional reaction partners and represent useful but underutilized building blocks in organic synthesis.
- Pospech, Jola,Taeufer, Tobias
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p. 7097 - 7111
(2020/06/27)
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- Catalytic Access to Functionalized Allylic gem-Difluorides via Fluorinative Meyer–Schuster-Like Rearrangement
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An unprecedented approach for efficient synthesis of functionalized allylic gem-difluorides via catalytic fluorinative Meyer–Schuster-like rearrangement is disclosed. This transformation proceeded with readily accessible propargylic fluorides, and low-cost B–F reagents and electrophilic reagents by sulfide catalysis. A series of iodinated, brominated, and trifluoromethylthiolated allylic gem-difluorides that were difficult to access by other methods were facilely produced with a wide range of functional groups. Importantly, the obtained iodinated products could be incorporated into different drugs and natural products, and could be expediently converted into many other valuable gem-difluoroalkyl molecules as well. Mechanistic studies revealed that this reaction went through a regioselective fluorination of alkynes followed by a formal 1,3-fluorine migration under the assistance of the B–F reagents to give the desired products.
- An, Rui,Li, Huimin,Liao, Lihao,Wu, Jin-Ji,Xu, Yang,Zhao, Xiaodan
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supporting information
p. 11010 - 11019
(2020/05/18)
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- Efficient cross-coupling of aryl/alkenyl triflates with acyclic secondary alkylboronic acids
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Aryl-secondary alkyl cross-coupling with aryl sulfonate esters as coupling partners remains a significant challenge. Efficient cross-coupling between aryl/alkenyl triflates and acyclic secondary alkylboronic acids is realized for the first time to provide a series of sterically congested acyclic secondary alkyl arenes/olefins in good to excellent yields. The employment of sterically bulky P,PO ligand L1/L2 is crucial for the high yields and selectivities. The method has enabled a concise and 4-step synthesis of a key intermediate of male contraceptive agent and PAF antagonist gossypol.
- Si, Tengda,Li, Bowen,Xiong, Wenrui,Xu, Bin,Tang, Wenjun
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supporting information
p. 9903 - 9909
(2017/12/12)
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- A novel anti-Alzheimer agent inhibiting oligomerization and fibriliation of beta-amyloid protects neuronal cell from Aβ-induced cytotoxicity
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The present invention relates to development of a novel treatment agent for Alzheimerandprime;s disease, having ability of protecting neural cells and inhibiting fibrosis and oligomerization of beta-amyloid. A compound of the present invention is capable of, while maintaining therapeutic effects on Alzheimerandprime;s disease, recovering ability of directly inhibiting oligomerized and fibrous amyloid beta, which is inherent activities of existing curcumin, thereby being useful as a novel inhibitor.COPYRIGHT KIPO 2017
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Paragraph 0058; 0059
(2017/04/25)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Paragraph 0184
(2016/10/06)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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Page/Page column 42
(2016/11/07)
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- A Mild and Selective Method for the Catalytic Hydrodeoxygenation of Cyanurate Activated Phenols in Multiphasic Continuous Flow
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A low-energy, high-selectivity approach to the catalytic hydrodeoxygenation of phenols is reported using batch or continuous flow methods to react 3 equiv of phenol with cyanuric chloride then hydrogenolyzing the triarylcyanurate intermediate to give 3 equiv of deoxo aromatic. The use of cyanuric chloride compares favorably with existing activation methods, showing improved scalability, atom efficiency, and economics. The scope of both the activation and hydrogenolysis stages are explored using lignin-related phenols. Initial development has identified that continuous stir tank reactors (CSTRs) enable a multiphasic process for converting guaiacol to anisole and at steady state overcome the catalyst deactivation issues observed in batch, seemingly caused by the cyanurate byproduct. Green chemistry aspects and the potential for industrial adoption are discussed.
