- Inhibition of aromatase (P450Arom) by some 1-(benzofuran-2-ylmethyl)imidazoles.
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Studies of a series of 1-(benzofuran-2-ylmethyl)imidazoles, 1-5, previously proposed as potential agents for prostatic cancer by their inhibition of 17beta-hydroxylase:17,20-lyase (P450 17), have been extended to their selectivity against placental microsomal aromatase (P450(Arom)) in man. The compounds were 3-7-fold more potent than aminoglutethimide and had some selectivity for P450 17 as expressed by the ratio (IC50 P450(Arom))/(IC50 P450) 17)/17.0 (2), 10.3 (3), 34.6 (4) and 42.0 (5), where IC50 is the concentration resulting in 50% inhibition. The lower potency of 1-5 towards P450(Arom) compared with the racemic alpha-phenyl-substituted compounds (6, 80-1000 x aminoglutethimide) and some racemic alpha-methyl (8.5 and 12.2 x aminoglutethimide) and alpha-ethyl (12.1 and 32.9 x aminoglutethimide) analogues has been rationalized. This work selectively extends studies of the P450 17 inhibitor 5, a potential prostatic cancer agent, towards other cytochrome P450 enzymes in the steroidogenic pathway and provides a general method for determining the relative influence of chemical manipulation of a parent inhibitor towards two enzymes in the pathway using additional literature data.
- Owen,Nicholls,Smith,Whomsley
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Read Online
- Synthesis, characterization and antimicrobial activities of 1-((5-bromobenzofuran-2yl)methyl)-4-substituted phenyl-1H-1,2,3-triazoles
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A synthesis of useful intermediate, 2-(azidomethyl)-5-bromobenzofuran starting from 5-bromobenzofuran-2-carboxylic acid is described The reaction of 5-bromo-2-(iodomethyl)benzofuran with sodium azide affords 2-(azidomethyl)-5-bromobenzofuran. 5-Bromo-2 (i
- Sanjeeva,Subba Rao,Kamala Prasad,Venkata Ramana
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p. 565 - 569
(2021/02/27)
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- PROTEIN KINASE C AGONISTS
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The present disclosure relates generally to certain diacylglycerol lactone compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions dis
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Paragraph 0341
(2020/09/12)
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- 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds and preparation method thereof
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The invention discloses 2'-carbonyl-3-bromo-spiro[benzofuran-2, 4'-oxazolidine] compounds and a preparation method thereof. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive compounds shown in the structural formula II. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive spiro compounds, photoactive chiral spiro compounds with multiple functional groups substituted, such as photoactive chiral spiro compounds with azido groups, hydroxyl groups, allyl groups and anisole groups substituted, can be obtained through substitution reactions of bromine atoms at site 3 under different reaction conditions. Therefore, different kinds of other photoactive chiral spiro compounds are prepared by using the substitution reactions of bromine atoms, the range of the compounds is enlarged, and the potential application value is great.
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Paragraph 0144; 0146-0148
(2017/08/02)
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- Chromium-Catalyzed Asymmetric Dearomatization Addition Reactions of Halomethyl Heteroarenes
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The first asymmetric dearomatization addition reaction of halomethyl arenes including benzofuran and benzothiophene was enabled by chromium catalysis. A variety of aldehydes served as suitable electrophiles under mild reaction conditions. Molecular complexities are quickly increased in a highly diastereo- and enantioselective manner.
- Tian, Qingshan,Bai, Jing,Chen, Bin,Zhang, Guozhu
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supporting information
p. 1828 - 1831
(2016/05/19)
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- Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
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The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
- Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
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scheme or table
p. 5591 - 5593
(2009/06/18)
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- A study of the Claisen-Eschenmoser reaction for hydroxymethylbenzofurans and-indoles
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N,N-Dimethylacetamide dimethyl acetal reacted with 5(7)-substituted 2-(hydroxy-methyl)benzofurans to give N,N-dimethyl-2-(2-methylbenzofuran-3-yl) acetamides. Analogous reactions with 3-(hydroxymethyl)indole and 1-hydroxy-6-methyl-1,2,3,4-tetrahydro-carbazole afforded N,N-dimethyl-3-(3- indolyl)propionamide and N, N-dimethyl-2-(6-methyl-1,2,3,4-tetrahydrocarbazol-1- yl)acetamide, respectively.
- Mukhanova,Kukushkin,Ivanov,Alekseeva,Granik
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p. 325 - 329
(2008/02/13)
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- ANTIFUNGAL AGENT CONTAINING PYRIDINE DERIVATIVE
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The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or -NH-, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.
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Page/Page column 48
(2008/06/13)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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- Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
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This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
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Page/Page column 31
(2010/01/31)
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- Alkoxycarbonylamino benzoic acid or alkoxycarbonylamino tetrazolyl phenyl derivatives as IP antagonists
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This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1, and b2 and A and G2 are as defin
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- Benzopyran derivatives having leukotriene-antagonistic action
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The present invention relates to novel 4-oxo-4H-1-benzopyran compounds containing benzyloxymethyl, 3-phenylpropyl, or other araliphatic substituents in their 8-position. These compounds show a leukotriene-antagonistic activity. The compounds are characterized by good oral adsorption. The compounds of the present invention may be used as anti-inflammatory and antiallergic medicaments, and in the treatment of cardiovascular diseases.
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- Syntheses of Biscationic, Trypanocidal 1-Benzofuran Compounds
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2-Phenyl-1-benzofurans with the substituents Br, NO2, CN, and -NH2, -NH-C(=NH)-NH2, -C(=NH)-NH2, in 4',5-position were synthesized. - For arylated formamidine derivatives a simple new preparation was found by reacting amine hydrochlorides with dimethylformamide in the presence of cyanamide. - Based on 5- or 6-cyano-1-benzofuran-2-carboxylates a series of α,ω-bis(1-benzofuran-2-yl) derivatives with cyano-, amidino-, or imidazolinyl groups in 5- or 6-position was prepared.
- Dann, Otto,Char, Helmut,Griessmeier, Helmut
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p. 1836 - 1869
(2007/10/02)
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