- NOVEL COMPOUNDS AS NADPH OXIDASE INHIBITORS
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The present invention is related to new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
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Paragraph 0291; 0292
(2020/04/09)
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- 5-Bromo-1-(4-chlorobenzyl)-1h-indole-2-carboxamides as new potent antibacterial agents
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Ten 5-bromoindole-2-carboxamides were synthesized, characterized and evaluated for antibacterial activity against pathogenic Gram-negative bacteria Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa and Salmonella Typhi using gentamicin and ciprofloxacin as internal standards. Compounds 7a-c, 7g and 7h exhibit high antibacterial activity with a minimum inhibitory concentration (MIC) of 0.35-1.25 μg/mL. Compounds 7a-c exhibit antibacterial activities that are higher than those of the standards against E. coli and P. aeruginosa.
- Mane, Yogesh D.,Patil, Smita S.,Biradar, Dhanraj O.,Khade, Bhimrao C.
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p. 327 - 332
(2018/11/27)
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- Lewis Acid Catalyzed Annulation of Cyclopropane Carbaldehydes and Aryl Hydrazines: Construction of Tetrahydropyridazines and Application Toward a One-Pot Synthesis of Hexahydropyrrolo[1,2- b]pyridazines
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In this report, a facile synthesis of tetrahydropyridazines via a Lewis acid catalyzed annulation reaction of cyclopropane carbaldehydes and aryl hydrazines has been demonstrated. Moreover, the generated tetrahydropyridazine further participated in a cycloaddition reaction with donor-acceptor cyclopropanes to furnish hexahydropyrrolo[1,2-b]pyridazines. We also performed these two steps in one pot in a consecutive manner. In addition, a monodecarboxylation reaction of hexahydropyrrolo[1,2-b]pyridazine was achieved with a good yield.
- Dey, Raghunath,Kumar, Pankaj,Banerjee, Prabal
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p. 5438 - 5449
(2018/05/28)
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- Design, synthesis, and antimicrobial activity of novel 5-substituted indole-2-carboxamide derivatives
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Abstract: A series of novel, bioactive 5-substituted indole-2-carboxamide derivatives (10a–t and 14a–k) are synthesized by the coupling of 5-substituted indole-2-carboxylic acids with various amines in the presence of EDC HCl/HOBt in DMF/CH2Cl2 as a solvent. In vitro, antibacterial activity of titled compounds against pathogenic bacteria Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi and antifungal activity against pathogenic fungi Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, and Candida parapsilosis are evaluated using gentamicin/ciprofloxacin and fluconazole/oxiconazole as standard drugs, respectively. The majority of the synthesized compounds exhibited good antibacterial activity, but surprisingly none showed antifungal activity. Compounds 10c, 10d, 10i, 10j, 10l–n, 14g, 14h, 14i, 14j, and 14k exhibited high inhibitory antibacterial activity with MIC values in the range of 0.12–6.25?μg/mL. Interestingly, compounds 14i, 14j, and 14k exhibited excellent antibacterial activity against K. pneumoniae and E. coli compare to synthesized compound. All the experimental results promote us to consider this series as a starting point for the development of novel and more potent antibacterial agents in the future. Graphical Abstract: [Figure not available: see fulltext.]
- Mane, Yogesh D.,Sarnikar, Yuvaraj P.,Surwase, Santosh M.,Biradar, Dhanraj O.,Gorepatil, Pratapsinha B.,Shinde, Vishnu S.,Khade, Bhimrao C.
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p. 1253 - 1275
(2017/02/10)
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- Synthesis and biological evaluation of benzimidazole phenylhydrazone derivatives as antifungal agents against phytopathogenic fungi
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A series of benzimidazole phenylhydrazone derivatives (6a-6ai) were synthesized and characterized by 1H-NMR, ESI-MS, and elemental analysis. The structure of 6b was further confirmed by single crystal X-ray diffraction as (E)-configuration. All the compounds were screened for antifungal activity against Rhizoctonia solani and Magnaporthe oryzae employing a mycelium growth rate method. Compound 6f exhibited significant inhibitory activity against R. solani and M. oryzae with the EC50 values of 1.20 and 1.85 μg/mL, respectively. In vivo testing demonstrated that 6f could effectively control the development of rice sheath blight (RSB) and rice blast (RB) caused by the above two phytopathogens. This work indicated that the compound 6f with a benzimidazole phenylhydrazone scaffold could be considered as a leading structure for the development of novel fungicides.
