DESIGN, SYNTHESIS AND BLOOD PRESSURE LOWERING ACTIVITY OF CERTAIN TETRAHYDROBENZO [b] THIOPHENE DERIVATIVES WITH ARYLPIPERAZINYL SIDE CHAINS

Abstract

Blocking the action of adrenergic neurotransmitters on α1-adrenoreceptor is a well known approach for the clinical treatment of hypertension. Thus, novel compounds characterized by tetrahydrobenzo[b]thiophene or their annelated tetrahydrobenzo[b]thieno[2,3-d]pyrimidin-4(3H)ones connected through an alkyl spacer to arylpiperazine residue were designed and synthesized as structural analogues to prazosin as α1-adrenoreceptor (α1-AR) antagonists. The synthesized compounds were screened for their effect on blood pressure of normotensive cats. Some of these compounds displayed appreciable hypotensive activity compared to prazosin as reference standard.