Metabolism of the antihypertensive drug methiapril

Considerable recent attention has been focused on the creation of drugs inhibiting the renin-angiotensin system (RAS) of an organism which are advantageous for treating various forms of arterial hypertension. In screening a broad range of derivatives of piperidinecarboxylic acids, cis-l-(3-acetylthiopropionyl)-6-methylpipecolinic acid was found to be the most efficient inhibitor of the RAS and was named METHIAPRIL (I) [ l ]. In the efficacy and duration of action on various models of arterial hypertension, it is close or superior to the foreign antihypertensive drug CAPTOPRIL (II).