Literature DB >> 21804258

Synthesis of N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamides and their inhibitory activities against secretory phospholipase A₂.

Hitoshi Nakayama1, Keiichi Ishihara, Satoshi Akiba, Jun'ichi Uenishi.   

Abstract

N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamide derivatives 3-6 were prepared by the reaction of 3-pyridylamines and sulfonyl chlorides. Inhibitory activities of these compounds toward secretory phospholipase A₂ (sPLA₂) were examined and N-[2-(2,4-difluorophenoxy)-5-trifluoromethyl-3-pyridyl]-2-naphthalenesulfonamide (5c) was found to be the most potent against sPLA₂ with an IC₅₀ value of 90 µM.

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Year:  2011        PMID: 21804258     DOI: 10.1248/cpb.59.1069

Source DB:  PubMed          Journal:  Chem Pharm Bull (Tokyo)        ISSN: 0009-2363            Impact factor:   1.645


  2 in total

1.  Chemical validation of a druggable site on Hsp27/HSPB1 using in silico solvent mapping and biophysical methods.

Authors:  Leah N Makley; Oleta T Johnson; Phani Ghanakota; Jennifer N Rauch; Delaney Osborn; Taia S Wu; Tomasz Cierpicki; Heather A Carlson; Jason E Gestwicki
Journal:  Bioorg Med Chem       Date:  2021-01-24       Impact factor: 3.641

2.  Design and synthesis of quinazoline carboxylates against Gram-positive, Gram-negative, fungal pathogenic strains, and Mycobacterium tuberculosis.

Authors:  Theivendren Panneer Selvam; Arumugam Sivakumar; Padmavathi P Prabhu
Journal:  J Pharm Bioallied Sci       Date:  2014-10
  2 in total

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