58386-33-7Relevant academic research and scientific papers
N-(piperidin-4-yl)-1H-indole-2-carboxamide derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating Urotensin-Ⅱ receptor activity related diseases containing the same as an active ingredient
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, (2017/05/18)
The present invention relates to N-(piperidin-4-yl)-1H-indole-2-carboxamide derivatives, a preparation method thereof, and a pharmaceutical composition for preventing or treating urotensin-II receptor activity-related diseases comprising the same as activ
Hydroxamic acids block replication of hepatitis c virus
Ai, Teng,Xu, Yanli,Qiu, Li,Geraghty, Robert J.,Chen, Liqiang
, p. 785 - 800 (2015/01/30)
Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be either relatively toxic or ineffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thiophen-2-hydroxamic acid gave rise to compounds 22 and 53, which showed potent and selective anti-HCV activity and therefore are promising starting points for further structural optimization and mechanistic studies.
Intramolecular reactions of 2-indolylacyl radicals: Cyclisation upon aromatic rings
Bennasar, M.-Llu?sa,Roca, Tomàs,Ferrando, Francesc
, p. 5605 - 5609 (2007/10/03)
The generation of 2-indolylacyl radicals from the corresponding selenoesters under reductive (tributyltin hydride-AIBN) and nonreductive (hexabutylditin, 300W) conditions and their behaviour in cyclisation reactions upon benzene rings attached either to t
Syntheses and biological evaluation of indole-2 and 3-carboxamides: New selective cyclooxygenase-2 inhibitors
Oelgen, Suereyya,Guener,Fabregat,Crespo,Nebioglu
, p. 238 - 242 (2007/10/03)
A series of indol-2 and 3-carboxamides were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1). Substitution on indol nitrogen with benzyl and p-fluorobenzyl group of indole-2 carboxamides 8, 10, 11 provides fairly active COX-2 enzyme inhibitors.
Synthesis and antioxidant properties of novel N-substituted indole-2-carboxamide and indole-3-acetamide derivatives
Oelgen, Suereyya,Coban, Tuelay
, p. 331 - 338 (2007/10/03)
A series of N-substituted indole-2-carboxamide and indole-3-acetamide derivatives have been prepared and their in vitro effects on rat liver lipid peroxidation levels and superoxide anion formation were determined. The results clearly demonstrate that indole derivatives 4, 5, 10, 15, 17 are very efficient antioxidants compared to α-toco-pherol.
Synthesis and receptor docking studies of N-substituted indole-2-carboxylic acid esters as a search for COX-2 selective enzyme inhibitors
Olgen, Sureyya,Akaho, Eiichi,Nebioglu, Dogu
, p. 747 - 770 (2007/10/03)
A series of N-substituted indole-2-carboxylic acid esters have been prepared by replacing the benzoyl group of indomethacin with a benzyl and a phenyl group. The carbocyclic acid side chain was extended via creating an ester structure by using several dialkylaminoalkyl groups. The receptor docking studies were performed to investigate the docking mode of each compound by using dock 4.0. All the compounds were shown to be docked at the site where intact flurbiprofen was embedded for COX-1 and s-58 (1-phenylsulphonamide-3-trifluoromethyl-5-para-bromophenylpyrazole) for COX-2. It was predicted that N-phenyl-indole-2-carboxylic acid piperazine ester 22 can be a fairly strong COX-2 selective compound which was compared to the others. Other predicted COX-2 selective compounds included are N-H indole-2-carboxylic acid diethyl 30 and piperazine 34 esters. In view of these findings, compounds 22, 30 and 34 were chosen for the in vitro biological assays.
