磺胺
环加成
恶性疟原虫
小檗碱
三唑
点击化学
化学
1,2,3-三唑
氯化物
效力
组合化学
催化作用
体外
生物
疟疾
立体化学
有机化学
生物化学
免疫学
作者
Neha Batra,Vinoth Rajendran,Drishti Agarwal,Ishan Wadi,Prahlad C. Ghosh,Rinkoo Devi Gupta,Mahendra Nath
标识
DOI:10.1002/slct.201801905
摘要
Abstract Malaria still remains a global health problem despite of the availability of effective control and treatment measures. In the present study, a novel series of [1, 2,3]‐triazole tethered sulfonamide‐berberine hybrids were synthesized in good yields via Huisgen [3+2] cycloaddition reaction of various primary, secondary and tertiary sulfonamide based azides with 9‐O‐(propyne)berberine chloride in t ‐BuOH:water (1:1) mixture containing a catalytic amount of sodium ascorbate and CuSO 4 .5H 2 O at 90 o C. After spectroscopic characterization, these novel hybrids were evaluated for their potency against asexual erythrocytic stages of P. falciparum (3D7) in vitro. Most of the synthesized compounds have shown significant antimalarial activity with IC 50 values in the range of 0.1‐20 μg/mL and were also found to be non‐cytotoxic under tested conditions.
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