02005nas a2200253   4500008004100000022001400041245007700055210006900132260000900201300001400210490000700224520117700231100002201408700002701430700002701457700002201484700002201506700002401528700002401552700002101576700002601597700002001623856010801643       2020                        eng d  a1144-054600aSynthesis and biological activity of imidazole based 1,4-naphthoquinones0 aSynthesis and biological activity of imidazole based 14naphthoqu  cMAY   a6889-69010 v443 a<p>Design and development of drugs in multi-drug resistant (MDR) infections have been of growing interest. We report the syntheses, and antibacterial and antifungal activities of imidazole-based 1,4-naphthoquinones (I-1 to I-4; 1-alkyl-2-methyl-1H-naphtho[2,3-d]imidazole-4,9-dione (alkyl = methyl to butyl)) and their precursors (B-3; N-(3-chloro-1,-dioxo-1,4-dihydronaphthalen-2-yl)acetamide) and A-1 to A-4; N-(3-(alkylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide (alkyl = methyl to butyl). Crystal structures of B-3, A-1 to A-3 and I-2 to I-4 were obtained through single crystal X-ray diffraction experiments. Electronic structure and charge distribution have further been characterized with the use of Density Functional Theory. Seven of these derivatives display a broad spectrum of antibacterial activity against few selected bacterial strains (Gram-positive and Gram-negative). As demonstrated MIC values with B-2 and B-3 against bacterial isolates were 8-64 mu g ml(-1) and those against pathogenic yeast, C. albicans, were observed in the range of 128-256 mu g ml(-1). MIC data of these derivatives suggest them to be promising against pathogens.</p>
1 aChoudhari, Dinkar1 aSalunke-Gawali, Sunita1 aChakravarty, Debamitra1 aShaikh, Samir, R.1 aLande, Dipali, N.1 aGejji, Shridhar, P.1 aRao, Pradeep, Kumar1 aSatpute, Surekha1 aPuranik, Vedavati, G.1 aGonnade, Rajesh  uhttps://library.ncl.res.in/content/synthesis-and-biological-activity-imidazole-based-14-naphthoquinones