NO-sartans: a new class of pharmacodynamic hybrids as cardiovascular drugs

  • J Med Chem. 2004 Nov 4;47(23):5597-600. doi: 10.1021/jm049681p.
Maria C Breschi  1 ,  Vincenzo Calderone ,  Maria Digiacomo ,  Alma Martelli ,  Enrica Martinotti ,  Filippo Minutolo ,  Simona Rapposelli ,  Aldo Balsamo
Affiliations
  • 1. Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
PMID: 15509155 DOI: 10.1021/jm049681p
Abstract

The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT1-antagonist and of a "slow NO donor", by adding NO-donor side chains to losartan. These new compounds, 2a and 2b, displayed vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of angiotensin II, with potency values similar to that of losartan. In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril.

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