Literature DB >> 18625562

Molecular features of the prazosin molecule required for activation of Transport-P.

Joaquim Fernando Mendes da Silva1, Marcus Walters, Saad Al-Damluji, C Robin Ganellin.   

Abstract

Closely related structural analogues of prazosin have been synthesised and tested for inhibition and activation of Transport-P in order to identify the structural features of the prazosin molecule that appear to be necessary for activation of Transport-P. So far, all the compounds tested are less active than prazosin. It is shown that the structure of prazosin appears to be very specific for the activation. Only quinazolines have been found to activate, and the presence of the 6,7-dimethoxy and 4-amino groups appears to be critically important.

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Year:  2008        PMID: 18625562     DOI: 10.1016/j.bmc.2008.06.037

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Regioselective Palladium-Catalyzed Cross-Coupling Reactions of 2,4,7-Trichloroquinazoline.

Authors:  Peter Wipf; Kara M George
Journal:  Synlett       Date:  2010-03-01       Impact factor: 2.454

2.  A new synthetic route to original sulfonamide derivatives in 2-trichloromethylquinazoline series: a structure-activity relationship study of antiplasmodial activity.

Authors:  Nicolas Primas; Pierre Verhaeghe; Anita Cohen; Charline Kieffer; Aurélien Dumètre; Sébastien Hutter; Sylvain Rault; Pascal Rathelot; Nadine Azas; Patrice Vanelle
Journal:  Molecules       Date:  2012-07-05       Impact factor: 4.411

3.  Electrosynthesis of Quinazolines and Quinazolinones via an Anodic Direct Oxidation C(sp3)-H Amination/C-N Cleavage of Tertiary Amine in Aqueous Medium.

Authors:  Zhenghong Zhou; Kangfei Hu; Jiawei Wang; Zhibin Li; Yan Zhang; Zhenggen Zha; Zhiyong Wang
Journal:  ACS Omega       Date:  2020-12-01

4.  The cytotoxicity of the α1-adrenoceptor antagonist prazosin is linked to an endocytotic mechanism equivalent to transport-P.

Authors:  Robert Fuchs; Anika Stracke; Nadine Ebner; Christian Wolfgang Zeller; Anna Maria Raninger; Matthias Schittmayer; Tatjana Kueznik; Markus Absenger-Novak; Ruth Birner-Gruenberger
Journal:  Toxicology       Date:  2015-10-09       Impact factor: 4.221

  4 in total

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