- Zhao, Yuhan,King, Georgina,Kwan, Maria H.T.,Blacker, A. John
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supporting information
p. 2012 - 2018
(2017/02/10)
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- As opioid receptor antagonists or inverse agonists of the novel compounds
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Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
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Paragraph 0609-0611
(2016/10/08)
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- I. Discovery of a novel series of CXCR3 antagonists. Multiparametric optimization of N,N-disubstituted benzylamines
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N,N-Disubstituted benzylamine derivatives have been identified as CXCR3 antagonists. Compounds were optimized to improve affinity and selectivity, to increase metabolic stability in human and mouse liver microsomes, to increase Caco-2 permeability. Optimization was supported by monitoring physico-chemical properties using both experimental and computational means. Several compounds with double-digit nanomolar CXCR3 affinity, favorable selectivity, microsomal stability, Caco-2 permeability and human hepatocyte clearance have been identified.
- Bata, Imre,T?m?sk?zi, Zsuzsanna,Buzder-Lantos, Péter,Vasas, Attila,Szeleczky, Gábor,Bátori, Sándor,Barta-Bodor, Veronika,Balázs, László,Ferenczy, Gy?rgy G.
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supporting information
p. 5418 - 5428
(2016/11/11)
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- Dicyanovinyl-substituted J147 analogue inhibits oligomerization and fibrillation of β-amyloid peptides and protects neuronal cells from β-amyloid-induced cytotoxicity
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A series of novel J147 derivatives were synthesized, and their inhibitory activities against β-amyloid (Aβ) aggregation and toxicity were evaluated by using the oligomer-specific antibody assay, the thioflavin-T fluorescence assay, and a cell viability assay in the transformed SH-SY5Y cell culture. Among the synthesized J147 derivatives, 3j with a 2,2-dicyanovinyl substituent showed the most potent inhibitory activity against Aβ42 oligomerization (IC50 = 17.3 μM) and Aβ42 fibrillization (IC50 = 10.5 μM), and disassembled the preformed Aβ42 fibrils with an EC50 of 10.2 μM. Finally, we confirmed that 3j is also effective at preventing neurotoxicity induced by Aβ42-oligomers as well as Aβ42-fibrils.
- Kim, Kyoungdo,Park, Kwang-Su,Kim, Mi Kyoung,Choo, Hyunah,Chong, Youhoon
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supporting information
p. 9564 - 9569
(2015/09/28)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kirl.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Page/Page column 70
(2014/07/08)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula(I) or a pharmaceutically acceptable salt thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure, kidney disease, edema, and conditions associated with excessive salt and water retention.
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Page/Page column 45
(2014/09/03)
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- An iterative in silico and modular synthetic approach to aqueous soluble tercyclic α-helix mimetics
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Tercyclic scaffolds, designed to have improved synthetic accessibility and aqueous solubility, were evaluated as structural α-helix mimetics by using an iterative in silico approach. The synthesis of these tercyclic scaffolds was accomplished using a modular synthetic approach by employing functionalised methoxyphenyl units which were readily manipulated to allow the introduction of various nitrogen-based heterocycles. The ability of these scaffolds to mimic the key i, i + 3 and i + 7 residues of a polyalanine α-helix was ratified by in silico studies, X-ray crystallographic and NOESY analysis, and their aqueous solubility was measured by a kinetic turbidimetric method. the Partner Organisations 2014.
- Lim, Zelong,Duggan, Peter J.,Meyer, Adam G.,Tuck, Kellie L.
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p. 4432 - 4444
(2014/06/23)
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- Selective deoxygenation of hydroxybenzaldehydes
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A method for selective deoxygenation of hydroxybenzaldehydes including, condensing syringaldehyde (3,5-dimethoxy-4-hydroxybenzaldehyde) and a functionalized phenylacetic acid with at least one first base and at least one anhydride to produce an arylcinnamic acid, decarboxylating of said arylcinnamic acid with at least one decarboxylation catalyst at temperatures ranging from about 30° C. to 200° C. or thermally at temperatures ranging from about 100° C. to 350° C. to produce a first stilbene, hydrodeoxygenating the stilbene by conversion to a sulfonate in the presence of at least one second base in water or at least one organic solvent to yield a sulfonate reducing the sulfonate(s) with a reductive elimination catalyst to produce a second stilbene, and reacting the second stilbene with a hydrolyzing agent to generate a polyphenol.
