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Synthesis and Antitrypanosomal Activity of 6-Substituted 7-Methyl-7-deazapurine Nucleosides
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SYSNO ASEP 0541879 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Synthesis and Antitrypanosomal Activity of 6-Substituted 7-Methyl-7-deazapurine Nucleosides Author(s) Perlíková, Pavla (UOCHB-X) RID, ORCID
Krajczyk, Anna (UOCHB-X)
Doleželová, Eva (BC-A) RID
Slapničková, Martina (BC-A) RID
Milisavljevič, Nemanja (UOCHB-X)
Poštová Slavětínská, Lenka (UOCHB-X) RID
Tloušťová, Eva (UOCHB-X) RID, ORCID
Gurská, S. (CZ)
Džubák, P. (CZ)
Hajdúch, M. (CZ)
Zíková, Alena (BC-A) RID, ORCID
Hocek, Michal (UOCHB-X) RID, ORCIDSource Title ACS Infectious Diseases. - : American Chemical Society - ISSN 2373-8227
Roč. 7, č. 4 (2021), s. 917-926Number of pages 10 s. Language eng - English Country US - United States Keywords nucleosides ; antiparasitic activity ; antitrypanosomal ; cytotoxicity OECD category Organic chemistry R&D Projects EF16_019/0000729 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) EF16_019/0000759 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) GA19-08124S GA ČR - Czech Science Foundation (CSF) GA19-07707S GA ČR - Czech Science Foundation (CSF) LM2015064 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Method of publishing Limited access Institutional support UOCHB-X - RVO:61388963 ; BC-A - RVO:60077344 UT WOS 000639068100019 EID SCOPUS 85104160540 DOI 10.1021/acsinfecdis.1c00062 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2022 Electronic address https://doi.org/10.1021/acsinfecdis.1c00062
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