- Wang, Xing,Chen, Yong-Fei,Yan, Wei,Cao, Ling-Ling,Ye, Yong-Hao
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- Synthesis of benzofuro[3,2-b] indoline amines via deamination-interrupted Fischer indolization and their unexpected reactivity towards nucleophiles
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We report the access to the benzofuro[3,2-b]indoline framework of phalarine from benzofuran-2-ones via the Fischer indolization reaction which was interrupted at the deamination step. Unexpectedly, allyl nucleophiles did not add to the aminal position of these benzofuro[3,2-b]indoline amines but to the adjacent ring junction center in the presence of trifluoroborane to deliver 3,3-disubstituted indolines containing a difluoroboron-containing six-membered ring with fluorescence properties.
- Tomakinian, Terry,Guillot, Régis,Kouklovsky, Cyrille,Vincent, Guillaume
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supporting information
p. 5443 - 5446
(2016/05/09)
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- MULTICYCLIC COMPOUND INCLUDING NITROGEN AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME
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The present invention relates to a nitrogen-containing polycyclic compound and an organic light emitting device including the same. According to an embodiment of the present invention, the nitrogen-containing polycyclic compound can be used to form an organic layer in the organic light emitting device.COPYRIGHT KIPO 2015
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Paragraph 0115-0118
(2016/10/08)
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- Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase
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In order to explore the interactions of bisphosphonate ligands with the active site and an allosteric pocket of the human farnesyl pyrophosphate synthase (hFPPS), substituted indole and azabenzimidazole bisphosphonates were designed as chameleon ligands. NMR and crystallographic studies revealed that these compounds can occupy both sub-pockets of the active site cavity, as well as the allosteric pocket of hFPPS in the presence of the enzyme's Mg2+ ion cofactor. These results are consistent with the previously proposed hypothesis that the allosteric pocket of hFPPS, located near the active site, plays a feed-back regulatory role for this enzyme.
- Gritzalis, Dimitrios,Park, Jaeok,Chiu, Wei,Cho, Hyungjun,Lin, Yih-Shyan,De Schutter, Joris W.,Lacbay, Cyrus M.,Zielinski, Michal,Berghuis, Albert M.,Tsantrizos, Youla S.
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supporting information
p. 1117 - 1123
(2015/02/19)
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- Remazol-Catalyzed Hydroperoxyarylation of Styrenes
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A mild photocatalytic hydroperoxyarylation of styrenes has been developed, in which a novel photocatalyst, remazol brilliant blue R (RBBR), is employed at low catalytic loading (1 mol%). The operationally easy procedure uses air as the dioxygen source. Simple mono-substituted styrenes react with aryl hydrazines in moderate-to-good yields. RBBR is proposed to act as a photosensitizer for the generation of singlet oxygen.
- Chen, Ying-Ho,Lee, Ming,Lin, Yi-Zhen,Leow, Dasheng
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supporting information
p. 1618 - 1621
(2015/08/06)
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- Design, synthesis and photophysical properties of A-D-A-D-A small molecules for photovoltaic application
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A series of linear-conjugated small molecule compounds featured with the acceptor-donor-acceptor-donor-acceptor (A-D-A-D-A) structure were designed, synthesized and characterized. The films of the compounds showed a broad UV-Vis absorption range of 300-800 nm with high molar absorption coefficient of more than 1.0 × 104 cm-1. Their hole-mobility can be as high as 1.0 × 10-3 cm2 V-1 s-1. The compounds have a compatible HOMO energy level of -5.0 eV to PC71BM and a high solubility up to 20 mg mL-1 in chloroform. Therefore, compounds can blend with PC71BM in the chloroform and form an active layer for a photovoltaic cell device by spin-coating of the blend solution. A maximum power conversion efficiency of 3.2% was achieved with the DERH3TT solar cell device. These results indicate that the A-D-A-D-A small molecules with electron-withdrawing dyes as terminals are promising candidates for the high efficiency solution processed organic photovoltaic cells.
- Yan, Weibo,Zhang, Qian,Qin, Qingsong,Ye, Senyun,Lin, Yuanwei,Liu, Zhiwei,Bian, Zuqiang,Chen, Yongsheng,Huang, Chunhui
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- Gold(I)-catalyzed rearrangement of alkynylaziridine indoles for the synthesis of spiro-tetrahydro-β-carbolines
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Functionalized spiro-tetrahydro-β-carbolines were formed by an efficient gold(I)-catalyzed rearrangement reaction of alkynylaziridine indoles. The reaction involved a Friedel-Crafts type intramolecular reaction of alkynylaziridine indoles, following by hydroamination of aminoallene intermediate.
