期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 75, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2022.128930
关键词
Nitrofuran; Nitroindazole; Nitroreductase; Medicinal chemistry; Trypanosoma; Leishmania
This review presents a comprehensive overview of nitrocompounds that have been reported as inhibitors against Trypanosoma cruzi, T. brucei rhodesiense, and T. b. gambiense parasites. The activities and structure-activity relationship analyses of these compounds are highlighted, providing valuable information for research teams seeking novel trypa-nocidal and leishmanicidal agents.
Chagas disease and Human African trypanosomiasis (HAT) are caused by Trypanosoma cruzi, T. brucei rhodesiense or T. b. gambiense parasites, respectively; while Leishmania is caused by parasites from the Leishmania genus. In recent years, many efforts have been addressed to develop inhibitors against these parasites, especially nitro -containing derivatives, which can interfere with essential enzymes from the protozoa. In this review, all anti-trypanosomatidae nitrocompounds reported so far are shown herein, highlighting their activities and SAR an-alyses, providing all the benefits and problems associated with this ambiguous chemical group. Finally, this review paper will be useful for many research teams around the world, which are searching for novel trypa-nocidal and leishmanicidal agents.
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