Antitrypanosomal activity of new semi-synthetic bergenin derivatives.
| Autor: | El-Hawary SS; Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Mohammed R; Pharmacognosy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt., AbouZid S; Pharmacognosy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt., Zaki MA; Pharmacognosy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt., Ali ZY; Biochemistry Department, National Organization for Drug Control and Research (NODCAR), Giza, Egypt., Elwekeel A; Pharmacognosy Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt., Elshemy HAH; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt. |
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| Jazyk: | angličtina |
| Zdroj: | Chemical biology & drug design [Chem Biol Drug Des] 2022 Feb; Vol. 99 (2), pp. 179-186. Date of Electronic Publication: 2021 Dec 29. |
| DOI: | 10.1111/cbdd.14000 |
| Abstrakt: | Bergenin and 11-O-(4'-O-methyl galloyl)-bergenin, previously isolated from Crassula capitella extract, were used as starting materials for the synthesis of eight derivatives; four derivatives 2a-2d were synthesized from bergenin through the formation of ester derivatives and four alkyl derivatives 4a-4d were synthesized from 11-O-(4'-O-methyl galloyl)-bergenin. The structures of the synthesized analogues were confirmed upon 1 H and 13 C NMR spectroscopic elucidation. Antileishmanial and antitrypanosomal activities of the synthesized derivatives were evaluated, compounds 11-O-(3',5' di-benzyl, 4'-O-methyl galloyl)-8,10-di-O-benzyl-bergenin (4c) and 11-O-(3',5'di-4-chlorobenzyl,4'-O-methyl galloyl)-8,10di-O-4-chlorobenzyl bergenin (4d) showed potent antitrypanosomal activity with IC (© 2021 John Wiley & Sons A/S.) |
| Databáze: | MEDLINE |
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