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Diclofenac‐Based Hydrazones and Spirothiazolidinones: Synthesis, Characterization, and Antimicrobial Properties
Ist Teil von
Archiv der Pharmazie (Weinheim), 2017-05, Vol.350 (5), p.n/a
Ort / Verlag
Germany: Wiley Subscription Services, Inc
Erscheinungsjahr
2017
Link zum Volltext
Quelle
Wiley Online Library Journals Frontfile Complete
Beschreibungen/Notizen
We report here the synthesis, structural characterization, and biological evaluation of novel diclofenac‐based hydrazone (4a–f) and spirothiazolidinone (5a–f, 6a–f) derivatives designed as potential antimicrobial agents. The compounds were evaluated in vitro for their antiviral activity against a wide spectrum of DNA and RNA viruses. They were further screened in vitro against different strains of bacteria and fungi. The hydrazone derivatives, 4a and 4c–f, were found to be active against herpesviruses (HSV‐1, HSV‐2, and HSV‐1 TK−), vaccinia virus, and Coxsackie B4 virus, with EC50 values between 6.6 µg/mL and 14.7 μg/mL, and the selectivity index values were greater than 10 for 4a and 4f. The newly synthesized compounds (4–6) were inactive against the bacterial and the fungal strains tested, at levels below 2500, 1250, or 625 μg/mL. Interestingly, the key intermediate 3 with a free hydrazide moiety displayed antifungal properties against Candida albicans and C. parapsilosis at MIC values of 4.88 µg/mL and 78.12 μg/mL, respectively.
A new series of diclofenac‐based hydrazones (4a–f) and spirothiazolidinones (5a–f, 6a–f) were synthesized and assayed for antimicrobial activity against a wide spectrum of viral, bacterial, and fungal pathogens. The hydrazone derivatives, 4a and 4c–f, were found to be active against herpesviruses (HSV‐1, HSV‐2, and HSV‐1 TK–), vaccinia virus, and Coxsackie B4 virus, with EC50 values between 6.6 µg/mL and 14.7 µg/mL, and the selectivity index values were greater than 10 for 4a and 4f.