Name: Mequinol. Authors Jia, RF; Zhang, J; Bertagnin, C; Cherukupalli, S; Ai, W; Ding, X; Li, Z; Zhang, JW; Ju, H; Ma, XL; Loregian, A; Huang, B; Zhan, P; Liu, XY in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Jia, Ruifang; Cherukupalli, Srinivasulu; Ai, Wei; Ding, Xiao; Li, Zhuo; Zhang, Jiwei; Ju, Han; Zhan, Peng; Liu, Xinyong] Shandong Univ, Cheeloo Coll Med, Sch Pharmaceut Sci, Dept Med Chem,Key Lab Chem Biol,Minist Educ, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China; [Zhang, Jian] Shandong Univ, Hosp 2, Cheeloo Coll Med, Inst Med Sci, Jinan 250033, Shandong, Peoples R China; [Bertagnin, Chiara; Loregian, Arianna] Univ Padua, Dept Mol Med, Via Gabelli 63, I-35121 Padua, Italy; [Ma, Xiuli; Huang, Bing] Shandong Acad Agr Sci, Inst Poultry Sci, 1 Jiaoxiao Rd, Jinan 250023, Shandong, Peoples R China; [Zhan, Peng; Liu, Xinyong] China Belgium Collaborat Res Ctr Innovat Antivira, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China in 2021, Cited 41. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5
Encouraged by our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Herein, we report the design, synthesis and biological evaluation of a series of novel oseltamivir derivatives via the structural modifications at C-5-NH2 of oseltamivir targeting 150-cavity. Among them, compound 5c bearing 4-(3-methoxybenzyloxy)benzyl group exhibited the most potent activity, which was lower or modestly improved activities than oseltamivir carboxylate (OSC) against N1 (H1N1), N1 (H5N1) and N1 (H5N1-H274Y). Specifically, there was 30-fold loss of activity against the wild-type strain H1N1. However, 5c displayed 4.85-fold more potent activity than OSC against H5N1-H274Y NA. Also, 5c demonstrated low cytotoxicity in vitro and no acute toxicity in mice. Molecular docking studies provided insights into the high potency of 5c against N1 and N1-H274Y mutant NAs. Besides, the in silico prediction of physicochemical properties and CYP enzymatic inhibitory ability of representative compounds were conducted to evaluate their drug-like properties. (C) 2020 Elsevier Masson SAS. All rights reserved.
Name: Mequinol. About Mequinol, If you have any questions, you can contact Jia, RF; Zhang, J; Bertagnin, C; Cherukupalli, S; Ai, W; Ding, X; Li, Z; Zhang, JW; Ju, H; Ma, XL; Loregian, A; Huang, B; Zhan, P; Liu, XY or concate me.
Reference:
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles