Molecular design and synthesis of 1,4-disubstituted piperazines as α(1)-adrenergic receptor blockers
Hussein, Mohammed M; Serya, Rabah; Abdel Naby, Rana M; Al-Abd, Ahmed M; Saleh, Dalia O; El-Eraky, Wafaa I; Khaled A M Abouzid; Abou El Ella, Dalal;
Abstract
A new series of 4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid amide and 3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4-one derivatives were designed, synthesized, their binding and functional properties as α1-adrenoreceptors blockers were evaluated. A new validated α1-adrenoreceptor blocker pharmacophore model (hypothesis) was generated using Discovery Studio 2.5. The compare-fit study for the designed molecules with the generated hypothesis was fulfilled and several compounds showed significant high fit values. Compounds IVa-c, VIIa-d, VIIIa-c, Xa-c, XIa-d have shown blocking activity ranging from 46.73% up to 94.74% compared to 99.17% for prazosin.
Other data
| Title | Molecular design and synthesis of 1,4-disubstituted piperazines as α(1)-adrenergic receptor blockers | Authors | Hussein, Mohammed M; Serya, Rabah ; Abdel Naby, Rana M; Al-Abd, Ahmed M; Saleh, Dalia O; El-Eraky, Wafaa I; Khaled A M Abouzid ; Abou El Ella, Dalal | Keywords | Phenylpiperazines;Pyridothienopyrimidine;α(1)-Adrenoreceptors blockers | Issue Date | Jun-2014 | Publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | Journal | Bioorganic Chemistry | Volume | 54 | Start page | 21 | End page | 30 | ISSN | 0045-2068 | DOI | 10.1016/j.bioorg.2014.03.005 | PubMed ID | 24727279 | Scopus ID | 2-s2.0-84898440797 | Web of science ID | WOS:000338732900004 |
Attached Files
| File | Description | Size | Format | Existing users please Login |
|---|---|---|---|---|
| البحث الرابع.pdf | 1.28 MB | Adobe PDF | Request a copy |
Similar Items from Core Recommender Database
Items in Ain Shams Scholar are protected by copyright, with all rights reserved, unless otherwise indicated.