Synthesis and in vitro antiprotozoal evaluation of novel metronidazole-Schiff base hybrids.
Archiv der Pharmazie(2023)
摘要
Herein we report the synthesis of 21 novel small molecules inspired by metronidazole and Schiff base compounds. The compounds were evaluated against Trichomonas vaginalis and cross-screened against other pathogenic protozoans of clinical relevance. Most of these compounds were potent against T. vaginalis, exhibiting IC values < 5 µM. Compound 20, the most active compound against T. vaginalis, exhibited an IC value of 3.4 µM. A few compounds also exhibited activity against Plasmodium falciparum and Trypanosomal brucei brucei, with compound 6 exhibiting an IC value of 0.7 µM against P. falciparum and compound 22 exhibiting an IC value of 1.4 µM against T.b. brucei. Compound 22 is a broad-spectrum antiprotozoal agent, showing activities against all three pathogenic protozoans under investigation.
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关键词
Schiff base,Trichomonas vaginalis,antiprotozoal agent,metronidazole
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