Synthesis and in vitro biological evaluation of novel coumarin derivatives containing isoxazole moieties on melanin synthesis in B16 cells and inhibition on bacteria
文献类型：期刊论文
| 作者 | Pang, GX (Pang, Guang Xian); Niu, C (Niu, Chao); Mamat, N (Mamat, Nuramina); Aisa, HA (Aisa, Haji Akber)
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2017 |
| 卷号 | 27期号:12页码:2674-2677 |
| 关键词 | Vitiligo Melanin synthesis Antimicrobial activity Coumarin derivatives SAR |
| 通讯作者 | Aisa, HA |
| 英文摘要 | 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. (C) 2017 Elsevier Ltd. All rights reserved. |
| 收录类别 | SCI |
| WOS记录号 | WOS:000402472600007 |
| 源URL | [http://ir.xjipc.cas.cn/handle/365002/4814]  |
| 专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 新疆理化技术研究所_资源化学研究室 |
| 作者单位 | Chinese Acad Sci, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China；Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China；Univ Chinese Acad Sci, 19 A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Pang, GX ,Niu, C ,Mamat, N ,et al. Synthesis and in vitro biological evaluation of novel coumarin derivatives containing isoxazole moieties on melanin synthesis in B16 cells and inhibition on bacteria[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2017,27(12):2674-2677. |
| APA | Pang, GX ,Niu, C ,Mamat, N ,&Aisa, HA .(2017).Synthesis and in vitro biological evaluation of novel coumarin derivatives containing isoxazole moieties on melanin synthesis in B16 cells and inhibition on bacteria.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,27(12),2674-2677. |
| MLA | Pang, GX ,et al."Synthesis and in vitro biological evaluation of novel coumarin derivatives containing isoxazole moieties on melanin synthesis in B16 cells and inhibition on bacteria".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27.12(2017):2674-2677. |
入库方式： OAI收割
来源：新疆理化技术研究所
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