- Yang, Yan-Fang,Li, Lian-Hua,He, Yu-Tao,Luo, Jian-Yi,Liang, Yong-Min
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p. 702 - 707
(2014/02/14)
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- GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 116; 117
(2014/10/03)
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- DIHYDROPYRAZOLE GPR40 MODULATORS
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The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
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Paragraph 00257
(2014/06/11)
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- Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors
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A series of novel 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b] indoles was synthesized through a newly developed approach. All these compounds were evaluated against DYRK1A, CDK5 and PI3Kα and showed promising inhibitory activities against PI3Kα with most IC50 values in the micromolar range. Among them, compound 18 was strongly considered as the most interesting compound with an IC50 value of 0.091 μM. This series exhibited also significant anti-proliferative effects in various human cancer cell lines including those resulting in activation of the PI3K pathway.
- Bruel, Amélie,Logé, Cédric,Tauzia, Marie-Ludivine De,Ravache, Myriam,Le Guevel, Rémy,Guillouzo, Christiane,Lohier, Jean-Fran?ois,Oliveira Santos, Jana Sopkova-De,Lozach, Olivier,Meijer, Laurent,Ruchaud, Sandrine,Bénédetti, Hélène,Robert, Jean-Michel
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p. 225 - 233
(2013/01/15)
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- Indole-phenylsulfonamide derivatives used as ppar-delta activating compounds
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The invention relates to novel indole-phenylfulfonamide derivatives, to methods for the production thereof, and to their use in medicaments, particularly as potent PPAR-delta activating compounds, for the prevention and/or treatment of cardiovascular diseases, particularly dyslipidemias and coronary heart diseases.
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- PIPERIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS
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A novel piperidine derivative represented by the formula (I) (I) wherein Ar is a phenyl group optionally having substituent(s), R?1? is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is a methylene group optionally having C?1-6#191 alkyl group(s), ring A is a piperidine ring optionally further having substituent(s), and B is a monocyclic aromatic heterocyclic group optionally having substituent(s) (substituents of monocyclic aromatic heterocycle may be bonded to each other to form a ring), or a salt thereof has a superior tachykinin receptor antagonistic action and the like, and is useful as an agent for the prophylaxis or treatment of lower urinary tract disease and the like.
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Page/Page column 87-88
(2010/11/28)
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- MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED WITH 5-MEMBERED HETEROCYCLES
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The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes (Formula (I)). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
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Page/Page column 25
(2008/06/13)
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- INDOLE-PHENYLSULFONAMIDE DERIVATIVES USED AS PPAR-DELTA ACTIVATING COMPOUNDS
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The invention relates to novel indole-phenylsulfonamide derivatives, to methods for the production thereof, and to their use in medicaments, particularly as potent PPAR-delta activating compounds, for the prevention and/or treatment of cardiovascular diseases, particularly dyslipidemias and coronary heart diseases.
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Page/Page column 30; 37-38
(2010/02/07)
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- Novel chemoselective reduction of aryldiazonium fluoroborates with Zn- NiCl2·6H2O-THF
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Substituted aryldiazonium fluoroborates are selectively reduced to the corresponding phenylhydrazines by using Zn-NiCl2·6H2O in THF as a reducing agent.
- Bandgar,Uppalla
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p. 714 - 715
(2007/10/03)
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- Selective reduction of aryl diazonium fluoroborates
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Substituted aryl diazonium fluoroborates have been selectively reduced to the corresponding phenylhydrazines by using borohydride exchange resin (BER).
- Bandgar,Thite
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p. 635 - 639
(2007/10/03)
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- Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine
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Pyrazolo[3,4-d]pyrimidines are pyrazolo analogues of purines. They have been shown to be a general class of compounds which exhibit A1 adenosine receptor affinity. Two series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine have been synthesized. The first involved substitution of the N1-position while the second involved substitution of the N5-position. Both alkyl and aryl substituents were examined. All compounds were tested for A1 adenosine receptor affinity by using a (R)-[3H]-N6-(phenylisopropyl)adenosine binding assay. The 3-chlorophenyl group showed the greatest activity in the N1-position and the butyl group produced the greatest activity in the N5-position. Combination of the best substituent in each of these positions enhanced the overall activity. The most potent compound was 4-amino-5-N-butyl-1-(3-chlorophenyl)-1H-pyrazolo[3,4-d] pyrimidin-6(5H)-one with an IC50 of 6.4 X 10-6 M. Selectivity at the receptor subclasses was examined by performing an A2 adenosine receptor affinity assay with [3H]CGS 21680. This series of compounds were slightly less potent at A2 receptors. 4-Amino-5-N-butyl-1-(3-chlorophenyl)-1H-pyrazolo[3,4-d] pyrimidin-6(5H)-one was the most potent compound with an IC50 of 19.2 X 10-6 M.
