Journal of Chemistry

Papers

Voulume: 17
Issue: 3
Article No. 1
Synthesis of Fluorinated Heterocyclic Compounds for Pharmacological Screening
NIVYA BINOY
Department Of Pharmaceutical Chemistry, Nargund College of Pharmacy, Rajiv Gandhi University of Health Sciences, Bengaluru. 560085 (India)
SHACHINDRA L. NARGUND
Department Of Pharmaceutical Chemistry, Nargund College of Pharmacy, Rajiv Gandhi University of Health Sciences, Bengaluru. 560085 (India)
SHRAVAN L. NARGUND
Department Of Pharmaceutics, Nargund College of Pharmacy, Rajiv Gandhi University of Health Sciences, Bengaluru-560085 (India)
RAMA NARGUND
Department Of Pharmacology, Nargund College of Pharmacy, Rajiv Gandhi University of Health Sciences, Bengaluru-560085 (India)
Abstract :

A series of derivatives of (E)-6-chloro-5-fluoro-2-styryl-1H-benzo[d]imidazole, and 5-fluoro-2-methylN-phenyl-1H-benzo[d]imidazol-6-amine was synthesized. Compounds confirmed by melting point, FT-IR, 1HNMR, Mass spectral analytical techniques and predicted for their ADME, Pharmacokinetic properties.Synthesized compounds screened for better antibacterial and antiinflammatory activity. To synthesize a series of novel trisubstituted fluorinated benzimidazole derivatives and evaluate the physicochemical, ADME and pharmacokinetic properties and biological activity. The starting material Flouro-chloro-aniline ona series of reaction such as acetylation, nitration, deacetylation followed by reductionto get 4-fluoro-5-chloroorthophenylene diamine. The di-amino compound cyclized with acetyl chloride to obtain 6-chloro-5-fluoro-2- methyl-1H-benzimidazole which on reaction with various aromatic aldehyde forms series of compounds 31(a-h), and with various anilines forms compounds 32(a-j). Physicochemical, ADME and pharmacokinetic properties predicted Insilco. Antimicrobial activity screened by Agar diffusion method. In vitro antiinflammatory activity screened by protein denaturation assay.The compounds synthesized confirmed by melting Point, FT-IR, 1HNMR, Mass spectral analytical techniques and predicted for their ADME, Pharmacokinetic properties in silico. The compounds screened and confirmed with moderate antimicrobial, and in vitro antiinflammatory activity.

Keyword : fluoro-chloro aniline, ; benzimidazole, aromatic aldehyde;, aniline
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