新型三氮基喹啉类药物的药理研究

IF 0.4 Q4 PHARMACOLOGY & PHARMACY Advances in Pharmacology and Pharmacy Pub Date : 2021-10-01 DOI:10.13189/app.2021.090401
N. R., G. Priyadarshini, S. G.
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引用次数: 2

摘要

氮杂环的药理重要性是数不胜数的。三嗪类化合物被发现具有特殊的生物抗肿瘤、抗hiv、抗病毒、抗疟疾、抗菌和细胞毒活性。本研究旨在评价新合成的取代的4'-甲基-3-硫氧基-1,2,4-三嗪喹啉-5- 1的体外抗菌、抗真菌、抗氧化潜力和细胞毒性。用琼脂孔扩散法测定其抑菌活性,用肉汤稀释法测定其MIC。化合物对革兰氏阳性金黄色葡萄球菌、化脓性葡萄球菌和革兰氏阴性细菌aeroginosa、E. coli、肺炎克雷伯菌、Pseudomonas Sp等具有良好的抑菌活性,抑菌范围为9 ~ 19nm。标准药物氨苄西林的最大抑制带为18 nm。在所筛选的化合物中,样品表现出良好的活性。同样,对化合物进行抗真菌特性筛选,结果表明,所选白色念珠菌菌株的生长具有良好的抑制作用。对化合物进行了DPPH(1,1-二苯基-2-苦味酰肼)活性筛选。对来自Amala癌症研究中心的道尔顿淋巴瘤腹水(DLA)细胞进行细胞毒性试验。所测化合物表现出显著的抗氧化活性,并呈浓度依赖性。
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Pharmacological Studies on Novel Triazino Quinolines
Pharmacological importance of the nitrogen heterocycles is countless. The triazines are found to possess exceptional biological antitumor, anti-HIV, antiviral, antimalarial, antimicrobial, cytotoxic activities. The current investigation attempts to evaluate invitro antibacterial, antifungal, antioxidant potential, and cytotoxicity of newly synthesized substituted 4'-methyl-3-thioxo-1,2,4-triazinoquinolin-5-one. The antimicrobial activity was done by Agar Well Diffusion Method and the MIC of the compound was found using the Broth dilution assay method. The compounds showed excellent antibacterial activity against selected bacterial strains, including Gram-positive S. aureus, S. pyogens , and Gram-negative bacteria P. aeroginosa, E. coli, K. peumoniae, Pseudomonas Sp with the zones of inhibition 9 to 19nm. The standard drug Ampicillin showed a maximum inhibitory zone 18 nm. Among all the screened compounds, sample exhibited good activity. Similarly, the compounds were screened for antifungal properties, which showed an excellent reduction in the growth of selected fungal strain for Candida albicans. The compounds were also screened for 1,1-diphenyl-2-picrylhydrazyl (DPPH) activity. Cytotoxicity was done in Dalton’s Lymphoma Ascites (DLA) cells which were obtained from Amala Cancer Research Center. The tested compounds exhibited significant antioxidant activity in a concentration-dependent manner.
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来源期刊
Advances in Pharmacology and Pharmacy
Advances in Pharmacology and Pharmacy PHARMACOLOGY & PHARMACY-
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