An article Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase WOS:000661282500043 published article about VIRUS; ZANAMIVIR; EPIDEMIOLOGY; DERIVATIVES; RESISTANCE in [Zhao, Hongqian; Jiang, Siyuan; Ye, Zhifan; Zhu, Hongxi; Meng, Peipei; Wang, Kuanglei; Tian, Yongshou] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Hu, Baichun] Shenyang Pharmaceut Univ, Sch Pharm, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Zhang, Huicong] Shenyang Pharmaceut Univ, Wuya Coll Innovat, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Hu, Yanmei; Wang, Jun] Univ Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA in 2021, Cited 41. Product Details of 123-11-5. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Neuraminidase (NA) inhibitors play a prime role in treating influenza. However, a variety of viruses containing mutant NAs have developed severe drug resistance towards NA inhibitors, so it is of crucial significance to solve this problem. Encouraged by urea-containing compound 12 disclosed by our lab, we designed a series of oseltamivir derivatives bearing hydrazide fragment for targeting the 150 cavity. Among the synthesized compounds, compound 17a showed 8.77-fold, 4.12-fold, 203-fold and 6.23-fold more potent activity than oseltamivir carboxylate against NAs from H5N1, H1N1, H5N1-H274Y, H1N1-H274Y, respectively. Meanwhile, the best compound 17a exhibited satisfactory metabolic stability in vitro. This study offers an important reference for the structural optimization of oseltamivir aiming at potent inhibition against H274Y mutant of NAs. (C) 2021 Elsevier Masson SAS. All rights reserved.
Product Details of 123-11-5. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Zhao, HQ; Jiang, SY; Ye, ZF; Zhu, HX; Hu, BC; Meng, PP; Hu, YM; Zhang, HC; Wang, KL; Wang, J; Tian, YS or concate me.
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