期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 -, 期 -, 页码 -出版社
WILEY
DOI: 10.1111/cbdd.14284
关键词
2-Aroyl quinazolinone derivatives; anti-leishmanial activity; anti-trypanosomal activity; one-pot oxidation
In this study, the synthesis of 2-aroyl quinazolinones and their antiprotozoal efficacy against Trypanosoma brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania infantum were reported. Thirteen out of the twenty target compounds inhibited the growth of these parasites, with compounds KJ1 and KJ10 exhibiting IC50 values of 4.7 μM (T. b. brucei) and 1.1 μM (T. b. rhodesiense), respectively.
Trypanosomes and Leishmania are parasitic protozoans that affect millions of people globally. Herein we report the synthesis of 2-aroyl quinazolinones and their antiprotozoal efficacy against Trypanosoma brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania infantum. These compounds were counter-screened against a human cell line for cytotoxicity. Thirteen of the twenty target compounds in this study inhibited the growth of these parasites, with compounds KJ1, and KJ10 exhibiting IC50 values of 4.7 mu M (T. b. brucei) and 1.1 mu M (T. b. rhodesiense), respectively.
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