Synthesis and antimicrobial activity evaluation of pyrazole derivatives containing the imidazo[2,1-b][1,3,4]thiadiazole moiety.
Arch Pharm (Weinheim)
; 356(8): e2300110, 2023 Aug.
Article
in En
| MEDLINE
| ID: mdl-37328442
ABSTRACT
Four series of novel pyrazole derivatives (compounds 17a-m, 18a-m, 19a-g, and 20a-g) were synthesized, and their antibacterial and antifungal activities were evaluated. Most of the target compounds (17a-m, 18k-m, and 19b-g) showed strong antifungal activity and high selectivity relative to both Gram-positive and Gram-negative bacteria. Among them, compounds 17l (minimum inhibitory concentration [MIC] = 0.25 µg/mL) and 17m (MIC = 0.25 µg/mL) showed the strongest antifungal activity, being 2- and 4-fold more active than the positive controls gatifloxacin and fluconazole, respectively. In particular, compound 17l showed little cytotoxicity against human LO2 cells and did not exhibit hemolysis at ultrahigh concentrations, as did the positive control compounds gatifloxacin and fluconazole. These results indicate that these compounds are valuable for further development as antifungal agents.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thiadiazoles
/
Anti-Bacterial Agents
Limits:
Humans
Language:
En
Journal:
Arch Pharm (Weinheim)
Year:
2023
Document type:
Article
Affiliation country:
China