1453172-41-2Relevant academic research and scientific papers
Synthesis and evaluation of novel 3-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents
Sakakibara, Norikazu,Hamasaki, Takayuki,Baba, Masanori,Demizu, Yosuke,Kurihara, Masaaki,Irie, Kohji,Iwai, Masatoshi,Asada, Eriko,Kato, Yoshihisa,Maruyama, Tokumi
, p. 5900 - 5906 (2013/09/12)
A novel series of uracil derivatives with a 3,5-dimethylbenzyl group at the N3-position were synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Some of these compounds showed good-to-moderate activity with EC50 values in the submicromolar range. Among them, compound 10c showed significant potency against HIV-1 activity with an EC50 value of 0.03 μM and a high selectivity index of 2863. Preliminary structure-activity relationships and molecular modeling analyses were used to explore the major interactions between HIV-1 reverse transcriptase and the potent inhibitor 10c, which may serve as an important lead for further optimization.
