Dr. APJ Kalam Research Lab, Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Kancheepuram, Tamil Nadu, 603 203, India.
Department of Pharmacy Practice, SRM College of Pharmacy, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur - 603 203, Kancheepuram, Tamil Nadu, India.
Future Med Chem. 2022 Jun;14(12):851-866. doi: 10.4155/fmc-2022-0052. Epub 2022 May 12.
The authors aimed to estimate the therapeutic potential of novel chalcones against tuberculosis. 11 synthesized compounds were tested for antimycobacterial activity against (H37RV; American Type Culture Collection number: 27294) using the microplate alamarBlue assay. Molecular docking and pharmacokinetic parameter analyses were then performed. The most potent compounds, (2E)-1-(4-bromophenyl) (2E)-1-(2-nitrophenyl) prop-2-en-1-one, -3-(2-nitrophenyl) prop-2-en-1-one (4-bromophenyl) (2E)-1-(3-phenoxyphenyl)prop-2-en-1-one, 3-(phenoxyphenyl)prop-2-en-1-one (4-bromophenyl) prop-2-en-1-one and (2E)-1-(4-bromophenyl)-3-(5-chloro-2-hydroxyphenyl)-prop-2-en-1-one, showed activity, with a minimum inhibitory concentration (MIC) of 6.25 μg/ml. Compounds LSD2, LSD12, LSD13 and LSD15 showed strong antimycobacterial activity at a concentration of 6.25 μg/ml.
作者旨在评估新型查耳酮类化合物在结核病治疗方面的潜力。 合成了 11 种化合物，并用微孔板 alamarBlue 法对其抗分枝杆菌活性（H37RV；美国典型培养物保藏中心编号：27294）进行了测试。然后进行了分子对接和药代动力学参数分析。 最有效的化合物是（2E）-1-（4-溴苯基）-（2E）-1-（2-硝基苯基）-1-丙烯酮、-3-（2-硝基苯基）-1-丙烯酮（4-溴苯基）-（2E）-1-（3-苯氧基苯基）-1-丙烯酮、3-（苯氧基苯基）-1-丙烯酮（4-溴苯基）-1-丙烯酮和（2E）-1-（4-溴苯基）-3-（5-氯-2-羟基苯基）-1-丙烯酮，其最低抑菌浓度（MIC）为 6.25 μg/ml。 LSD2、LSD12、LSD13 和 LSD15 这 4 种化合物在 6.25 μg/ml 的浓度下显示出很强的抗分枝杆菌活性。
