title: Discovery of inhibitors of plasminogen activator inhibitor-1: structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives.
abstract: Two novel series of 5-nitro-2-phenoxybenzoic acid derivatives are designed as potent PAI-1 inhibitors using hybridization and conformational restriction strategy in the tiplaxtinin and piperazine chemo types. The lead compounds 5a, 6c, and 6e exhibited potent PAI-1 inhibitory activity and favorable oral bioavailability in the rodents.
authors: Zydus Research Centre, Sarkhej-Bavla N.H. 8A, Moraiya, Ahmedabad 382 210, India. vrajeshpandya@zyduscadila.com
authors: Vrajesh
authors: V
authors: Pandya
authors: Mukul
authors: M
authors: Jain
authors: Ganes
authors: G
authors: Chakrabarti
authors: Hitesh
authors: H
authors: Soni
authors: Bhavesh
authors: B
authors: Parmar
authors: Balaji
authors: B
authors: Chaugule
authors: Jigar
authors: J
authors: Patel
authors: Jignesh
authors: J
authors: Joshi
authors: Nirav
authors: N
authors: Joshi
authors: Akshyaya
authors: A
authors: Rath
authors: Mehul
authors: M
authors: Raviya
authors: Mubeen
authors: M
authors: Shaikh
authors: Kalapatapu V V M
authors: KV
authors: Sairam
authors: Harilal
authors: H
authors: Patel
authors: Pankaj
authors: P
authors: Patel
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001565:Benzoates / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D004195:Disease Models, Animal; D015195:Drug Design; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D007210:Indoleacetic Acids / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D010647:Phenyl Ethers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry; D017395:Plasminogen Activator Inhibitor 1 / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013927:Thrombosis / Q000139:chemically induced / Q000188:drug therapy
chemical_list: D001565:Benzoates; D007210:Indoleacetic Acids; D010647:Phenyl Ethers; D010879:Piperazines; D017395:Plasminogen Activator Inhibitor 1; C488103:tiplaxtinin; D000077489:Piperazine