291758-01-5

Upstream product

• 291757-98-7 4-bromo-2-(3-methoxy-benzyl)-5-phenyl-2H-pyrazole-3-carboxylic acid ethyl ester 
• 179110-53-3 5-ethoycarbonyl-4-bromo-3-phenylpyrazole 
• 13599-12-7 ethyl 3-phenyl-1H-pyrazole-5-carboxylate 
• 179110-31-7 ethyl beta-benzoyl 6-chloro alpha-oxo-1,3-benzodioxol 5-butanoate 
• 98-86-2 acetophenone 
• 6296-54-4 ethyl 2,4-dioxo-4-phenylbutyrate 
• 179110-36-2 4-(6-chloro-benzo[1,3]dioxol-5-ylmethyl)-5-phenyl-2H-pyrazole-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Nonpeptide endothelin antagonists: From lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids

Random screening of compounds in endothelin receptor (ET(A) and ET(B)) binding assays led to the discovery of a new class of pyrazol-5-ol ligands. Characterization of structural features crucial for binding activities of these pyrazol-5-ols, by structure-activity-relationship (SAR) studies, allowed us to design a novel class of pyrazole-5-carboxylic acids as more potent ET antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.

Potent nonpeptide endothelin antagonists: Synthesis and structure-activity relationships of pyrazole-5-carboxylic acids

We have previously reported the identification of pyrazole-5-carboxylic acids as a new class of endothelin antagonists from low affinity pyrazol-5-ol ligands, which were obtained by random screening assays.1 We describe herein the synthesis and the structure-activity relationships (SARs) of these pyrazole-5-carboxylic acids with potent ET(A) selective, mixed ET(A)/ET(B) or moderately ET(B) selective antagonist activities. (C) 2000 Elsevier Science Ltd.