Synthesis and Biological Activities of New 1,4-Benzothiazine Derivatives

Abstract

New 2H-l,4-benzothiazin-3(4H)-one derivatives possessing (4-phenyl-l-piperazinyl)alkyl moieties at the 2-position were synthesized and tested for calcium antagonistic and calmodulin antagonistic activities. Antihypertensive effects in spontaneously hypertensive rats were also evaluated. In general, these compounds were rather weak calcium channel blockers, although, in contrast, many of them had moderate to potent calmodulin antagonistic activity, and 2-[3-(4-(4-fluorophenyl)-l-piperazinyl]propyl]-2H-l,4-benzothiazin-3(4H)-one derivatives 45, 74 and 75 showed potent antihypertensive effects. © 1991, The Pharmaceutical Society of Japan. All rights reserved.