The present invention is directed to an .alpha. thio-containing compound
that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP
or APP), whose natural substrate is bradykinin. The compound is useful as
a pharmaceutical agent because by inhibiting bradykinin degradation, the
compound allows bradykinin to exert its beneficial effects on the
cardiovascular system, to improve renal function, and to improve glucose
tolerance and insulin-sensitivity. The present invention is also directed
to a pharmaceutical composition comprising the mAPP inhibitor of the
present invention and a pharmaceutically acceptable carrier. In another
aspect, the present invention is directed to a method of inhibiting
bradykinin degradation in a mammalian patient, preferably human, in need
of treatment comprising administering to the patient a therapeutically
effective amount of an .alpha. thio-containing compound of the present
invention. The method of the present invention also contemplates the
further step of administering to the mammalian patient in need of
treatment a therapeutically effective amount of an inhibitor of
angiotensin converting enzyme (ACE).