Discovery of inhibitors of plasminogen activator inhibitor-1: Structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives

Vrajesh Pandya, Mukul Jain, Ganes Chakrabarti, Hiteshkumar Soni, Bhavesh Parmar, Balaji Chaugule, Jigar Patel, Jignesh Joshi, Nirav Joshi, Akshyaya Rath, Mehul Raviya, Mubeen Shaikh, Kalapatapu V.V.M. Sairam, Harilal Patel, Pankaj Patel

Research output: Contribution to journalArticle

9 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)5701-5706
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number19
DOIs
StatePublished - Oct 1 2011

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Plasminogen Activator Inhibitor 1
Lead compounds
Derivatives
Acids
Biological Availability
Rodentia
piperazine
tiplaxtinin

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Discovery of inhibitors of plasminogen activator inhibitor-1 : Structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives. / Pandya, Vrajesh; Jain, Mukul; Chakrabarti, Ganes; Soni, Hiteshkumar; Parmar, Bhavesh; Chaugule, Balaji; Patel, Jigar; Joshi, Jignesh; Joshi, Nirav; Rath, Akshyaya; Raviya, Mehul; Shaikh, Mubeen; Sairam, Kalapatapu V.V.M.; Patel, Harilal; Patel, Pankaj.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 19, 01.10.2011, p. 5701-5706.

Research output: Contribution to journalArticle

Pandya, V, Jain, M, Chakrabarti, G, Soni, H, Parmar, B, Chaugule, B, Patel, J, Joshi, J, Joshi, N, Rath, A, Raviya, M, Shaikh, M, Sairam, KVVM, Patel, H & Patel, P 2011, 'Discovery of inhibitors of plasminogen activator inhibitor-1: Structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives', Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 19, pp. 5701-5706. https://doi.org/10.1016/j.bmcl.2011.08.031
Pandya, Vrajesh ; Jain, Mukul ; Chakrabarti, Ganes ; Soni, Hiteshkumar ; Parmar, Bhavesh ; Chaugule, Balaji ; Patel, Jigar ; Joshi, Jignesh ; Joshi, Nirav ; Rath, Akshyaya ; Raviya, Mehul ; Shaikh, Mubeen ; Sairam, Kalapatapu V.V.M. ; Patel, Harilal ; Patel, Pankaj. / Discovery of inhibitors of plasminogen activator inhibitor-1 : Structure-activity study of 5-nitro-2-phenoxybenzoic acid derivatives. In: Bioorganic and Medicinal Chemistry Letters. 2011 ; Vol. 21, No. 19. pp. 5701-5706.
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