A new class of diacidic nonpeptide angiotensin II receptor antagonists

N. Cho; K. Kubo; S. Furuya; Y. Sugiura; Yasuma T.; Kohara Y.; Ojima M.; Inada Y.; Nishikawa K.; Naka T.

doi:10.1016/S0960-894X(01)81118-5

A new class of diacidic nonpeptide angiotensin II receptor antagonists

N. Cho, K. Kubo, S. Furuya, Y. Sugiura, Yasuma T., Kohara Y., Ojima M., Inada Y., Nishikawa K., Naka T.

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

15 Citations (Scopus)

Abstract

A novel series of heterocyclic compounds I bearing two acidic funcitonalities, a carboxyl group and a tetrazole ring, was prepared and evaluated for in vitro and in vivo angiotensin II (AII) antagonistic activity. These compounds showed significantly more potent All antagonistic activities than the parent compounds without the carboxyl groups. This structure-activity relationhsip (SAR) study revealed the importance of the carboxyl group attached to the heterocyclic moieties especially for insurmountable antagonism and enhancement of in vivo (po) activity.

Original language	English
Pages (from-to)	35-40
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	4
Issue number	1
DOIs	https://doi.org/10.1016/S0960-894X(01)81118-5
Publication status	Published - Jan 6 1994
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)81118-5

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AU - Cho, N.

AU - Kubo, K.

AU - Furuya, S.

AU - Sugiura, Y.

AU - T., Yasuma

AU - Y., Kohara

AU - M., Ojima

AU - Y., Inada

AU - K., Nishikawa

AU - T., Naka

PY - 1994/1/6

Y1 - 1994/1/6

N2 - A novel series of heterocyclic compounds I bearing two acidic funcitonalities, a carboxyl group and a tetrazole ring, was prepared and evaluated for in vitro and in vivo angiotensin II (AII) antagonistic activity. These compounds showed significantly more potent All antagonistic activities than the parent compounds without the carboxyl groups. This structure-activity relationhsip (SAR) study revealed the importance of the carboxyl group attached to the heterocyclic moieties especially for insurmountable antagonism and enhancement of in vivo (po) activity.

AB - A novel series of heterocyclic compounds I bearing two acidic funcitonalities, a carboxyl group and a tetrazole ring, was prepared and evaluated for in vitro and in vivo angiotensin II (AII) antagonistic activity. These compounds showed significantly more potent All antagonistic activities than the parent compounds without the carboxyl groups. This structure-activity relationhsip (SAR) study revealed the importance of the carboxyl group attached to the heterocyclic moieties especially for insurmountable antagonism and enhancement of in vivo (po) activity.

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EP - 40

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

A new class of diacidic nonpeptide angiotensin II receptor antagonists

Abstract

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