Faculty Publications

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    Synthesis, and antitubercular and antimicrobial activity of 1?-(4-chlorophenyl)pyrazole containing 3,5-disubstituted pyrazoline derivatives
    (Royal Society of Chemistry, 2016) Harikrishna, N.; Isloor, A.M.; Kulal, K.; AlObaid, A.; Fun, H.-K.
    A new series of 1?-(4-chlorophenyl)-5-(substituted aryl)-3?-(substituted aryl)-3,4-dihydro-2H,1?H-[3,4?]bipyrazolyl derivatives (6a-e, 8a-e, 10a-e) have been synthesized, characterized and screened for antimicrobial and antitubercular activity. Among the synthesized compounds, the minimum inhibition concentration of 10e was found to be as low as 1.56 ?g ml-1 and that of 10c was 6.25 ?g ml-1 as compared to the standard anti-tb drugs pyrazinamide and streptomycin. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2016.
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    Antitubercular and antimicrobial activity of nh4vo3 promoted 1,4-dihydropyridine incorporated 1,3,4-Trisubstituted pyrazole
    (Bentham Science Publishers B.V. P.O. Box 294 Bussum 1400 AG, 2017) Harikrishna, N.; Isloor, A.M.; Kulal, K.; Parish, T.; Jamalis, J.; Ghabbour, H.A.; Fun, H.-K.
    Background: A new series of pyrazole containing 1,4-dihydropyridine derivatives 5a-i and 6a-i were synthesized from substituted acetylated aryls and substituted phenylhydrazine by the multistep reaction. Method: The target compounds 1,4-dihydropyridine derivatives were obtained from green synthesis of 1,3-disubstituted phenyl-1H-pyrazole-4-carbaldehydes 4a-i with ethyl acetoacetate and methyl acetoacetate at higher temperatures in the presence of ammonium acetate and the catalytic amount of ammonium metavanadate (NH4VO3). The role of ammonium metavanadate was increases rate of the reaction and obtained high yields. Result: Structures of newly synthesized 1,4-dihydropyridine moiety containing pyrazole derivatives were confirmed by FT-IR, NMR and Mass spectral studies. The structure of compound 5b was confirmed by S-XRD study. Further, these compounds were tested for in-vitro antitubercular and antimicrobial studies. Compounds 5a, 5b, 5i, 6a, 6b, 6g, 6h, and 6i were found to be active against all the bacterial microorganisms. Conclusion: The above mentioned compounds have shown lowest MIC ranging between 3.12-12.5 ?g/ml against Mycobacterium tuberculosis and MIC values ranging between 7.8- 15.6 ?g/ml for Mycobacterium smegmatis, Staphylococcus aureus and Pseudomonas aeruginosa. For the control of life threatening diseases such as tuberculosis, these eight compounds may be strongly promising synthetic compounds. © 2017 Bentham Science Publishers.
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    Structural modification of zolpidem led to potent antimicrobial activity in imidazo[1,2-: A] pyridine/pyrimidine-1,2,3-triazoles
    (Royal Society of Chemistry, 2019) Reddyrajula, R.; Udayakumar, U.
    Ambien (zolpidem), an imidazo[1,2-a]pyridine derivative, is a commercial drug to treat insomnia which also possesses antitubercular activity against Mycobacterium tuberculosis H37Rv. In this paper, we describe the synthesis of three diverse lead series of imidazo[1,2-a]pyridine/pyrimidine-1,2,3-triazoles (IPTs) which are designed by specific structural modifications of zolpidem. Most of the IPTs exhibited remarkable in vitro antitubercular activity with an MIC of 1.56 ?g mL-1, which is two-fold higher than the MIC of zolpidem. Further, the synthesized IPTs displayed moderate inhibitory activity against several bacterial and fungal strains as well, and also showed an acceptable safety profile as verified through in vitro cytotoxicity assessment against Vero cells. In addition, the potent IPTs exhibited promising binding interactions within the active site of the InhA enzyme. An interesting correlation between the in vitro inhibitory activity and the binding mode was observed: most of the potent molecules (MIC = 1.56 ?g mL-1) interact through a H-bond with the Tyr 158 residue of the target enzyme. These efforts toward the structural modification of zolpidem could be helpful for further optimization of the IPT core to develop new anti-TB drugs. This journal is © 2019 The Royal Society of Chemistry and the Centre National de la Recherche Scientifique.