|
Synthesis and Investigation of Antibacterial, Antimycobacterial Activity and Cytotoxicity Study of Sparfloxacin Derivatives
|
|
| Author:
|
GULSHAN GURUNANI, KAPIL AGRAWAL, SHEELPRIYA WALDE, ABHAY ITTADWAR
|
| Abstract:
|
Based on earlier pieces of evidence of N-piperazinyl fluoroquinolone, and in search of new bioactive molecules
from the fluoroquinolone class, the derivates of N-substituted piperazinyl quinolones were synthesized. A
series of 2-((amino-1,3,4-thiadiazol-2yl)thio)-1-(4-subst.) (3a–j) were used for diazotization of amines in
concentrated hydrochloric acid in the presence of Cu-powder, resulting into 2-((5-chloro-1, 3, 4-thiadiazol-
2yl)thio)-1-(4-subst.)ethanone (4a-j). The reaction of (4a-j) with piperazinyl quinolone in dimethylformamide
resulted (5a-j). The structure of synthesized compounds was confirmed by their spectral analysis. The
compounds are screened against Staphylococcus aureus, Bacillus subtilis(Gram positive)and Escherichia coli,
Pseudomonas aeruginosa,(Gram negative) and mycobacterium tuberculosis. The findings revealed moderate
activity against Gram-positiveand poorly active against Gram-negative bacteria. Results indicated that
halogenated analogs with nitro substitution (5b, 5e, and 5j) derivatives revealed antibacterial and
antimycobacterial activity. The results advocate the need for further exploration of such derivatives, coupled
with their preclinical and clinical investigation.
|
| Keyword:
|
2-amino-benzoylthio-1, 3, 4-thiadiazole, Fluoroquinolone, N-piperazinyl quinolone, Sparfloxacin, synthesis, antibacterial activity
|
| EOI:
|
-
|
| DOI:
|
https://doi.org/10.31838/ijpr/2021.13.02.492
|
| Download:
|
Request For Article
|
|
|