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Page/Page column 7-8
(2015/01/07)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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Page/Page column 80
(2013/03/26)
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- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
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Paragraph 0571; 0572
(2013/11/05)
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- Cycloalkane carboxylic acid derivatives as CXCR3 receptor antagonists
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Paragraph 0075; 0076
(2013/06/27)
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- CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Page/Page column 46
(2013/06/27)
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- Substituted B-amino acid derivatives as CXCR3 receptor antagonist
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Paragraph 0076; 0077
(2014/01/07)
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- SUBSTITUTED ?-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.
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Page/Page column 45; 46
(2014/01/07)
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- NOVEL DIHYDROPYRIDIN-2(1H)-ONE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS AND NEUROKININ-3 RECEPTOR ANTAGONISTS
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The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
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Page/Page column 49
(2012/02/02)
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- METHOD FOR TREATMENT OF BRONCHIAL ASTHMA
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The present invention relates to a method for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising administering to the patient suffering from asthama and COPD an effective dose of carbazole derivatives or salt the
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Page/Page column 5
(2012/08/27)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure
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Page/Page column 57
(2010/11/18)
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- (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES
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The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 26-27
(2010/12/31)
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- Syntheses of macrocyclic bis(bibenzyl) compounds derived from perrottetin e
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Macrocyclic bis(bibenzyl) compounds are natural products from liverworts and are of growing interest due to recent reports on new isolated compounds and on their remarkable biological activities. We report here on a flexible and general approach to the to
- Speicher, Andreas,Groh, Matthias,Hennrich, Markus,Huynh, Anh-Minh
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experimental part
p. 6760 - 6778
(2011/03/18)
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- NOVEL ANTI-INFLAMMATORY AGENTS
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Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.
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Page/Page column 127-129
(2010/11/05)
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- (DIHYDRO) IMIDAZOISO (5, 1-A) QUINOLINES AS FSH RECEPTOR AGONISTS FOR THE TREATMENT OF FERTILITY DISORDERS
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The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula (1) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
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Page/Page column 55-56
(2010/12/26)
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- Ring strain and total syntheses of modified macrocycles of the isoplagiochin type
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Macrocycles of the bisbibenzyl-type are natural products that are found exclusively in bryophytes (liverworts). The molecular framework of the subtype "isoplagiochin" is of substantial structural interest because of the chirality of the entire molecule, w
- Speicher, Andreas,Backes, Timo,Hesidens, Kerstin,Kolz, Juergen
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supporting information; experimental part
(2010/04/22)
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- Compounds with medicinal effects due to interaction with the glucocorticoid receptor
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The invention provides for compounds having the structure according to the formula I
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Page/Page column 15-16
(2010/11/27)
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- Purinenucleoside derivative modified in 8-position and medical use thereof
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The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
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Page/Page column 23
(2010/11/28)
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- ISOXAZOLINE-SUBSTITUTED BENZAMIDE COMPOUND AND NOXIOUS ORGANISM CONTROL AGENT
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An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A 1 , A 2 and A 3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., X is halogen atom, C 1 -C 6 haloalkyl, etc., Y ia halogen atm, C 1 -C 6 alkyl, etc., R 1 is C 1 -C 12 alkyl arbitrarily substituted with R 16 , C 3 -C 12 alkenyl, arbitrarily substituted with R 16 is oxygen atom or sulfur atom, -N(R 20 )R 19 , etc., R 2 is hydrogen atom, C 1 -C 4 alkoxy C 1 -C 6 alkyl, etc., R 3 is C 1 -C 6 haloalkyl, etc., R 16 is halogen atom, cyano, phenyl substituted with (Z) p1 , D-1 to D-60, E-1 to E-49, etc., R 19 is phenyl, phenyl substituted with (Z) p1 , etc., R 20 is hydrogen atom, C 1 -C 6 alkyl, etc., Z is halogen atom, nitro, C 1 -C 4 alkoxy, etc., D-1 to D-60 are 5- or 6-membered aromatic heterocyclic rings, E-1 to E-49 are 5- or 6-membered saturated heterocyclic rings, m is an integer of 0 to 5, n is an integer of 0 to 4, p1 is an integer of 1 to 5. The pesticide containing these compounds.
