SYNTHESIS AND EVALUATION OF NOVEL CALCIUM CHANNEL BLOCKING AGENTS

摘要

Benzothiopyran is a heterocyclic compound which contains sulphur as a heteroatom which is responsible for biological and pharmacological activity. Changing heterocyclic ring size will generate derivatives that are not only retained the calcium channel blocking activity but also resulted in several compounds that were more active than diltiazem. A receptor-binding model identifying the benzene ring as a lipophilic group that facilitates transport into the channel and the absolute stereochemistry for the selective binding. Benzothiopyran nucleus is similar to the benzothiazepine nucleuses which are used as calcium channel blockers. In these synthesis series, benzothiazepine nucleus containing nitrogen atom which is replace by bioisosterism of nitrogen.