1428879-18-8

Basic information

• Product Name: C₁₉H₁₄FN₃O₂S
• CAS NO: 1428879-18-8
• Molecular Weight: 367.403
• Mol File: 1428879-18-8.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: C₁₉H₁₄FN₃O₂S(CAS DataBase Reference)
• NIST Chemistry Reference: C₁₉H₁₄FN₃O₂S(1428879-18-8)
• EPA Substance Registry System: C₁₉H₁₄FN₃O₂S(1428879-18-8)

Safety Data

• Hazardous Substances Data: 1428879-18-8(Hazardous Substances Data)

Upstream product

• 2920-38-9 4-cyano-1,1'-biphenyl 
• 149506-86-5 4'-cyano[1,1'-biphenyl]-4-sulfonyl chloride 
• 110919-71-6 2-amino-5-fluoro-6-methylpyridine 

Relevant articles and documents

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Strategies to eliminate reactive metabolites

N-(Pyridin-2-yl) arylsulfonamides 1 and 2 (PF-915275) were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1. A screen for bioactivation revealed that these compounds formed glutathione conjugates. This communication presents the results of a risk benefit analysis carried out to progress 2 (PF-915275) to a clinical study and the strategies used to eliminate reactive metabolites in this series of inhibitors. Based on the proposed mechanism of bioactivation and structure-activity relationships, design efforts led to N-(pyridin-2-yl) arylsulfonamides such as 18 and 20 that maintained potent 11β-hydroxysteroid dehydrogenase type 1 activity, showed exquisite pharmacokinetic profiles, and were negative in the reactive metabolite assay.