Synthesis of 2-substituted-N-carboxymethyl-1,5-benzothiazepin-4-ones and -1,4-benzothiazin-3-ones and their evaluation as angiotensin converting enzyme inhibitors

G Trapani; A Latrofa; M Franco; G Liso

Synthesis of 2-substituted-N-carboxymethyl-1,5-benzothiazepin-4-ones and -1,4-benzothiazin-3-ones and their evaluation as angiotensin converting enzyme inhibitors

Farmaco. 1995 Feb;50(2):107-12.

Authors

G Trapani¹, A Latrofa, M Franco, G Liso

Affiliation

¹ Dipartimento Farmacochimico, Università di Bari.

PMID: 7766274

Abstract

The title compounds 7a-d and 8a-e were synthesized and their in vitro inhibitory activity of angiotensin-converting enzyme (ACE) was examined. In general, these compounds possess poor ACE inhibitory activity. Among the benzothiazinone compounds, which are generally more active than the cyclohomologous compounds 7, 8b is the most effective (IC50 of 170 microM).

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Angiotensin-Converting Enzyme Inhibitors / chemical synthesis*
Angiotensin-Converting Enzyme Inhibitors / chemistry
Angiotensin-Converting Enzyme Inhibitors / pharmacology
Captopril / pharmacology
Drug Evaluation
Spectrophotometry
Structure-Activity Relationship
Thiazepines / chemical synthesis*
Thiazepines / chemistry
Thiazepines / pharmacology

Substances

Angiotensin-Converting Enzyme Inhibitors
Thiazepines
Captopril