新型二苯甲基哌嗪偶联硝基苯磺酰胺杂化物的合成与生物学评价
Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids.
作者信息
Murthy Vallabhaneni S, Tamboli Yasinalli, Krishna Vagolu Siva, Sriram Dharmarajan, Zhang Fang Xiong, Zamponi Gerald W, Vijayakumar Vijayaparthasarathi
机构信息
Centre for Organic and Medicinal Chemistry, Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, Tamil Nadu 632014, India.
Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science Pilani, Hyderabad Campus, Hyderabad, Telangana 500078, India.
出版信息
ACS Omega. 2021 Mar 31;6(14):9731-9740. doi: 10.1021/acsomega.1c00369. eCollection 2021 Apr 13.
A series of novel benzhydryl piperazine-coupled nitrobenzenesulfonamide hybrids were synthesized with good to excellent yields. They were tested for inhibition of mycobacterial activity against the H37Rv strain, cytotoxicity MTT (RAW 264.7cells) assay, nutrient starvation (H37Rv strain), and ability to block Cav3.2 T-type calcium channels. Novel hybrids did not inhibit T-type calcium channels, whereas they showed excellent antituberculosis (TB) activity and low cytotoxicity with a selectivity index of >30. A direct impact of the amino acid linker was not observed. Studied hybrids exhibited good inhibition activities, and the 2,4-dinitrobenzenesulfonamide group emerged as a promising scaffold for further drug design by hybridization approaches for anti-TB therapy.
合成了一系列新型的二苯甲基哌嗪偶联硝基苯磺酰胺杂化物，产率良好至优异。对它们进行了测试，以评估其对结核分枝杆菌H37Rv菌株的抑制活性、细胞毒性MTT（RAW 264.7细胞）测定、营养饥饿（H37Rv菌株）以及阻断Cav3.2 T型钙通道的能力。新型杂化物不抑制T型钙通道，然而它们显示出优异的抗结核（TB）活性和低细胞毒性，选择性指数>30。未观察到氨基酸连接体的直接影响。所研究的杂化物表现出良好的抑制活性，并且2,4-二硝基苯磺酰胺基团成为通过杂交方法进行抗结核治疗的进一步药物设计的有前景的骨架。
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