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Relevant academic research and scientific papers

QSAR modeling of synthesized 3-(1,3-benzothiazol-2-yl) 2-phenyl quinazolin-4(3H)-ones as potent antibacterial agents

Present communication elicits the designing and synthesis of 3-(1,3-benzothiazol-2-yl) 2-phenyl quinazolin-4(3H)-ones as potential antibacterial agents. A number of substituted 2-amino benzothiazoles, 2-amino-5-[(E)-phenyl diazenyl] benzoic acid, and 2-phenyl-4H benzo[d] [1,3] oxazin-4-one were synthesized as the precursor substrates. The compounds were synthesized in excellent yields and the structures were corroborated on the basis of IR, 1H NMR, Mass, and elemental analysis data. These compounds were screened in vitro for their antibacterial activity against a representative panel of Gram positive and Gram negative bacteria and models were generated through quantitative structure-activity relationship (QSAR).The activity contributions due to structural and substituent effects were determined using sequential regression procedure. The antimicrobial assay data show that the synthesized compounds are found to manifest profound antimicrobial activity. Springer Science+Business Media, LLC 2011.

Rapid microwave-assisted solution phase synthesis of 6,8-disubstituted 2-phenyl-3-(substituted- benzothiazol-2-yl)-4-[3H]-quinazolinones as novel anticonvulsants

A fast and highly efficient microwave accelerated solution phase procedure for the synthesis of a series of 2-phenyl-3-(benzothiazol-2-yl)-4[3H]- quinazolinones, substituted in the benzothiazole ring, is developed. The title compounds were characterized by elemental analyses, IR, 1H NMR, and EI-MS data. The anticonvulsant activity of all the new compounds (3a-m and 4a-m) was evaluated against Maximum Electroshock (MES) induced seizures and against subcutaneous pentylenetetrazole (PTZ) induced seizures model in mice. The neurotoxicity was assessed using the Rotorod procedure. All the compounds tested were administered intraperitoneally at a various dose levels ranging from 7-200 mg/Kg body weight and the median toxic dose (TD50) and the protection index (PI) values were determined. In general compounds 3a-m were found to be more potent compared to compounds 4a-m. Among the compound tested, the compound 3e in the 2-phenyl-3-(benzothiazole-2-yl)-4[3H]-quinazolinone series and 4l in the 6,8-dibromo-2-phenyl-3-(benzothiazole-2-yl)-4[3H]-quinazolinone series were found to be the most potent. Copyright Taylor & Francis Group, LLC.