4912-02-1Relevant academic research and scientific papers
Synthesis and selective inhibitory activity against human COX-1 of novel 1-(4-substituted-thiazol-2-yl)-3,5-di(hetero)aryl-pyrazoline derivatives
Carradori, Simone,Secci, Daniela,Bolasco, Adriana,De Monte, Celeste,Yá?ez, Matilde
, p. 973 - 979 (2012)
Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2-pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1-thiocarbamoyl-2- pyrazolines with the ethyl ester of α-bromo-pyruvic acid. The synthesized compounds were confirmed by spectroscopic data and assayed to evaluate their in vitro ability to inhibit both isoforms of human cyclooxygenase (hCOX). Some derivatives (compounds 5, 6, 13, 16, and 17) displayed promising selectivity against hCOX-1 in the micromolar range and were shown to have a selectivity index similar or better than the reference drugs (indometacin, diclofenac). The introduction of a phenyl or a 4-F-phenyl ring on the C5 associated with a 4-substituted phenyl or a heteroaryl group on the C3 of (4-substituted-thiazol- 2-yl)pyrazoline derivatives improved the activity against hCOX-1. Thanks to these preliminary results it could be possible to extend our knowledge of the pharmacophoric requirements for the discovery of new pyrazoline-based hCOX-1 inhibitors. Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2- pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1- thiocarbamoyl-2-pyrazolines with the ethyl ester of α-bromo-pyruvic acid. Some derivatives displayed promising selectivity against human cyclooxygenase 1 (hCOX-1) in the micromolar range, with a selectivity index similar or better than the reference drugs, indometacin and diclofenac. Copyright
Anti-bacterial and anti-leishmanial studies of 4, 6-diarylpyrimidin-2- amines
Bukhari, Mujahid Hussain,Siddiqui, Hamid Latif,Ashraf, Chaudhary Muhammad,Hussain, Tanvir
scheme or table, p. 720 - 725 (2012/06/18)
Seven new chalcones along with nine already reported ones were synthesized from aryl aldehydes and substituted acetophenones by Claisen-Schmidt condensation. Each chalcone was treated with guanidine hydrochloride followed by oxidation with H2O
Synthesis, pharmacological and biological screening of new isoxazolines
Ishwar Bhat,Anil Kumar,Kumar, Abhishek
, p. 163 - 166 (2013/09/24)
A new series of 3-(substituted phenyl)-5-(1 H-pyrrol-2-yl)-2,3- dihydroisoxazoles (Al1-Al10) have been synthesized by reacting various substituted chalcones with hydroxyl amine in presence of 2% NaOH. The intermediate chalcones were
