In 2020 EUR J MED CHEM published article about REVERSE-TRANSCRIPTASE INHIBITORS; DIARYLPYRIMIDINES DAPYS; BROAD POTENCY; DERIVATIVES; DISCOVERY; BENZOPHENONES; DOCKING; ANALOGS; FAMILY; SERIES in [Xiao, Ting; Tang, Jia-Fan; Liu, Gen-Yan; Xu, Zhi-Qiang; Wu, Feng-Shou; Gu, Shuang-Xi; Chen, Fen-Er] Wuhan Inst Technol, Sch Chem Engn & Pharm, Minist Educ, Key Lab Green Chem Proc, Wuhan 430205, Peoples R China; [Meng, Ge; Chen, Fen-Er] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China; [Pannecouque, Christophe] Katholieke Univ Leuven, Dept Microbiol & Immunol, Lab Virol & Chemotherapy, Rega Inst Med Res, B-3000 Leuven, Belgium; [Zhu, Yuan-Yuan] Wuhan Inst Technol, Sch Chem & Environm Engn, Wuhan 430205, Peoples R China in 2020, Cited 36. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Recommanded Product: 98-17-9
A series of indazolyl-substituted piperidin-4-yl-aminopyrimidines (IPAPYs) were designed from two potent HIV-1 NNRTIs piperidin-4-yl-aminopyrimidine 3c and diaryl ether 4 as the lead compounds by molecular hybridization strategy. The target molecules 5a-q were synthesized and evaluated for their anti-HIV activities and cytotoxicities in MT-4 cells. 5a-q displayed moderate to excellent activities against wild-type (WT) HIV-1 with ECK values ranging from 1.5 to 0.0064 mu M. Among them, 5q was regarded as the most excellent compound against WT HIV-1 (EC50 = 6.4 nM, SI = 2500). And also, it displayed potent activities against K103 N (EC50 = 0.077 mu M), Y181C (EC50 = 0.11 mu M), E138K (EC50 = 0.057 mu M), and moderate activity against double mutants RES056 (EC50 = 8.7 mu M). Moreover, the structure-activity relationships (SARs) were summarized, and the molecular docking was performed to investigate the binding mode of IPAPYs and HIV-1 reverse transcriptase. (C) 2019 Elsevier Masson SAS. All rights reserved.
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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