Volume 27, Issue 11
Heterocyclic Compounds
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ChemInform Abstract: 4-(Heteroarylthio)-2-biphenylyltetrazoles as Nonpeptide Angiotensin II Antagonists.

M. H. NORMAN

M. H. NORMAN

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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H. D. SMITH

H. D. SMITH

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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C. W. ANDREWS

C. W. ANDREWS

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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F. L. M. TANG

F. L. M. TANG

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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C. L. COWAN

C. L. COWAN

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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R. P. STEFFEN

R. P. STEFFEN

Div. Org. Chem., Burroughs Wellcome Co., Research Triangle Park, NC 27709, USA

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First published: March 12, 1996

Abstract

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ChemInform Abstract

A series of the title compounds (7 examples), such as (VIIa) and (VIIb) , are prepared and their ability to displace (3H)AII from angiotensin II receptors is investigated by comparing with already known antagonists (VIIIa) to (VIIIc). The most potent compounds (VIIa) and ( VIIb) exhibit also concentration-dependent reversal of angiotensin II contraction in rabbit isolated aortic rings. The effects of the novel sulfide bridging unit as well as changes in the heteroaromatic residue R on the biological activity are discussed.

chemical structure image

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