Structure activity relationships of synthetic antibiotic analogues of chryscandin
| Autor: | Hiroshi Imanaka, Hiroyuki Setoi, Kazuo Sakane, Tsutomu Teraji, Tadaaki Komori, Yoshio Kawai, Masanobu Kohsaka |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
Pharmacology
Antifungal Agents medicine.drug_class Stereochemistry Antibiotics Biological activity Microbial Sensitivity Tests Biology Puromycin Aminonucleoside Corpus albicans In vitro Mice Structure-Activity Relationship Biochemistry In vivo Drug Discovery medicine Moiety Animals Ketoconazole Nucleoside medicine.drug |
| Zdroj: | The Journal of antibiotics. 38(9) |
| ISSN: | 0021-8820 |
| Popis: | Anti-yeast activity with a series of chryscandin derivatives showed that the O-methyl-L-tyrosyl moiety is not always required for activity at the target site. On the other hand, the adenyl-3'-aminoribofuranuronic acid moiety seems to be essential for biological activity. Therefore, the various acyl derivatives on the amino group of the sugar part of the nucleoside were synthesized. 1-(6-Amino-9H-purin-9-yl)-3-(S-benzyl-L-cysteinylamino)- 1,3-dideoxy-beta-D-ribofuranuronic acid (16) showed the highest efficacy among them against Candida albicans. It exhibited sixteen-fold enhanced activity in vitro compared with that of native chryscandin. The in vivo activity of 16 against experimental infection of C. albicans showed the almost same as that of 5-fluorocytosine and a superior to that of ketoconazole. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|