Asian Journal of Research in Chemistry

Hemant Badwaik ¹, S. Venkataraman ², Deepa Thakur ¹, Minu Vinod ¹, J. Raamamurthy ¹, Kiran Deshmukh ²

Affiliations
1 Rungta College of Pharmaceutical Sciences and Research, Bhilai (C.G), IN
2 K.M. College of Pharmacy, Madurai (T.N), IN

Abstract

Acetanilide was cyclized via Vilsmeier-Haack reagent to give 2- chloro -3- formyl quinoline. The aldehydic group was protected to prevent the preferential attack of nitrogen nucleophiles. The protection of aldehydic group in the present system was achieved with ethylene glycol to afford dioxolan derivative. Dioxolan derivative treated with nitro substituted phenyl hydrazine in alcoholic solution followed by deprotection of aldehydic group afforded the 2-(2-(2- nitrophenyl) hydrazinyl) quinoline-3-carbaldehyde and 2-(2-(2, 4-dinitrophenyl) hydrazinyl) quinoline-3- carbaldehyde. The synthesized derivatives were screened for antimicrobial activity.

Keywords

Vilsmeier–Haack Reagent, Dioxolan, 2-(2-(2, 4-Dinitrophenyl) Hydrazinyl) Quinoline-3- Carbaldehyde, Antimicrobial Agent.

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Suresh Rajput ¹, Dharamveer Sisodia ¹, Hemant Badwaik ², Deepa Thakur ², Kushagra Nagori ²

Affiliations
1 Ultra College of Pharmacy, Madurai (T.N), IN
2 Rungta College of Pharmaceutical Sciences and Research, Bhilai (C.G), IN

Abstract

A novel 5(4-(4-substituted)Aminobenzylidine)thiazolidine-2,4-dione derivatives were synthesized and characterized by IR and H-NMR spectral analysis. Antibacterial and antifungal activities of the compounds were assessed by in vitro growth inhibitory activity against Escherichia coli, Staphylococcus aureus, Asperigillus niger, Candida albicans by using the disc diffusion method. Most of all compounds exhibited significant antibacterial activity against Staphylococcus aureus and Escherichia coli, while weak antifungal activity against Asperigillus niger and Candida albicans.

Keywords

Thiazolidine-2,4-dione, Antibacterial and Antifungal Activity, Disc Diffusion Method.

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Hemant Badwaik ¹, Sandeep Sonkar ¹, Mukesh Singh ¹, Suresh Rajpal ¹, Dharamveer Sisodiya ¹, Ajit Pandey ¹

Affiliations
1 Ultra College of Pharmacy, Madurai, Tamil Nadu, IN

Abstract

The present work deals with synthesis and evaluation of some novel phenylthiazole and quinazoline combination derivatives of biological interest. The reaction of acetophenone with thiourea formed 4-phenylthiazol-2-amine (I) was refluxed with N-chloroacetyl anthranillic acid (II) in the presence of K₂CO₃ in dry ethanol under anhydrous condition yields 2-chloromethyl-3-[4-(phenyl)thiazol-2-yl]-quinazolin-4(3H)one(III). The 2-chloromethyl-3-[4-(phenyl) thiazol-2-yl] quinazolin-4(3H)–one(III) and respective aromatic amines was refluxed in dry pyridine and acetic anhydride formed N-3-[4-(4–phenyl) thiazol–2–yl]-[2-(substituted amino) methyl] quinazoline-4 (3H)-one derivatives (IV).The synthesized compounds are to be screened for antibacterial activity.

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