Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists

Holger Stark; Xavier Ligneau; Bassem Sadek; C. Robin Ganellin; Jean Michel Arrang; Jean Charles Schwartz; Walter Schunack

doi:10.1016/S0960-894X(00)00473-X

Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H₃-receptor antagonists

Holger Stark, Xavier Ligneau, Bassem Sadek, C. Robin Ganellin, Jean Michel Arrang, Jean Charles Schwartz, Walter Schunack

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

5 Citations (Scopus)

Abstract

Novel derivatives of the highly potent and selective histamine H₃-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H₃-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd.

Original language	English
Pages (from-to)	2379-2382
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	10
Issue number	20
DOIs	https://doi.org/10.1016/S0960-894X(00)00473-X
Publication status	Published - Oct 16 2000
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(00)00473-X

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title = "Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists",

abstract = "Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd.",

author = "Holger Stark and Xavier Ligneau and Bassem Sadek and Ganellin, {C. Robin} and Arrang, {Jean Michel} and Schwartz, {Jean Charles} and Walter Schunack",

note = "Funding Information: We gratefully thank A. Piripitsi for the synthesis of compound 4 . This work was supported by the Biomedical & Health Research Programme BIOMED of the European Union and by the Fonds der Chemischen Industrie, Verband der Chemischen Industrie (Frankfurt/Main, Germany).",

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doi = "10.1016/S0960-894X(00)00473-X",

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T1 - Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists

AU - Stark, Holger

AU - Ligneau, Xavier

AU - Sadek, Bassem

AU - Ganellin, C. Robin

AU - Arrang, Jean Michel

AU - Schwartz, Jean Charles

AU - Schunack, Walter

N1 - Funding Information: We gratefully thank A. Piripitsi for the synthesis of compound 4 . This work was supported by the Biomedical & Health Research Programme BIOMED of the European Union and by the Fonds der Chemischen Industrie, Verband der Chemischen Industrie (Frankfurt/Main, Germany).

PY - 2000/10/16

Y1 - 2000/10/16

N2 - Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd.

AB - Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose. (C) 2000 Elsevier Science Ltd.

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Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H₃-receptor antagonists

Abstract

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