Abstract

S. RaghunadhAcharyulu^1,2, N. Srinivasu^1*, Sivaranjani Jampala²and Arundhuthi M²

DOI : http://dx.doi.org/10.13005/ojc/400506

Synthesis of “5-(2,5-difluoro-4-((4-methylpiperazin-1-yl) methyl) phenyl)-N-(2-methoxybenzyl)-2-ethyl nicotinamide and 2-fluoro-4-(6-fluoro pyridine-2-yl)-6-(4-methyl piperazine-1-yl)” benzaldehyde derivatives has been developed using the 4−bromo−2,5 –difluoro benzaldehyde and 4−bromo−2,6−diflouro benzaldehyde and further this chemical to prepare the various novel derivatives. Synthesized compounds have been characterized using FTIR, ¹H-NMR, ¹³CNMR  etc. Such developed molecules are novel, cost-effective, and can be prepared by industrially viable methods. As a result of the fewer reaction steps, the high yield, and the purity of the organic chemical generated, the procedure described is less strenuous. Compared to earlier synthetic approaches, the newly discovered route is thought to be the most efficient and shortest. The established method may make it easier to prepare a variety of important intermediates and active medicinal compounds. The versatility of this work is the same reagent Titanium isopropoxide was used for both reductive aminations and SNAr couplings.The primary goal of this endeavor is to create novel compounds based on Fab I inhibitor analogs and assess their antibacterial efficacy.The produced substances were examined on “gram-positive bacteria (S.aureus, B.subtilis)and also on gram-negative bacteria (E. coli, P.aeruginosa).” Among all the compounds examined, the nicotinamide derivative 9B showed the MIC 32 (g/ml) against staphylococcus aureus and also on B.subtilis. The derivatives 9C and 9D also haveanti-bacterial resistance at 64 (g/ml) on gram-positive bacteria.  The aldehyde derivatives 13C and 13D had bacterial resistance at MIC 32 (g/ml) against staphylococcus aureus and also on B.subtilis. The docking studies of the synthesized molecules were also examined on the 7ap6 enzyme. The synthesized molecules are very well fit into the enzyme and they have better binding energy than the standard molecules triclosan and MUTO56399.

Fab inhibitors; Nicotanamide; Piperazine; Staphylococcus aureus; Triclosan

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