SYNTHESIS, IN VITRO ANTIMICROBIAL ACTIVITY OF SCHIFF'S BASE, AZETIDINONES AND THIAZOLIDINONES

Objective: The objective of the present study is to synthesize 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n]. The structure of all synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral studies. Methods: The titled compounds 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n] were synthesized by the reaction of N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene } substituted anilin [3a-n] with chloro acetyl chloride and thioglycolic acid respectively. Compounds N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene} substituted aniline [3a-n] were synthesized by the reaction of 3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-carbaldehyde [2] with primary aromatic amine in alcohol. All compounds were evaluated for their antimicrobial activity.Results: Compounds 3a,3b,3d,3j,3l,4d,4e,4j,4l,4m,5e,5g,5h,5n exhibited excellent to good antibacterial activity as compared to reference drugs.Conclusion: In summary, N-{[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyraol-4-yl] methylene } substituted anilin [3a-n], 3-Chloro-4-[3-(2,4-dichloro-5-fluoro phenyl)-1H-pyrazol-4-yl]-1-(substituted) azetidin-2-one [4a-n] and 2-[3-(2,4-Dichloro-5-fluoro phenyl)-1H-pyraol-4-yl]-3-(substituted phenyl)-1,3-thiazolidin-4-one [5a-n] derivatives have been synthesized and characterized. In vitro antimicrobial testing of the compounds was carried out by microdilution Method. Amongst the synthesised compounds, many of them had proven their antimicrobial potency which varies from good to excellent

COMPARATIVE STUDIES OF NOVEL OXADIAZOLE DERIVATIVE HAVING CHIRAL CENTER ANDTHEIRANTI-MICROBIAL ACTIVITIES

Objective: To synthesize a series of (-) S & (+) S oxadiazole derivatives by the reaction of (-) (2S)-2-amino-2-(2-chlorophenyl) acetohydrazide & (+) (2S)-2-amino-2-(2-chloro phenyl) acetohydrazide with con. H2SO4, L(+) Tartaric acid, L(-) Tartaric acid, Hydrazine Hydrate, POCl3 and Various aromatic acid respectively. Methods: The structures of novel synthesized compounds have been established on the basis of elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data and screened for their antibacterial and antifungal activities against different microorganisms by micro dilution method. Gentamycin, Ampicillin, Chloramphenicol, Ciprofloxacin, Norfloxacin, Nystatin, Greseofulvin were used as standard drugs for bacterial and fungus. Results: The newly synthesized compounds indicate that some of them show better antibacterial and antifungal activity than compared to their reference drug. Conclusion: Comparison of 1, 3, 4 oxadiazole having chiral center, characterized and exhibited promising antibacterial and antifungal activity