Počet záznamů: 1
Synthesis and Antitrypanosomal Activity of 6-Substituted 7-Methyl-7-deazapurine Nucleosides
- 1.0541879 - ÚOCHB 2022 RIV US eng J - Článek v odborném periodiku
Perlíková, Pavla - Krajczyk, Anna - Doleželová, Eva - Slapničková, Martina - Milisavljevič, Nemanja - Poštová Slavětínská, Lenka - Tloušťová, Eva - Gurská, S. - Džubák, P. - Hajdúch, M. - Zíková, Alena - Hocek, Michal
Synthesis and Antitrypanosomal Activity of 6-Substituted 7-Methyl-7-deazapurine Nucleosides.
ACS Infectious Diseases. Roč. 7, č. 4 (2021), s. 917-926. ISSN 2373-8227
Grant CEP: GA MŠMT(CZ) EF16_019/0000729; GA MŠMT(CZ) EF16_019/0000759; GA ČR(CZ) GA19-08124S; GA ČR(CZ) GA19-07707S; GA MŠMT(CZ) LM2015064
Grant ostatní: AV ČR(CZ) AP1501
Program: Akademická prémie - Praemium Academiae
Institucionální podpora: RVO:61388963 ; RVO:60077344
Klíčová slova: nucleosides * antiparasitic activity * antitrypanosomal * cytotoxicity
Obor OECD: Organic chemistry; Organic chemistry (BC-A)
Impakt faktor: 5.578, rok: 2021
Způsob publikování: Omezený přístup
https://doi.org/10.1021/acsinfecdis.1c00062
Human African Trypanosomiasis caused by Trypanosoma brucei species is one of the most damaging neglected tropical diseases. While the number of newly diagnosed cases per year is record low, there is still high interest in the development of new antitrypanosomal agents in case of resistance to currently used drugs and their combinations, and to replace drugs with serious side effects. We report a series of 7-methyl-7-deazapurine (5-methyl-pyrrolo[2,3-d]pyrimidine) ribonucleosides bearing alkyl, methylsulfanyl, methylamino, or diverse alkoxy groups at position 6 that was prepared through glycosylation of 6-chloro-7-methyl-7-deazapurine followed by nucleophilic substitutions or cross-coupling reactions at position 6 and deprotection. Most of the title nucleosides displayed significant activity against Trypanosoma brucei brucei and T. b. gambiense at submicromolar or nanomolar concentrations and low cytotoxicity and thus represent promising candidates for further development.
Trvalý link: http://hdl.handle.net/11104/0319376
Počet záznamů: 1