SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL IMIDAZOLE BASED COMPOUNDS

Abstract

Objective: Some new imidazole derivatives (3i-xii) were synthesized as per design synthetic protocol scheme. The structures of newly prepared compounds were confirmed by modern analytical technique and elemental analysis.

Methods: All the synthetic compounds were screened for their antimicrobial activity against bacterial results showed good to remarkable activity. The MIC (minimum inhibitory concentration) values were determined by comparison to ciprofloxacin (anti-bacterial) and fluconazole (anti-fungal) as standard drug. Among them, compound 3iv and 3x exhibited notable antimicrobial activity. These compounds may be used as new template for the searching of potential antimicrobial agents.

Results: The purity of the compound was verified with the help of TLC (B: A, 9:1). % age of yield was found 83% and melting point noted 151-1520C. Compounds (3ii, 3viii and 3ix) were shown moderate activity against E. coli, S. aureus, M. luteus and K. pneumonia, whereas compounds (3iii, 3vii, 3xi and 3xii) showed mild activity against few bacterial strainsμg/ml.  The compounds of electron releasing imidazole derivatives (3ii, 3iv, 3viii, 3ix, 3x and xi) presented comparatively better anti-fungal activity than the compounds of electron withdrawing imidazole derivatives (3iii, 3vii and 3xii).

Conclusion: The biological activity result revealed that all the newly synthetic compounds 3i-xii [4-(biphenyl-4-yl)-2-(substituted phenyl)-1H-imidazole] exhibited better antibacterial activity as compared to antifungal activity in compare to reference drug.

     

Peer Review History:

Received 4 December 2016;   Revised 9 January 2017; Accepted 10 February, Available online 15 March 2017

Academic Editor: Dr. Asia Selman Abdullah, Al-Razi university, Department of Pharmacy, Yemen, asia_abdullah65@yahoo.com

Received file:        Reviewer's Comments:

Average Peer review marks at initial stage: 6.5/10

Average Peer review marks at publication stage: 8.5/10

Reviewer(s) detail:

Dr. Emmanuel O. Olorunsola, Department of Pharmaceutics & Pharmaceutical Technology, University of Uyo, Nigeria, olorunsolaeo@yahoo.com

Dr. Xinwei Li, Jilin University, China, lixinwei100@jlu.edu.cn