Wu, YM; Tang, CR; Rui, RM; Yang, LM; Ding, W; Wang, JY; Li, YM; Lai, CC; Wang, YP; Luo, RH; Xiao, WL; Zhang, HB; Zheng, YT; He, YP in [Wu, Yumeng; Rui, Ruomei; Ding, Wei; Wang, Jiangyuan; Li, Yiming; Wang, Yueping; Xiao, Weilie; Zhang, Hongbing; He, Yanping] Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resources, Minist Educ & Yunnan Prov, Kunming 650091, Yunnan, Peoples R China; [Tang, Chengrun; Yang, Liumeng; Luo, Ronghua; Zheng, Yongtang] Chinese Acad Sci, Natl Kunming High Level Biosafety Res Ctr Nonhuma, Key Lab Bioact Peptides Yunnan Prov,Key Lab Anim, Kunming Inst Zool,KIZ CUHK Joint Lab Bioresources, Kunming 650223, Yunnan, Peoples R China; [Lai, Christopher C.] NCI, Chem Biol Lab, Ctr Canc Res, NIH, Frederick, MD 21702 USA; [Tang, Chengrun] Kunming Med Univ, Sch Pharmaceut Sci, Kunming 650500, Yunnan, Peoples R China; [Tang, Chengrun] Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650500, Yunnan, Peoples R China published Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors in 2020.0, Cited 40.0. Quality Control of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.
A series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones were synthesized and their anti-HIV-1 activities were evaluated. Most of these compounds were highly active against wild-type (WT) HIV-1 strain (IIIB) with EC50 values in the range of 0.0038-0.4759 mmol/L. Among those compounds, I-11 had an EC50 value of 3.8 nmol/L and SI (selectivity index) of up to 25,468 indicating excellent activity against WT HIV-1. In vitro anti-HIV-1 activity and resistance profile studies suggested that compounds I-11 and I-12 displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (EC(50)s range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, respectively). On the other hand, it was observed that those two compounds were less effective with EC50 values of 2.77 and 4.87 mmol/L for HIV-1A(17) (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds. Both I-11 and I-12 obtained sub-micromolar IC50 values showing their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound I-11 has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and molecular modeling studies were also discussed. (C) 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
About 4′-Hydroxyacetophenone, If you have any questions, you can contact Wu, YM; Tang, CR; Rui, RM; Yang, LM; Ding, W; Wang, JY; Li, YM; Lai, CC; Wang, YP; Luo, RH; Xiao, WL; Zhang, HB; Zheng, YT; He, YP or concate me.. Quality Control of 4′-Hydroxyacetophenone
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles