@article { ISI:000258784000005,
	title = {Antibacterial activity of synthesized 2,4,5-trisubstituted imidazole derivatives},
	journal = {Chemical Biology \& Drug Design},
	volume = {72},
	number = {3},
	year = {2008},
	month = {SEP},
	pages = {197-204},
	publisher = {WILEY-BLACKWELL},
	type = {Article},
	address = {COMMERCE PLACE, 350 MAIN ST, MALDEN 02148, MA USA},
	abstract = {<p>Some novel chemically synthesized 2,4,5-trisubstituted imidazoles from aryl aldehydes and 1,2-diketones or alpha-hydroxyketone were screened against eight different human pathogenic bacteria and fungi. Seven compounds were found to be active against different bacteria. These compounds showed variation in activity and were found to be active against Gram-positive as well as Gram-negative bacteria. Compound 4-(4,5-diphenyl-1H-imidazol-2-yl)-phenol, 3d was the only compound which showed activity against Klebsiella pneumoniae while rest of the compounds did not show significant activity against this micro-organism. Minimum inhibitory concentrations of the compounds were in the range of 0.50 to 6.1 mu g/mL and minimum bactericidal concentration ranges from 1.11 to 12.9 mu g/mL. The candidature of active compounds to be an effective and novel drug was examined based on Lipinski{\textquoteright}s rule of Five which explained ClogP, LogS, H-bond acceptors, H-Bond donors and rotational bonds. Compounds 3a-d and 3f satisfies Lipinski{\textquoteright}s rule of Five and could be proposed as potent new antibacterial drugs.</p>},
	keywords = {1, 2, 2-Diketones, 4, 5-trisubstituted imidazoles, alpha-hydroxyketone, antibacterial activity, aryl aldehydes},
	issn = {1747-0277},
	doi = {10.1111/j.1747-0285.2008.00691.x},
	author = {Khan, Mohd Sajid and Siddiqui, Shafi Ahmad and Siddiqui, Mohammad Shaik Rafi Ahmad and Goswami, Usha and Srinivasan, Kumar Venkatraman and Khan, Mohammad Islam}
}
@article { ISI:000324465000030,
	title = {Design, synthesis, evaluation and thermodynamics of 1-substituted pyridylimidazo[1,5-a]pyridine derivatives as cysteine protease inhibitors},
	journal = {Plos One},
	volume = {8},
	number = {8},
	year = {2013},
	month = {AUG},
	pages = {e69982},
	publisher = {PUBLIC LIBRARY SCIENCE},
	address = {1160 BATTERY STREET, STE 100, SAN FRANCISCO, CA 94111 USA},
	abstract = {<p>Targeting papain family cysteine proteases is one of the novel strategies in the development of chemotherapy for a number of diseases. Novel cysteine protease inhibitors derived from 1-pyridylimidazo[1,5-a]pyridine representing pharmacologically important class of compounds are being reported here for the first time. The derivatives were initially designed and screened in silico by molecular docking studies against papain to explore the possible mode of action. The molecular interaction between the compounds and cysteine protease (papain) was found to be very similar to the interactions observed with the respective epoxide inhibitor (E-64c) of papain. Subsequently, compounds were synthesized to validate their efficacy in wet lab experiments. When characterized kinetically, these compounds show their K-i and IC50 values in the range of 13.75 to 99.30 mu M and 13.40 to 96.50 mu M, respectively. The thermodynamics studies suggest their binding with papain hydrophobically and entropically driven. These inhibitors also inhibit the growth of clinically important different types of Gram positive and Gram negative bacteria having MIC50 values in the range of 0.6-1.4 mu g/ml. Based on Lipinski{\textquoteright}s rule of Five, we also propose these compounds as potent antibacterial prodrugs. The most active antibacterial compound was found to be 1-(2-pyridyl)-3-(2-hydroxyphenyl)imidazo[1,5-a]pyridine (3a).</p>},
	issn = {1932-6203},
	doi = {10.1371/journal.pone.0069982},
	author = {Khan, Mohd Sajid and Baig, Mohd Hassan and Ahmad, Saheem and Siddiqui, Shapi Ahmad and Srivastava, Ashwini Kumar and Srinivasan, Kumar Venkatraman and Ansari, Irfan A.}
}
