Manetti, Fabrizio published the artcileParallel Solution-Phase and Microwave-Assisted Synthesis of New S-DABO Derivatives Endowed with Subnanomolar Anti-HIV-1 Activity, Name: (4-Butoxyphenyl)methanol, the main research area is arylthiopyrimidinone preparation HIV 1 transcriptase inhibitor.
A simple and efficient methodol. for the parallel solution-phase synthesis has been set up to obtain a series of thiouracils, in turn selectively S-benzylated under microwave irradiation to give new S-DABOs. Biol. screening led to the identification of compounds with nanomolar activity toward both the highly purified recombinant human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) enzyme (wild-type and mutants) and wild-type (wt) and mutant HIV-1 strains. In particular, I was found to be the most potent S-DABO reported so far (ID50 = 26 nM toward the isolated wt enzyme) with subnanomolar activity toward both the wt and the pluriresistant virus (IRLL98) HIV-1 strain (EC50 < 0.14 nM and EC50 = 0.22 nM, resp.). Mol. modeling calculations were also performed to investigate the binding mode of such compounds onto the non-nucleoside reverse transcriptase inhibitor binding site and to rationalize the relationships between their chem. structure and activity values toward wt RT. Journal of Medicinal Chemistry published new progress about Homo sapiens. 6214-45-5 belongs to class alcohols-buliding-blocks, name is (4-Butoxyphenyl)methanol, and the molecular formula is C11H16O2, Name: (4-Butoxyphenyl)methanol.
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