Al-Qawasmeh, Raed A. published the artcileDesign, synthesis and antibacterial activity studies of new thiadiazoloquinolone compounds, Recommanded Product: Ethyl 3-(dimethylamino)acrylate, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2014), 29(6), 777-785, database is CAplus and MEDLINE.
New 9-(alkyl/aryl)-4-fluoro-6-oxo-[1,2,5]thiadiazolo[3,4-h]quinoline-5-carboxylic acids I [R = Et, C6H5, 4-FC6H4, 4-MeOC6H4; R1 = H] and their esters I [R1 = Me, Et] were designed and synthesized. A detailed discussion of the reactions utilized in the preparation of the intermediates and target compounds was reported. All the intermediates and the final acids and esters were tested against bacterial and fungal strains. Among the tested compounds, the carboxylic acid derivatives I [R = Et, 4-FC6H4; R1 = H] proved to be very active against Gram pos. and Gram neg. bacteria with MIC 0.15-3 μg/mL. The structure-activity relationship of antibacterial thiadiazoloquinolones showed that carboxylic acid derivatives I [R = Et, 4-FC6H4; R1 = H] are twice less potent than the corresponding cyclopropyl derivative I [R = cyclopropyl; R1 = H]. Therefore, the cyclopropyl moiety on N-9 of thiadiazoloquinolone seems to be the most suitable substituent.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 924-99-2. 924-99-2 belongs to esters-buliding-blocks, auxiliary class Alkenyl,Amine,Aliphatic hydrocarbon chain,Ester, name is Ethyl 3-(dimethylamino)acrylate, and the molecular formula is C7H13NO2, Recommanded Product: Ethyl 3-(dimethylamino)acrylate.
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