2. Academic Validation
  3. Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents

Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents

  • Bioorg Med Chem Lett. 2014 Jan 15;24(2):560-4. doi: 10.1016/j.bmcl.2013.12.022.
Faith Mjambili 1,  Mathew Njoroge 1,  Krupa Naran 2,  Carmen De Kock 3,  Peter J Smith 3,  Valerie Mizrahi 4,  Digby Warner 4,  Kelly Chibale 5
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Cape Town, Private Bag X3, Rondebosch 7701, South Africa.
  • 2 MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Division of Medical Microbiology, Department of Clinical Laboratory Sciences, University of Cape Town, Rondebosch 7701, South Africa.
  • 3 Division of Pharmacology, Department of Medicine, University of Cape Town, K45, OMB, Groote Schuur Hospital, Observatory 7925, South Africa.
  • 4 MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Division of Medical Microbiology, Department of Clinical Laboratory Sciences, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
  • 5 Department of Chemistry, University of Cape Town, Private Bag X3, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address: kelly.chibale@uct.ac.za.
PMID: 24373723 DOI: 10.1016/j.bmcl.2013.12.022
Abstract

A series of compounds derived from the 2-amino-4-(2-pyridyl) thiazole scaffold was synthesized and tested for in vitro antimycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, antiplasmodial activity against the chloroquine sensitive NF54 Plasmodium falciparum strain and cytotoxicity on a mammalian cell line. Optimal antimycobacterial activity was found with compounds with a 2-pyridyl ring at position 4 of the thiazole scaffold, a substituted phenyl ring at the 2-amino position, and an amide linker between the scaffold and the substituted phenyl. The antiplasmodial activity was best with compounds that had the phenyl ring substituted with hydrophobic electron withdrawing groups.

Keywords

2-Amino-4-(2-pyridyl)thiazoles; Antimycobacterial; Antiplasmodial; Hit optimisation; Structure–activity relationship.

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