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In the present work, a series of novel oxazolidinone derivatives containing thieno-pyridine ring system ( 11a–n ) were synthesized in six steps. Synthesis of amino oxazolidinone scaffold ( 10 ) involved nucleophilic substitution of thienopyridine ( 4 ) with P-chloro-nitrobenzene ( 3 ) in dimethyl formamide at 65 °C give nitro compound ( 5 ) which was further reduced in catalytic hydrogenation condition using Raney-Nickel in isopropyl alcohol afforded amine ( 6 ). Reaction of compound ( 6 ) with 2-[(2S)-oxiran-2-ylmethyl]-1H-isoindole-1,3(2H)-dione ( 7 ) at mild reflux condition in isopropyl alcohol gives compound ( 8 ). Hydroxy amine compound ( 8 ) further undergo carbonyl insertion reaction with 1, 1’-carbonylbis(1H-imidazole) afforded oxazolidinone compound ( 9 ). The de-protection of phthalamide group of compound ( 9 ) carried by treating with aqueous solution of hydrazine hydrate in methanol at room temperature give compound ( 10 ). Finally, compound ( 10 ) reacts with acetyl chloride, carboxylic acid, sulfonyl chloride and chloro format by customary method provided amides, sulfonamide and carbamate derivative of (5S)-5-(aminomethyl)-3-[4-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)phenyl]-1,3-oxazolidin-2-one. The developed synthetic approach was operationally simple and high yielding. The structures of the synthesized compounds were elucidated by IR, MS,  1 H and  13 C-NMR. Synthesized compounds ( 11a–n ) were tested for antibacterial activity against a panel of Gram-positive bacteria comprising  Staphylococcus aureus (ATCC5638) ,  Streptococcus pyogenes (ATCC12344) ,  Bacillus subtilis (ATCC6051) ,  Bacillus pumilus (ATCC27142) , and  Enterococcus faecalis (NCIM5253) . The investigation of antimicrobial screening data revealed that, most of the compounds tested have demonstrated sensible to good bacterial activity. In summary, preliminary results of activity indicate that, acetyl derivative ( 11a ), methane sulfonamide derivative ( 11c ) and  p -toluene sulfonamide derivative ( 11e ) found to be good activity and di-(methane sulfonamide) derivative ( 11d)  showed comparable activity to reference drug substances.

polycyclic aromatic compounds

Synthesis and Evaluation of Novel (5S)-5-(Aminomethyl)-3-[4-(6,7-Dihydrothieno[3,2- c ]Pyridin-5(4 H )-yl)Phenyl]-1,3-Oxazolidin-2-One Derivatives as Potent Antimicrobial Agents