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Synthesis of new 3-phenylquinazolin-4(3H)-one derivatives as potent antibacterial agents effective against methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA)
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-08-11 , DOI: 10.1016/j.bioorg.2018.08.012
Srikanth Gatadi , Jitendra Gour , Grace Kaul , Manjulika Shukla , Arunava Dasgupta , Ravikumar Akunuri , Richa Tripathi , Y.V. Madhavi , Sidharth Chopra , Srinivas Nanduri

Occurrence of infections due to the drug resistant Staphylococcus aureus is on rise necessitating the need for rapid development of new antibacterial agents. In our present work, a series of new 3-phenylquinazolin-4(3H)-one derivatives were designed, synthesized and evaluated for their antibacterial activity against ESKAP (E. coli, S. aureus, K. pneumoniae, A. baumannii, P. aeroginosa) pathogen panel and pathogenic mycobacterial strains. The study revealed that compounds 4a, 4c, 4e, 4f, 4g, 4i, 4o and 4p exhibited selective and potent inhibitory activity against Staphylococcus aureus with MIC values in the range of 0.125–8 µg/mL. Further, the compounds 4c, 4e and 4g were found to be non toxic to Vero cells (CC50 = >10–>100 µg/mL) and exhibited favourable selectivity index (SI = 40–>200). The compounds 4c, 4e and 4g also showed potent inhibitory activity against various MDR-S. aureus including VRSA. The promising results obtained indicated the potential use of the above series of compounds as promising antibacterial agents for the treatment of multidrug resistant Staphylococcus aureus infections.



中文翻译:

合成新型3-苯基喹唑啉-4(3 H)-one衍生物作为有效的抗甲氧西林和耐万古霉素的金黄色葡萄球菌(MRSA和VRSA)的有效抗菌剂

由于耐药性金黄色葡萄球菌引起的感染正在增加,因此需要快速开发新的抗菌剂。在我们目前的工作中,设计,合成并评估了一系列新的3-苯基喹唑啉-4(3 H)-one衍生物对ESKAP的抗菌活性(大肠杆菌,金黄色葡萄球菌,肺炎克雷伯菌,鲍曼不动杆菌, P. aeroginosa)病原体和致病性分枝杆菌菌株。研究表明,化合物4a4c4e4f4g4i4o4p金黄色葡萄球菌具有选择性和有效的抑制活性,MIC值为0.125–8  µg / mL。此外,发现化合物4c4e4g对Vero细胞无毒(CC 50 => 10–> 100  µg / mL),并显示出良好的选择性指数(SI = 40–> 200)。化合物4c4e4g还显示出对各种MDR-金黄色葡萄球菌的有效抑制活性包括VRSA。获得的有希望的结果表明上述系列化合物作为潜在的抗菌剂在治疗多​​药耐药金黄色葡萄球菌感染中的潜在用途。

更新日期:2018-08-11
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