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Page/Page column 241
(2008/06/13)
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- HELIX 12 DIRECTED STEROIDAL PHARMACEUTICAL PRODUCTS
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Compounds having the structure or their salts: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Some of these compounds having tissue-specific antiandrogenic activity and tissue-specific androgenic activity can be used to treat or reduce the risk of developing diseases related to loss of androgenic stimulation. Combinations with other active pharmaceutical agents are also disclosed.
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Page/Page column 161
(2010/02/12)
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- Novel tricyclic pyridyl carboxamides and derivatives thereof tocolytic oxytocin receptor antagonists
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This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
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- Novel tricyclic diazepines tocolytic oxytocin receptor antagonists
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This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
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- Certain thiol inhibitors of endothelin-converting enzyme
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Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.
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- Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure - Activity relationship of substituents on the benzene ring of the cinnamide
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We have shown that p-arylthio cinnamides can inhibit the interaction of LFA-1 and ICAM-1, which is involved in cell adhesion and the inflammatory process. We now show that 2,3-disubstitution on the aryl portion of the cinnamide results in enhanced activit
- Winn,Kester,Von Geldern,Leitza,Devries,Dickinson,Mussatto,Okasinski,Reilly,Liu,Huth,Jae,Freeman,Pei,Xin,Lynch
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p. 4393 - 4403
(2007/10/03)
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- 1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists
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Phenylalkylamines such as 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB; 1a) and its corresponding iodo derivative DOI (2) are commonly used 5-HT2 serotonin agonists. Previous studies have established that the 2,5-dimethoxy substitution p
- Dowd,Herrick-Davis,Egan,DuPre,Smith,Teitler,Glennon
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p. 3074 - 3084
(2007/10/03)
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- Synthesis of 2-phenylbenzofuran derivatives as testosterone 5α- reductase inhibitor
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A series of 2-phenylbenzofuran derivatives with a carbamoyl, alkylamino, or alkyloxy group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. Against rat enzyme, the carbamoyl derivatives had more potent inhibitory activities than the alkylamino or alkyloxy derivatives, and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl derivatives. Against human enzyme, the 6-substituted derivatives had more potent inhibitory activities than the 5-substituted derivatives. The 6-carbamoyl and 6-alkylamino derivatives tended to show stronger inhibitory activities against human type 1 enzyme than against type 2 enzyme, but they were not largely selective.
- Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Sugiyama, Mitsuo,Hamada, Takakazu,Horikoshi, Hiroyoshi,Nishi, Takahide
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p. 226 - 240
(2007/10/03)
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- Synthesis and 5α-reductase inhibitory activities of benzofuran derivatives with a carbamoyl group
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A series of 2-phenylbenzofuran derivatives with a diphenylmethylcarbamoyl group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5α-reductase inhibitory activities in vitro. They had inhibitory activities against both enzymes and the 6-carbamoyl derivatives tended to be more potent than the 5-carbamoyl compounds.
- Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Sugiyama, Mitsuo,Hamada, Takakazu,Horikoshi, Hiroyoshi,Nishi, Takahide
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p. 561 - 566
(2007/10/03)
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