Yadav, M. R. published the artcileDesign and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1– and AII-receptors antagonism, SDS of cas: 178928-58-0, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(13), 3959-3966, database is CAplus and MEDLINE.
Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Mols. with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α1-blockers and AII-antagonists it was planned to develop dual α1– and AII-antagonists. Five series of quinazoline derivatives were synthesized and evaluated as dual α1– and AII-antagonists on rat aortic strips for the blockade of known α1– and AII-agonist mediated contractions. Many compounds showed balanced activity on both the receptors but compound (22) was the most active derivative having higher antagonistic activity on both the receptors. In the in vivo experiments the chosen compound (22) was slightly less active than prazosin but was equipotent to losartan. These findings shed a new light on the structural requirements for both α1– and AII-receptor antagonists.
Bioorganic & Medicinal Chemistry Letters published new progress about 178928-58-0. 178928-58-0 belongs to piperazines, auxiliary class Piperazine,Nitrile,Benzene, name is 1-(3-Cyanophenyl)piperazine, and the molecular formula is C44H28ClFeN4, SDS of cas: 178928-58-0.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics