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

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

Affiliation

  • 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.

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