Abstract |
A novel series of coumarin derivatives 6a-o, bearing isoxazole moieties were designed and synthesized. After that, they were evaluated for melanin synthesis in murine B16 cells and inhibitory effect on the growth of CA (Candida albicans), EC (Escherichia coli), SA (Staphylococcus aureus). It was found that eleven compounds (6b-f, 6j-o) showed a better activity on melanin synthesis than positive control (8-MOP). Among them, compounds 6d (242%) and 6f (390%), with nearly 1.6 and 2.6-fold potency compared with 8-MOP (149%) respectively, were recognized as the most promising candidate hits for further pharmacological study of anti- vitiligo. Seven halogen substituted compounds exhibited moderate antimicrobial activity against CA. It is interesting that 6e-f and 6l-m, which had two halogens on the benzene showed a comparable activity with Amphotericin B against CA. The evaluation of melanin synthesis in B16 cells and inhibitory effect on bacteria of above structurally diverse derivatives had also led to an outline of structure-activity relationship.
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Authors | Guang Xian Pang, Chao Niu, Nuramina Mamat, Haji Akber Aisa |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 27
Issue 12
Pg. 2674-2677
(06 15 2017)
ISSN: 1464-3405 [Electronic] England |
PMID | 28476568
(Publication Type: Journal Article)
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Copyright | Copyright © 2017 Elsevier Ltd. All rights reserved. |
Chemical References |
- Anti-Bacterial Agents
- Coumarins
- Isoxazoles
- Melanins
- coumarin
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Topics |
- Anti-Bacterial Agents
(chemical synthesis, chemistry, pharmacology)
- Candida albicans
(drug effects, growth & development)
- Cell Line, Tumor
- Cell Survival
(drug effects)
- Coumarins
(chemical synthesis, chemistry, pharmacology)
- Dose-Response Relationship, Drug
- Escherichia coli
(drug effects, growth & development)
- Humans
- Isoxazoles
(chemistry, pharmacology)
- Melanins
(biosynthesis)
- Microbial Sensitivity Tests
- Molecular Structure
- Staphylococcus aureus
(drug effects, growth & development)
- Structure-Activity Relationship
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