4-methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4361-4. doi: 10.1016/j.bmcl.2003.09.043.
Patrick Angibaud  1 ,  Ashis K Saha ,  Xavier Bourdrez ,  David W End ,  Eddy Freyne ,  Patricia Lezouret ,  Geert Mannens ,  Laurence Mevellec ,  Christophe Meyer ,  Isabelle Pilatte ,  Virginie Poncelet ,  Bruno Roux ,  Gerda Smets ,  Jacky Van Dun ,  Marc Venet ,  Walter Wouters
Affiliations
  • 1. Medicinal Chemistry Department Johnson & Johnson Pharmaceutical Research & Development (J&JPRD), Campus de Maigremont BP615, 27106, Val de Reuil, France. [email protected]
PMID: 14643326 DOI: 10.1016/j.bmcl.2003.09.043
Abstract

Replacement of the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA series by a 4-methyl-1,2,4-triazol-3-yl group gave us compounds with similar structure-activity relationship profiles showing that this triazole is potentially a good surrogate to imidazole for farnesyltransferase inhibition.