He, Xiao-Yang; Lu, Lu; Qiu, Jiayin; Zou, Peng; Yu, Fei; Jiang, Xing-Kai; Li, Lin; Jiang, Shibo; Liu, Shuwen; Xie, Lan published the artcile< Small molecule fusion inhibitors: Design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles and related derivatives targeting HIV-1 gp41>, Reference of 10574-69-3, the main research area is benzyloxothioxothiazolidinylidenemethyl carboxyhydroxyphenyl dimethylpyrrole preparation antiaids AIDS HIV fusion inhibitor; 3-Substituted N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrrole derivatives; Anti-HIV agents; HIV-1 gp41; Small-molecule fusion inhibitors.
By a scaffold elongation strategy, a series of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene)methyl)-N-(3-carboxy-4-hydroxy)phenyl-2,5-dimethylpyrroles I [R = Ph, 4-BrC6H4, 4-MeOC6H4, etc.; X = (CH2)n; n = 0-2] and related derivatives with a linear multiarom.-ring skeleton were designed, synthesized, and evaluated in HIV-1 gp41 and cellular assays. the most active compounds I [R = 4-MeO2CC6H4; 4-tBuC6H4; 3-MeO2CC6H4; X = CH2] exhibited very promising inhibitory potency with IC50 values of 1.8-2.6 μM and EC50 values of 0.3-1.5 μM against gp41 6-HB formation and HIV-1 replication in MT-2 cells, resp. Addnl., they were almost equally effective against both T20-sensitive and resistant strains. The related SAR studies and mol. modeling results provided potential for further developing a new class of nonpeptide small mol. fusion inhibitors targeting the HIV-1 gp41.
Bioorganic & Medicinal Chemistry published new progress about AIDS (disease). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Reference of 10574-69-3.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica