1214740-92-7

Upstream product

• 1072-83-9 2-Acetylpyrrole 
• 104-88-1 4-chlorobenzaldehyde 
• 79-19-6 thiosemicarbazide 
• 22563-58-2 3-(4-chloro-phenyl)-1-pyrrol-2-yl-propenone 

Downstream Products

• 1430116-76-9 C₁₉H₁₇ClN₄O₂S 

Relevant 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

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

Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives

A series of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives has been synthesized and assayed for their ability to inhibit the activity of the A and B isoforms of human monoamine oxidase (hMAO). Some of these compounds were endowed with a selective inhibitory activity against hMAO-B in the micromolar range. The most active of the series is the compound 13, N1-thiocarbamoyl-3-(fur-2′-yl)-5-(4′-fluoro-phenyl)-4,5-dihydro-(1H)-pyrazole, with IC50 2.75 ± 0.81 μM value and selectivity ratio of 25, which is the best candidate for further investigations.