The design, synthesis and antiplasmodial evaluation of novel sulfoximine-isoxazole hybrids as potential antimalarial agents

被引：3

作者：

Mabasa, Jackie L. ^{[1
]}

Mabasa, Tommy F. ^{[1
]}

Nyathi, Musawenkosi L. ^{[1
]}

Moshapo, Paseka T. ^{[1
]}

机构：

[1] Univ Johannesburg, Res Ctr Synth & Catalysis, Dept Chem Sci, ZA-2006 Johannesburg, South Africa

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS | 2024年 / 10卷

基金：

新加坡国家研究基金会;

关键词：

Sulfoximine; Isoxazole; Antimalarial; Antiplasmodial; Sulfoximine-isoxazole hybrids; NH-SULFOXIMINES; ARYL IODIDES; METAL-FREE; REDUCTION; MALARIA; THIOLS; INHIBITORS; CATALYST; ACCESS;

D O I：

10.1016/j.ejmcr.2023.100128

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of novel sulfoximine-isoxazole hybrids was synthesized and evaluated for antimalarial activity. The subsequential synthetic pathways, which included the alkylation of thiols and simultaneous sulfide oxidation and imination, yielded a library of sulfoximine derivatives 3a-s. These were coupled with brominated-isoxazoles 6a -c, to give sulfoximine-isoxazole hybrids 7a-v and further derivatized to compounds 8 and 9. The hybrid com-pounds were then investigated for their antiplasmodial activity against the wild-type drug-sensitive strain (NF54) and multidrug-resistant strain (K1). Only six (6) hybrids showed minor potency against the drug-sensitive and drug-resistant strains (IC50 values ranging between 4.1 and 5.8 mu M). The selectivity studies indicated no significant toxicity of the hybrid compounds against mammalian cells.

引用

页数：11

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