On December 16, 2020, Wang, Peng-Fei; Jensen, Anders A.; Bunch, Lennart published an article.Related Products of 89-77-0 The title of the article was From Methaqualone and Beyond: Structure-Activity Relationship of 6-, 7-, and 8-Substituted 2,3-Diphenyl-quinazolin-4(3H)-ones and in Silico Prediction of Putative Binding Modes of Quinazolin-4(3H)-ones as Positive Allosteric Modulators of GABAA Receptors. And the article contained the following:
Methaqualone (2-methyl-3-(o-tolyl)-quinazolin-4(3H)-one, MTQ) is a moderately potent pos. allosteric modulator (PAM) of GABAA receptors (GABAARs). In a previous structure-activity relationship (SAR) study probing the importance of 2- and 3-substituents in the quinazolin-4(3H)-one scaffold, several potent GABAAR PAMs were identified, including 2,3-diphenylquinazolin-4(3H)-one (PPQ) and 3-(2-chlorophenyl)-2-phenylquinazolin-4(3H)-one (Cl-PPQ). Here, PPQ was applied as lead in a SAR study of 6-, 7-, and 8-substituents in the quinazolin-4(3H)-one by synthesis and functional characterization of 36 PPQ analogs at various GABAAR subtypes. While none of the new analogs were significantly more potent than PPQ or displayed pronounced subtype selectivity across the GABAARs tested, several interesting SAR observations were extracted from the study. In an in silico study, the putative binding modes of MTQ, PPQ, and Cl-PPQ in the transmembrane β2(+)/α1(-) interface of the α1β2γ2S GABAAR were predicted. Several plausible binding modes were identified for the three PAMs, and rationalization of the mol. basis for their different modulatory potencies was attempted. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Related Products of 89-77-0
The Article related to quinazolinone preparation gaba receptor allosteric modulator, structure quinazolinone binding selectivity gaba receptor, mol docking complex quinazolinone gabaa transmembrane domain, gabaa positive allosteric modulators (pams), gabaa receptors, docking, methaqualone, structure−activity relationship (sar) study, transmembrane domain and other aspects.Related Products of 89-77-0
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