6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverse transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase was written by Tang, Jing;Kirby, Karen A.;Huber, Andrew D.;Casey, Mary C.;Ji, Juan;Wilson, Daniel J.;Sarafianos, Stefan G.;Wang, Zhengqiang. And the article was included in European Journal of Medicinal Chemistry in 2017.Recommanded Product: 2-Cyclohexylacetonitrile This article mentions the following:
3-Hydroxypyrimidine-2,4-dione (HPD) represents a versatile chem. core in the design of inhibitors of human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated RNase H and integrase strand transfer (INST). We report herein the design, synthesis and biol. evaluation of an HPD subtype (4, IV) featuring a cyclohexylmethyl group at the C-6 position. Antiviral testing showed that most analogs of 4 inhibited HIV-1 in the low nanomolar to submicromolar range, without cytotoxicity at concentrations up to 100 μM. Biochem., these analogs dually inhibited both the polymerase (pol) and the RNase H functions of RT, but not INST. Co-crystal structure of 4a (IV; R1 = i-Pr, R2 = H) with RT revealed a nonnucleoside RT inhibitor (NNRTI) binding mode. Interestingly, chemotype 11, the synthetic precursor of 4 lacking the 3-OH group, did not inhibit RNase H while potently inhibiting pol. By virtue of the potent antiviral activity and biochem. RNase H inhibition, HPD subtype 4 could provide a viable platform for eventually achieving potent and selective RNase H inhibition through further medicinal chem. In the experiment, the researchers used many compounds, for example, 2-Cyclohexylacetonitrile (cas: 4435-14-7Recommanded Product: 2-Cyclohexylacetonitrile).
2-Cyclohexylacetonitrile (cas: 4435-14-7) belongs to nitriles. There has been no report on the microbial biosynthesis of nitriles and the physiological function of such enzymes, nor was it not even known whether aliphatic and aromatic nitriles are biological compounds or just petrochemicals. Nitriles are susceptible to hydrogenation over diverse metal catalysts. The reaction can afford either the primary amine (RCH2NH2) or the tertiary amine ((RCH2)3N), depending on conditions.Recommanded Product: 2-Cyclohexylacetonitrile
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts