Polycyclic Aromatic Compounds ( IF 2.4 ) Pub Date : 2021-09-01 , DOI: 10.1080/10406638.2021.1970586 Amit B. Patel 1 , Jignesh V. Rohit 2
Abstract
Novel series of 1,3,4-thiadiazole and piperazine substituted quinazoline derivatives have been designed, synthesized, and tested in vitro for antimycobacterial activity. The synthetic procedure involved Suzuki C-C cross-coupling on a quinazoline ring and subsequently by the formation of 1,3,4-thiadiazole based piperazines. Many synthesized analogs were observed active against Mycobacterium H37Rv strain in preliminary analysis using the BACTEC MGIT method. A secondary antimycobacterial assay using the Lowenstein-Jensen MIC method indicates that bromo (7c), trifluoromethyl (7f), and hydroxy (7 h) groups substituted analogs have shown strong efficacy in the range of 3.12–6.25 µg/mL. Active compounds were also tested for their cytotoxic activity against Human cervical (HeLa) cells at their MICs. The synthesized analogs were analyzed by IR, 1H NMR, 13 C NMR, MS, and elemental analysis for their structure determination.
中文翻译:
作为动态抗分枝杆菌剂的 1,3,4-噻二唑和哌嗪融合杂合喹唑啉衍生物的开发
摘要
新型系列的 1,3,4-噻二唑和哌嗪取代的喹唑啉衍生物已被设计、合成并在体外测试其抗分枝杆菌活性。合成过程包括铃木 CC 在喹唑啉环上交叉偶联,随后形成 1,3,4-噻二唑基哌嗪。在使用 BACTEC MGIT 方法的初步分析中,观察到许多合成的类似物对分枝杆菌H37Rv 菌株具有活性。使用 Lowenstein-Jensen MIC 方法的二级抗分枝杆菌测定表明溴 ( 7c )、三氟甲基 ( 7f ) 和羟基 ( 7h) 组取代的类似物在 3.12–6.25 µg/mL 范围内显示出强大的功效。还测试了活性化合物在其 MIC 处对人宫颈 (HeLa) 细胞的细胞毒活性。通过 IR、1H NMR、13 C NMR、MS 和元素分析对合成的类似物进行结构测定。