The recently derived algorithm for identifying the COmmon REactivity PAttern (COREPA) of structurally diverse chems. having similar biol. behavior was employed to recognize the structural requirements for high ACE inhibition.COREPA is based on an assessment of all energetically-reasonable conformations of the compounds under study.It is not dependent upon a predetermined and specified pharmacophore or an alignment of active conformers.The approach describes the common reactivity pattern in terms of global and local stereoelectronic parameter ranges.These ranges are associated with compounds having extreme (highest and lowest) biol. activity through a comparison of conformer distributions for specific descriptors.The defined parameter ranges were combined into Boolean expressions providing flexible screening of chems. by making use of a new chem. rule interpreter allowing a simultaneous search according to all available 2-D and 3-D information.The structural combinations, i.e., COREPAs, derived on a training set of ACE inhibitors were used for screening chems. in an external test series for identifying those with high ACE inhibition activity.The obtained results showed that the structural requirements derived in the present work can be useful for screening chems. from databases as potential lead ACE inhibitors.

01 Jan 1985·Journal of medicinal chemistryQ1 · MEDICINE

Angiotensin-converting enzyme inhibitors. New orally active antihypertensive (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives

Q1 · MEDICINE

Article

Author: Jones, Howard ; Skiles, Jerry W. ; Williams, Bruce E. ; Youssefyeh, Raymond D. ; Loev, Bernard ; Schwab, Alfred ; Neiss, Edward S. ; Mann, William S. ; Suh, John T.

A variety of N-substituted (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives was synthesized and their ability in inhibiting the activity of angiotensin-converting enzyme (ACE) was examined in vitro and in vivo. The acylthio derivatives prepared are assumed to act as prodrugs since they are much less active than the corresponding free SH compounds in vitro and can be expected to act in vivo only after conversion to the free sulfhydryl compounds. A number of these compounds are potent ACE inhibitors that lowered blood pressure in Na-deficient, conscious spontaneously hypertensive rats (SHR), a high renin model. One of the most active members of the series was (S)-N-cyclopentyl-N-[3-[(2,2-dimethyl-1-oxopropyl)thio]-2-methyl-1 -oxopropyl]glycine (REV 3659-(S), pivopril). Structure-activity relationships are discussed.

01 Jan 1985·Journal of cardiovascular pharmacologyQ4 · MEDICINE

The Present Molecules of Converting Enzyme Inhibitors

Q4 · MEDICINE

Review

Author: H. R. Brunner ; J. Nussberger ; B. Waeber

Since the end of 1976 ten orally active converting enzyme inhibitors [SQ 14,225 (captopril), MK 421 (enalapril), MK 422, MK 521 (lysinopril), RHC 3659, CGS 13945, CGS 13928C, CGS 14824A, Hoe 498, S 9490-3, and Ro 31-2848] have been evaluated by our group in normal volunteers. Their ability to blunt the pressor response to exogenous angiotensin I and their effect on the different components of the renin-angiotensin system were tested. This approach has made it possible to establish the efficacy of the different molecules and to predict with a considerable degree of accuracy onset and duration of action of the various compounds as well as the doses needed to treat hypertensive patients. All ten molecules were effective in blocking converting enzyme and thereby the pressor response to angiotensin I. Potency and time course of the inhibition varied considerably among the compounds. Thus, a number of highly effective angiotensin-converting enzyme inhibitors are actually in clinical evaluation and several of them should become available for general clinical use within a few years.

100 Deals associated with Pivopril

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension	Preclinical	United States	Revlon Group Holdings LLC	01 May 2002

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