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Information × Registration Number 0221U106656, 0120U104978 , R & D reports Title Design and synthesis of new electron-deficient azoles active against viruses causing opportunistic infections popup.stage_title Head Brovarets Volodymyr S., д.х.н. Registration Date 16-12-2021 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2  Preparative methods for the synthesis of new 4,5-disulfonyl-substituted imidazoles and azoles containing triphenylphosphonium group at the 4 position have been developed. Preparative methods for the synthesis of new 5-amino-, 5-sulfur-containing oxazoles containing cyano-, ester, phosphoryl, thio-, and sulfonyl groups at the different positions have been developed and improved. Methods for obtaining new trisulfonyl-substituted thiazoles have been improved. A number of QSAR models have been developed to predict the antiviral activity of azole derivatives against Cytomegalovirus, Varicella-Zoster Virus, Herpes Simplex Virus, Papillomavirus, Zika Virus, resulting in the identification for further research of 20 imidazoles, 69 oxazoles and 31 thiazoles with potential activity, among which compounds with significant action were found. The activity of imidazole, oxazole and thiazole derivatives has been investigated in vitro against Cytomegalovirus, Rabies Virus, Herpes Simplex Virus and Varicella-Zoster Virus, including substances with high antiviral activity, which in some cases exceed the activity of control drugs. A number of enzymes and proteins that may be involved in the antiviral mechanisms of azoles have been analyzed. It has been shown that imidazole derivatives can be efficiently located in the substrate centers of thymidylate synthase and thymidine kinase of Varicella-Zoster Virus, as well as in ATP-binding centers of casein kinases and cyclin-dependent human kinases. Oxazole and thiazole derivatives have been demonstrated to be inhibitors of CK2, CDK1, CDK2, CDK9, p38 MAP kinase and mTOR. The work is performed at a high scientific level using modern methods. Product Description popup.authors Buldenko Vladyslav M. Veligina Yevheniia S. Zhirnov Viktor V. Zyabrev Volodymyr S. Kachaeva Maryna V. Kobzar Olexandr L. Kovalishyn Vasiliy V. Pilyo Stepan G. popup.nrat_date 2021-12-16 Close