
Journal of Medicinal Chemistry p. 1277 - 1282 (1983)
Update date:2022-07-30
Topics:
Gruenfeld, Norbert
Stanton, James L.
Yuan, Andrew M.
Ebetino, Frank H.
Browne, Leslie J.
et al.
The preparation of a series of 1-glutarylindoline-2(S)-carboxylic acid derivatives, 6a-v and 21a-c, is described.The above compounds were tested for inhibition of angiotensin converting enzyme.The structure-activity relationship of the series is also discussed.Compound 6u, the most potent member of the series, had an in vitro IC50 of 4.8*10-9 M.Compound 6v, an ethyl ester of 6u, lowered blood pressure 70 mm in spontaneous hypertensive rats at an oral dose of 30 mg/kg.
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Doi:10.1021/jo00145a038
(1982)Doi:10.1016/S0040-4039(97)01061-7
(1997)Doi:10.1021/jo00145a033
(1982)Doi:10.1055/s-1982-29894
(1982)Doi:10.1021/acs.orglett.8b01506
(2018)Doi:10.1039/c39820000563
(1982)