1580456-76-3

Upstream product

• 483366-11-6 (2S,4S)-4-fluoropyrrolidine-2-carbonitrile; 4-methylbenzene-1-sulfonic acid 
• 1580457-44-8 (2S)-2-[(tert-butoxycarbonyl)amino]-3-(2-(4-chlorophenyl)thiazol-4-yl)propanoic acid 
• 40216-83-9 L-4-hydroxyproline methyl ester hydrochloride 
• 74844-91-0 1-tert-butyl 2-methyl (2S,4R)-4-hydroxy-1,2-pyrrolidinedicarboxylate 
• 203866-16-4 1-tert-butyl 2-methyl (2S,4S)-4-fluoropyrrolidine-1,2-dicarboxylate 
• 203866-13-1 (2S,4S)-1-(tert-butoxycarbonyl)-4-fluoropyrrolidine-2-carboxylic acid 
• 426844-22-6 tert-butyl (2S,4S)-2-carbamoyl-4-fluoropyrrolidine-1-carboxylate 
• 426844-76-0 tert-butyl (2S,4S)-2-cyano-4-fluoropyrrolidine-1-carboxylate 
• 1580457-18-6 tert-butyl N-[(2S)-3-(2-(4-chlorophenyl)thiazol-4-yl)-1-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors

A series of novel hetero-aromatic moieties substituted α-amino pyrrole-2-carbonitrile derivatives was designed and synthesized based on structure-activity relationships (SARs) of pyrrole-2-carbonitrile inhibitors. All compounds demonstrated good dipeptidyl peptidase IV (DPP4) inhibitory activities (IC50 = 0.004-113.6 μM). Moreover, compounds 6h (IC50 = 0.004 μM) and 6n (IC50 = 0.01 μM) showed excellent inhibitory activities against DPP4, good selectivity (compound 6h, selective ratio: DPP8/DPP4 = 450.0; DPP9/DPP4 = 375.0; compound 6n, selective ratio: DPP8/DPP4 = 470.0; DPP9/DPP4 = 750.0) and good efficacy in an oral glucose tolerance test in ICR mice. Furthermore, compounds 6h and 6n demonstrated moderate PK properties (compound 6h, F% = 37.8%, t1/2 = 1.45 h; compound 6n, F% = 16.8%, t1/2 = 3.64 h).