New Antihypertensive Agents. I. Synthesis and Antihypertensive Activity of Some 4-Piperidylbenzimidazolinone Derivatives

New Antihypertensive Agents. I. Synthesis and Antihypertensive Activity of Some 4-Piperidylbenzimidazolinone Derivatives

A series of 4-piperidylbenzimidazolinones, of formula I, has been synthesized. Selective syntheses of erythro and threo isomers of α-alkyl phenylethanolamines were investigated. Most members of the series have been shown to have antihypertensive effects in various animal models. Compounds 27 and 31...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1982/02/25, Vol.30(2), pp.462-473
Hauptverfasser: OBASE, HIROYUKI, NAKAMIZO, NOBUHIRO, TAKAI, HARUKI, TERANISHI, MASAYUKI, KUBO, KAZUHIRO, SHUTO, KATSUICHI, KASUYA, YUTAKA, KATO, HITOSHI, SHIGENOBU, KOKI, KURIHARA, JUNICHI
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antihypertensive Agents - chemical synthesis
Benzimidazoles - chemical synthesis
Benzimidazoles - pharmacology
Male
Rats
Rats, Inbred Strains
structure-activity relationship
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Zusammenfassung:A series of 4-piperidylbenzimidazolinones, of formula I, has been synthesized. Selective syntheses of erythro and threo isomers of α-alkyl phenylethanolamines were investigated. Most members of the series have been shown to have antihypertensive effects in various animal models. Compounds 27 and 31 (threo isomers) showed the strongest hypotensive activities in the present screening series.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.30.462