15755-15-4Relevant articles and documents
Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents
Rawal, Ravindra K.,Tripathi, Rajkamal,Katti,Pannecouque, Christophe,De Clercq, Erik
, p. 3134 - 3142 (2007)
A series of 2-(2,6-dihalophenyl)-3-(substituted pyrimidinyl)-1,3-thiazolidin-4-ones were designed on the prediction of quantitative structure-activity relationship (QSAR) studies, synthesized, and evaluated as HIV-1 reverse transcriptase inhibitors. Our attempts in correlating the identified molecular surface features related properties for modeling the HIV-1 RT inhibitory activity resulted in some statistically significant QSAR models with good predictive ability. The results showed that compounds 4m and 4n were highly active in inhibiting HIV-1 replication with EC50 values in the range of 22-28 nM in MT-4 as well as in CEM cells with selectivity indexes of >10,000. The derived models collectively suggest that the compounds should be compact without bulky substitution on its peripheries for better HIV-1 RT inhibitory activity. These models also indicate a preference for hydrophobic compounds to obtain good HIV-1 RT inhibitory activity.
Cyclization of Ketones with Nitriles under Base: A General and Economical Synthesis of Pyrimidines
Su, Lebin,Sun, Kang,Pan, Neng,Liu, Long,Sun, Mengli,Dong, Jianyu,Zhou, Yongbo,Yin, Shuang-Feng
, p. 3399 - 3402 (2018/06/11)
A facile, general, and economical synthesis of diversely functionalized pyrimidines has been realized under basic conditions via the copper-catalyzed cyclization of ketones with nitriles. The reaction proceeds via a novel pathway involving the nitriles ac
THE REACTION OF β-AMINOENONES WITH CYANAMIDE. A HIGH EFFICIENT SYNTHESIS OF 2-AMINOPIRIMIDINES.
Alberola, Angel,Andres, Celia,Ortega, Alfonso Gonzalez,Pedrosa, Rafael,Vicente, Martina
, p. 1309 - 1314 (2007/10/02)
β-aminoenones react with cyanamide, molar ratio 1:2, to yield 2-aminopyrimidines in nearly quantitative yields.