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A series of copper(II) and cobalt(II) coordination compounds with 2-substituted benzimidazole derived monodentate and bidentate ligands have been prepared and characterized by microanalysis, IR and UV-Vis spectroscopy. Synthesized metal complexes have been screened for their in vitro antioxidant and antitumor activity. The complex 4a showed significant nitric oxide free radical scavenging activity (IC 50 65µg/ml), while 3i and 3g showed potent superoxide dismutase activity with IC 50 of 0.26 and 0.28 µM respectively. In vitro cytotoxicity study with human breast MCF-7 and CNS SF 268 cancer cell lines showed that the most active 2-benzyl-1H-benzimidazole Cu(II) complex 3a inhibited the growth of cancer cells at 20 µM concentration.

Substituted aryl-N-chalconyl aminophenols 1a-f were synthesized by base catalysed condensation of equimolar mixture of N-(4-hydroxyphenyl)-acetamide and appropriate araldehydes. Treatment of compounds 1a-f with hydroxylamine hydrochloride in ethanol afforded a series of novel 4-(5′-substituted-aryl-4′,5′-dihydroisoxazole-3′-yl-amino) phenols have been synthesized by treating substituted aryl-N-chalconyl aminophenol with hydroxylamine hydrochloride. Structures of newly synthesized compounds 2a-f were confirmed by IR, 1 H-NMR and elemental analysis data. The synthesized compounds were investigated for their analgesic and antimicrobial activities. Compounds 2e and 2f exhibited significant analgesic activity in comparison to the reference drug paracetamol. In in vitro anti-microbial screening, compounds 2c and 2f showed higher antibacterial and antifungal activity in comparison to the reference standard ciprofloxacin and clotrimazole, respectively. Compound 2f bearing 4-Cl phenyl substitution at 5 position of Ioxazoline ring was found to be the most potent compound of the series.

Bacterial resistance is one of the biggest threat to health community, especially hospital acquired MRSA. There are various mechanisms are involved in bacterial resistance out of which, the penetration of cell wall and the mutation of target receptor are the most important. From the beginning, the later stage of Peptidoglycan synthesis has been targeted which occurs outside the cytoplasm. The early stage of peptidoglycan synthesis has never been exploited. Inside the cytoplasm a group of enzyme known as Mur enzymes having similar mechanism of action using ATP, act consecutively and the active residues for all the enzymes are conserved. These make them ideal for multi-target. The MurD involve in adding the D-glu amino acid whereas MurE involve for L-Lys/m-DAP amino acid addition. The MurE act as a gatekeeper for gram-positive and gram-negative bacteria. The product of the previous enzyme act as a substrate for the next one. By designing similar chemical nature to the MurD product, will be having the dual affinity. But the major drawback of these inhibitors are penetration. The IC 50 values and the MIC values have not correlated for most of the inhibitors. The current work is focused on this problem and we have designed some novel scaffold using various drug designing tools to get the desired hits. The MIC values and time kill studies of the synthesized compound has been carried out against MRSA (ATCC-43300). All the MICs were within µg/ml and better time-kill studies shown against the standard drug ciprofloxacin. These hits can optimized further to get the desired lead.

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