Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles

Hakan Göker; Gülgün Ayhan-Kilcigil; Meral Tunçbilek; Canan Kus; Rahmiye Ertan; Engin Kendi; Süheyla Özbey; Mercé Fort; Celia Garcia; Antonio J. Farré

doi:10.3987/COM-99-8585

Synthesis and antihistaminic H₁ activity of 1,2,5(6)-trisubstituted benzimidazoles

Hakan Göker
, Gülgün Ayhan-Kilcigil
, Meral Tunçbilek
, Canan Kus
, Rahmiye Ertan
, Engin Kendi
, Süheyla Özbey
, Mercé Fort
, Celia Garcia
, Antonio J. Farré

Hacettepe University

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

49 Citations (Scopus)

Abstract

A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N¹-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H₁- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.

Original language	English
Pages (from-to)	2561-2573
Number of pages	13
Journal	Heterocycles
Volume	51
Issue number	11
DOIs	https://doi.org/10.3987/COM-99-8585
Publication status	Published - 1 Nov 1999

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title = "Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles",

abstract = "A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.",

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doi = "10.3987/COM-99-8585",

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T1 - Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles

AU - Göker, Hakan

AU - Ayhan-Kilcigil, Gülgün

AU - Tunçbilek, Meral

AU - Kus, Canan

AU - Ertan, Rahmiye

AU - Kendi, Engin

AU - Özbey, Süheyla

AU - Fort, Mercé

AU - Garcia, Celia

AU - Farré, Antonio J.

PY - 1999/11/1

Y1 - 1999/11/1

N2 - A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.

AB - A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.

UR - https://www.scopus.com/pages/publications/0344129077

U2 - 10.3987/COM-99-8585

DO - 10.3987/COM-99-8585

M3 - Article

AN - SCOPUS:0344129077

SN - 0385-5414

VL - 51

SP - 2561

EP - 2573

JO - Heterocycles

JF - Heterocycles

IS - 11

ER -

Synthesis and antihistaminic H₁ activity of 1,2,5(6)-trisubstituted benzimidazoles

Abstract

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