A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F3

Iwao Ojima; Fabian A. Jameison

doi:10.1016/S0960-894X(01)81155-0

A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F₃

Iwao Ojima
, Fabian A. Jameison

Chemistry

Stony Brook University

Research output: Contribution to journal › Article › peer-review

22 Scopus citations

Abstract

Trifluoromethyl analogs of captopril, i.e (R,S)- and (S,S)-captopril-f₃, are synthesised and submitted to in vitro assay for inhibition of angiotensin converting enzyme (ACE). It is found that (R,S)-captopril-f₃ is substantially more potent than captoril (captopril-f₃: IC₅₀= 2.9 × 10^-10 M). Stereoelectronic and conformational effects attributed to trifluoromethyl incorporation serve to explain the enhanced inhibitory activity.

Original language	English
Pages (from-to)	581-584
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	1
Issue number	11
DOIs	https://doi.org/10.1016/S0960-894X(01)81155-0
State	Published - 1991

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title = "A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F3",

abstract = "Trifluoromethyl analogs of captopril, i.e (R,S)- and (S,S)-captopril-f3, are synthesised and submitted to in vitro assay for inhibition of angiotensin converting enzyme (ACE). It is found that (R,S)-captopril-f3 is substantially more potent than captoril (captopril-f3: IC50= 2.9 × 10-10 M). Stereoelectronic and conformational effects attributed to trifluoromethyl incorporation serve to explain the enhanced inhibitory activity.",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - A new potent inhibitor for angiotensin converting enzyme

T2 - (R,S)-captopril-F3

AU - Ojima, Iwao

AU - Jameison, Fabian A.

PY - 1991

Y1 - 1991

N2 - Trifluoromethyl analogs of captopril, i.e (R,S)- and (S,S)-captopril-f3, are synthesised and submitted to in vitro assay for inhibition of angiotensin converting enzyme (ACE). It is found that (R,S)-captopril-f3 is substantially more potent than captoril (captopril-f3: IC50= 2.9 × 10-10 M). Stereoelectronic and conformational effects attributed to trifluoromethyl incorporation serve to explain the enhanced inhibitory activity.

AB - Trifluoromethyl analogs of captopril, i.e (R,S)- and (S,S)-captopril-f3, are synthesised and submitted to in vitro assay for inhibition of angiotensin converting enzyme (ACE). It is found that (R,S)-captopril-f3 is substantially more potent than captoril (captopril-f3: IC50= 2.9 × 10-10 M). Stereoelectronic and conformational effects attributed to trifluoromethyl incorporation serve to explain the enhanced inhibitory activity.

UR - https://www.scopus.com/pages/publications/0025997192

U2 - 10.1016/S0960-894X(01)81155-0

DO - 10.1016/S0960-894X(01)81155-0

M3 - Article

AN - SCOPUS:0025997192

SN - 0960-894X

VL - 1

SP - 581

EP - 584

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F₃

Abstract

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