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 CuSO₄.5H₂O at 90^oC. 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 IC₅₀ values in the range of 0.1‐20 μg/mL and were also found to be non‐cytotoxic under tested conditions.

中文翻译：

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[1，2,3]-三唑系磺酰胺-小ber碱杂种的合成及抗疟疾评估

尽管有有效的控制和治疗措施，疟疾仍然是一个全球性的健康问题。在本研究中，通过不同的伯，仲和叔磺酰胺基叠氮化物与9-的惠斯根[3 + 2]环加成反应，以高收率合成了一系列新的[1,2,3]-三唑系磺酰胺-小ber碱杂种。在t- BuOH：水（1：1）混合物中的O-（丙炔）小ber碱氯化物，在90 ^o C时含有催化量的抗坏血酸钠和CuSO ₄ .5H ₂ O.在光谱表征后，对这些新型杂种的功效进行了评估对抗恶性疟原虫的无性红细胞生成阶段（3D7）体外。大多数合成的化合物显示出显着的抗疟活性，IC ₅₀值在0.1-20μg/ mL的范围内，并且在测试条件下也被发现具有无细胞毒性。