期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 176, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.ejps.2022.106242
关键词
Leishmaniasis; Amastigote; Nifuroxazide; Analogues; Cytotoxicity
资金
- National Research Foundation of South Africa [129324]
- North-West University
Leishmaniasis is a neglected tropical disease, and new drugs are needed to overcome the limitations of current treatments. This study synthesized a series of nifuroxazide analogues and identified compounds 1l, 2c, and 2d as potential candidates with antileishmanial activity.
Leishmaniasis is a neglected tropical disease affecting millions of people worldwide, with 650 000 to 1.1 million new infections reported annually by the World Health Organization. Current antileishmanial treatments are unsatisfactory due to the development of parasitic resistance and the toxicity associated with the drugs used, and this highlights the need for the development of new antileishmanial drugs. In this study, a series of nifuroxazide analogues were synthesized in a single step reaction and investigated for their antileishmanial potential. The sulfonate 1l, bearing pyridine ring, was deemed an antileishmanial hit, targeting the amastigotes of Leishmania (L.) donovani and L. major, the pathogens of visceral and cutaneous leishmaniasis, respectively, with micromolar potencies. The benzyl analogues 2c and 2d were also confirmed as submicromolar active leads against amasti-gotes of L. major. These analogues stand as promising candidates for further investigation involving the evalu-ation of their in vivo activities and molecular targets.
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