Benzimidazole, Benzoxazole and Benzothiazole Derivatives as 5HT2B Receptor Ligands. Synthesis and Preliminary Pharmacological Evaluation

被引：0

作者：

G. Giorgioni

B. Accorroni

A. Di Stefano

G. Marucci

A. Siniscalchi

F. Claudi

机构：

[1] Università di Camerino,Dipartimento di Scienze Chimiche

[2] Università G. D'Annunzio,Dipartimento di Scienze del Farmaco

[3] Università di Ferrara,Dipartimento di Medicina Sperimentale e Clinica, Sezione di Farmacologia

来源：

Medicinal Chemistry Research | 2005年 / 14卷

关键词：

Serotonin; Receptor Antagonist; Structural Feature; Binding Affinity; Benzimidazole;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2-phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT2B receptor antagonists. Those molecules were designed to recognize the 5-HT2B receptor and to discriminate it from the 5-HT2A and 5-HT2C subtypes. All compounds were characterized by binding affinity determination for 5-HT2A and 5-HT2C subtypes and antagonistic activity for 5-HT2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT2A and 5-HT2C subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations.

引用

页码：57 / 73

页数：16

共 50 条

[21] A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT1A receptor ligands
Caliendo, G
Fiorino, F
Perissutti, E
Severino, B
Scolaro, D
Gessi, S
Cattabriga, E
Borea, PA
Santagada, V
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 16 (1-2) : 15 - 28
[22] Design and synthesis of potent and selective 5-HT1A receptor ligands.
Zhang, G
Palmer, Y
Kelly, MG
Smith, DL
Schechter, LE
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2000, 220 : U557 - U557
[23] Design, synthesis, and evaluation of 5-hydroxy-2-(3-phenylpropyl)chromone derivatives as 5-HT2B receptor ligands
Kim, Min Soo
Truss, Myles
Plascencia, Victor
Wang, Huiqun
Zaidi, Saheem
Zhang, Yan
Williams, Dwight
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2019, 258
[24] Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists
Moritomo, Ayako
Yamada, Hiroyoshi
Matsuzawa-Nomura, Takaho
Watanabe, Toshihiro
Itahana, Hirotsune
Oku, Makoto
Akuzawa, Shinobu
Okada, Minoru
BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 22 (21) : 6026 - 6038
[25] Design, synthesis and biological evaluation of some novel benzothiazole/benzoxazole and/or benzimidazole derivatives incorporating a pyrazole scaffold as antiproliferative agents
Abdelgawad, Mohamed A.
Bakr, Rania B.
Omar, Hany A.
BIOORGANIC CHEMISTRY, 2017, 74 : 82 - 90
[26] Synthesis and in Vitro Antiproliferative Evaluation of Some B-norcholesteryl Benzimidazole and Benzothiazole Derivatives
Cui, Jianguo
Qi, Binbin
Gan, Chunfang
Liu, Zhipin
Huang, Hu
Lin, Qifu
Zhao, Dandan
Huang, Yanmin
MARINE DRUGS, 2015, 13 (04) : 2488 - 2504
[27] Synthesis and pharmacological evaluation of benzamide derivatives as selective 5-HT4 receptor agonists
Sonda, S
Kawahara, T
Katayama, K
Sato, N
Asano, K
BIOORGANIC & MEDICINAL CHEMISTRY, 2005, 13 (09) : 3295 - 3308
[28] SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 2-SUBSTITUTED BENZOTHIAZOLE DITHIOMIDOCARBONATE DERIVATIVES
Tasleem
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2015, 6 (09): : 4058 - 4068
[29] SYNTHESIS AND IN-VITRO EVALUATION OF HALOGENATED PHENETHYLPIPERIDINE DERIVATIVES AS POTENT 5-HT2 RECEPTOR LIGANDS
HWANG, DR
BANKS, WR
ADKINS, J
SATTER, M
MANTIL, JC
JOURNAL OF NUCLEAR MEDICINE, 1994, 35 (05) : P252 - P252
[30] Synthesis and pharmacological evaluation of novel 4-(4-fluorobenzoyl)piperidine derivatives as mixed 5-HT1A/5-HT2A/D2 receptor ligands
Diouf, O
Carato, P
Lesieur, I
Rettori, MC
Caignard, DH
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1999, 34 (01) : 69 - 73

← 1 2 3 4 5 →