A.M. Venkatesan

The synthesis of 2,3-dihydro-4(1H)-quinazolinone angiotensin II receptor antagonists

Abstract The synthesis and biological evaluation of a series of 2,3,-dihydro-4-(1H)-quinazolinone angiotensin II receptor antagonists is described.

An efficient method to prepare α-sulfonyl hydroxamic acid derivatives

Abstract α-Sulfonyl hydroxamic acid derivatives are biologically important molecules. An efficient protocol has been developed to make these molecules via a direct sulfonylation of enolates. Several piperidine containing α-sulfonyl hydroxamic acid compounds have been prepared by this procedure.

2,3,6-Substituted quinazolinones as angiotensin II receptor antagonists

Abstract The synthesis and biological evaluation of a series of 2,3,6-substituted 4(3H)quinazolinones is described. One of these compounds, CL329, 167, was found to be a potent, orally active, competitive angiotensin II receptor antagonist with a long duration of action.

6-Substituted quinazolinone angiotensin II receptor antagonists

Abstract 4(3H)-quinazolinones with a variety of heterocyclic substituents bound to the 6-position have been synthesized and evaluated as angiotensin II receptor antagonists both in vitro and in vivo. Some of these compounds have been shown to be potent, long-lasting, orally active antihypertensives.

6-isoxazolinyl and isoxazolidinyl substituted quinazolinones as angiotensin II receptor antagonists

Abstract The synthesis and biological evaluation of a series of 4(3H)-quinazolinones substituted at the 6-position with isoxazolines and isoxazolidines is described. Of these, compound 25a was found to be an especially potent, orally active, non-competitive angiotensin II receptor antagonist.

Substituted 4H-pyrido[1,2-a]pyrimidin-4-one angiotensin II receptor antagonists.

Abstract Several substituted 4H-pyrido[1,2-a]pyrimidin-4-ones have been synthesized and investigated as potential angiotensin II receptor antagonists.

Synthesis and biological evaluation of the potent isoxazolidinyl angiotensin II receptor antagonist CL332,877 and its enantiomers.

Abstract An alternative synthesis of CL332,877, a potent isoxazolidinyl-quinazolinone angiotensin II receptor antagonist, is described. In addition, the enantiomers of CL332,877 were separated and evaluated both in vitro and in vivo .