HPLC of Formula: 29004-73-7On March 31, 2020, Wu, Yumeng; Tang, Chengrun; Rui, Ruomei; Yang, Liumeng; Ding, Wei; Wang, Jiangyuan; Li, Yiming; Lai, Christopher C.; Wang, Yueping; Luo, Ronghua; Xiao, Weilie; Zhang, Hongbing; Zheng, Yongtang; He, Yanping published an article in Acta Pharmaceutica Sinica B. The article was 《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》. The article mentions the following:
A series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones I [R1 = H, Me, Ph, etc.; R2 = H, Me, Et; X = H, Cl] 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 0.0038-0.4759μmol/L. Among those compounds,I [R1 = 4-hydroxyphenyl, R2 = Et, X = H (II)] 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 (II) and I [R1 = 4-(methylsulfanyl)phenyl, R2 = Et, X = H (III)] displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (EC50s range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, resp.). On the other hand, it was observed that those two compounds (II) and (III) were less effective with EC50 values of 2.77 and 4.87μmol/L for HIV-1A17 (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds Both (II) and (III) obtained sub-micromolar IC50 values showed their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound (II) has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and mol. modeling studies were also discussed. In the experiment, the researchers used (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7HPLC of Formula: 29004-73-7)
(3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.HPLC of Formula: 29004-73-7
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics