Synthesis and in vitro antiprotozoal evaluation of novel metronidazole-Schiff base hybrids.
Arch Pharm (Weinheim)
; 356(3): e2200409, 2023 Mar.
Article
in En
| MEDLINE
| ID: mdl-36446720
ABSTRACT
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 IC50 values < 5 µM. Compound 20, the most active compound against T. vaginalis, exhibited an IC50 value of 3.4 µM. A few compounds also exhibited activity against Plasmodium falciparum and Trypanosomal brucei brucei, with compound 6 exhibiting an IC50 value of 0.7 µM against P. falciparum and compound 22 exhibiting an IC50 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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Trichomonas vaginalis
/
Malaria, Falciparum
/
Antiprotozoal Agents
Limits:
Humans
Language:
En
Journal:
Arch Pharm (Weinheim)
Year:
2023
Document type:
Article
Affiliation country:
South Africa