Alan Charles Tinker

1,2-diaminobenzimidazoles : Selective inhibitors of nitric oxide synthase derived from aminoguanidine

Abstract The synthesis of a series of novel 1,2-diaminobenzimidazoles is described. While the parent compound 4a is a weak, modestly selective inhibitor of the induced isoform of nitric oxide synthase (both mouse and human), a small structural change led to compound 5, a highly selective inhibitor of neuronal enzyme.

New non-peptide angiotensin II receptor antagonists. 1: structure - activity relationships of a series of a series of 2(1H)-pyridinones.

Abstract The synthesis and angiotensin II antagonist activity of biphenyl tetrazole substituted fused bicyclic analogues of 2-pyridinone is described. Potent antagonist activity was found in the 2-quinolinone, thieno[2,3-b] pyridine and imidazo[c]pyridine series.