Synthesis of Perspicamide A and Related Diverse Analogues: Their Bioevaluation as Potent Antileishmanial Agents

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• 作者：Anand Kumar Pandey ; Rashmi Sharma ; Rahul Shivahare ; Ashish Arora ; Neeraj Rastogi ; Suman Gupta ; Prem M. S. Chauhan
• 刊名：The Journal of Organic Chemistry
• 出版年：2013
• 出版时间：February 15, 2013
• 年：2013
• 卷：78
• 期：4
• 页码：1534-1546
• 全文大小：484K
• 年卷期：v.78,no.4(February 15, 2013)
• ISSN：1520-6904

文摘

The first protocol for the synthesis of perspicamide A and related diverse analogues has been developed from economical and readily available starting materials. Furthermore, a few synthesized analogues, 24a, 24b, 24c, 24d, and 24l, exhibited potent activity against Leishmania donovani with IC₅₀ values ranging from 3.75 to 10.37 渭M and a selectivity index (SI) ranging from 9.58 to 53.12, which is improved compared to the standard drug Miltefosine (IC₅₀ 12.4 渭M and SI 4.1).