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Synthesis and in vitro biological evaluation of novel coumarin derivatives containing isoxazole moieties on melanin synthesis in B16 cells and inhibition on bacteria
Pang, GX (Pang, Guang Xian); Niu, C (Niu, Chao); Mamat, N (Mamat, Nuramina); Aisa, HA (Aisa, Haji Akber)
2017
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume27Issue:12Pages:2674-2677
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. (C) 2017 Elsevier Ltd. All rights reserved.

KeywordVitiligo Melanin Synthesis Antimicrobial Activity Coumarin Derivatives Sar
DOI10.1016/j.bmcl.2017.04.039
Indexed BySCI
WOS IDWOS:000402472600007
Citation statistics
Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/4814
Collection省部共建新疆特有药用资源利用重点实验室
资源化学研究室
Corresponding AuthorAisa, HA (Aisa, Haji Akber)
Affiliation1.Chinese Acad Sci, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China
2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China
3.Univ Chinese Acad Sci, 19 A Yuquan Rd, Beijing 100049, Peoples R China
Recommended Citation
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.
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