1025916-63-5Relevant academic research and scientific papers
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6- (arylcarbonyl or α-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
Ji, Lei,Chen, Fen-Er,De Clercq, Erik,Balzarini, Jan,Pannecouque, Christophe
, p. 1778 - 1786 (2008/02/01)
A series of novel S-DABO analogues (S-DABOs, 1) were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Key structural modifications included replacement of the 6-arylmethyl group by a 6-arylcarbonyl or 6-(α-cyanoarylmethyl) group. Most of the compounds showed only micromolar potency against HIV-1 in MT-4 cells in vitro, though two of them (3e and 3g) were unusually potent (IC50 = 0.09 and 0.002 μM, respectively) and selective (SI = 1500 and 4600, respectively). Structure-activity relationships among the newly synthesized S-DABOs are discussed.