- Harden,Quinn,Scammells
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p. 2892 - 2898
(2007/10/02)
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- Reduction electrochimique des sels d'aryldiazonium en milieu aqueux: II. Effet de substituants sur la stabilisation du radical libre intermediaire de reduction et sur le rendement de la synthese d'arylhydrazines primaires
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The polarographic behaviour of a series of aromatic diazonium salts , BF4- in aqueous media is reported and discussed.The half-wave potentials corresponding to the first reduction step have been correlated to Hammett substituent constant ? and are defined by the equation : E=0.14?-0.015+/-0.01 V vs SCE.Substituent effects on the yield of electrochemical synthesis on a mercury pool of by electrochemical reduction of aryldiazoniums salts 10E-3 mol.l-1 at 0 1,1 V vs.SCE are also investigated at low temperature.The best yield (70percent) are obtained with the electron donating substituents on the phenyl ring.Unfortunately, large scale electrolytic reduction of aromatic diazoniums 10E-2 mol.l-1 at -1,1 V vs SCE results in the formation of primary hydrazines in poor yields.On such a large scale, it no longer seems possible to minimize the competitive chemical side reactions.
- Hamet-Elfakir, Claire,Caullet, ClAude
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p. 687 - 692
(2007/10/02)
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- Antiimplantation Agents: Part I - 1-Arylthiosemicarbazides
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Several 1-arylthiosemicarbazides, 2-arylhydrazinothiazolines and 2-arylhydrazinodihydrothiazines have been examined for their antiimplantation activity in rats.Among the active compounds, 4-methyl-1-(3,5-bistrifluoromethylphenyl)thiosemicarbazide (3, C 2696-Go) and the corresponding 4,4-dimethyl (47), ethyl (4), n-butyl (5) and allyl (6) derivatives completely inhibit implantation at doses 10, 3, 20, 20 and 30 mg/kg respectively.The 3,4-dichlorophenyl analogue (32) is effective at a dose of 30 mg/kg. 2-(3,5-Bistrifluoromethylphenyl)hydrazinothiazoline (51) and the corresponding dihydrothiazine (63) show a weaker activity.The biological profile of C 2696-Go has been investigated in detail.It appears to prevent implantation by its antiuterotropic activity and ability to inhibit desiduoma formation.
- Nagarajan, K.,Talwalker, P.K.,Kulkarni, C.L.,Venkateswarlu, A.,Prabhu, S.S.,Nayak, G.V.
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p. 1243 - 1257
(2007/10/02)
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- Pyrazol-4-acetic acid compounds
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Pyrazol-4-acetic acid compounds, such as substituted pyrazol-4-acetic acid, its esters, amides, nitriles and their pharamaceutically acceptable salts and method for the preparation of these compounds are disclosed. The novel compounds are useful analgesics, anti-inflammatory, and antipyretics.
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- (Nitrofuryl)pyrazoles, their synthesis and use, and compositions containing them
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3-(5-Nitro-2-furyl)pyrazoles unsubstituted in the 5-position and 5-(5-nitro-2-furyl)pyrazoles unsubstituted in the 3-position are antimicrobials and disinfectants. The compounds are structurally represented by one of the formulae: STR1 wherein A is --CHO, --CN, --COOH, a protected or derived aldehyde group or a protected or derived carboxylic acid group; B is 5-nitro-2-furyl; R1 is --H, substituted or unsubstituted hydrocarbyl (saturated or unsaturated; acyclic, alicyclic or aromatic; or araliphatic); substituted or unsubstituted (cycloaliphatic or aromatic) heterocyclic or acyl (carboxylic or carbonic acid); R2 is --H; and n is a positive whole number of at most 2.
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- Process for producing 3-anilino-5-pyrazolones
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A process for producing a 3-anilino-5-pyrazolone which comprises reacting a β-anilino-β-alkoxy-acrylate with a hydrazine in the presence of a compound having a pKa of about 8 up to about 14.
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