Synthesis and characterization of novel benzothiazole amide derivatives and screening as possible antimitotic and antimicrobial agents
Synthesis and characterization of novel benzothiazole amide derivatives and screening as possible antimitotic and antimicrobial agents
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DOI：
10.1007/s11164-016-2627-3
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发表时间：
2017-01-01
影响因子：
3.3
通讯作者：
Kumar, S. Mahadeva
中科院分区：
文献类型：
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作者：
Bhat, Mahesh;Belagali, S. L.;Kumar, S. Mahadeva
合成了一系列新的苯并噻唑酰胺类化合物(9a-L)，并用傅立叶变换红外光谱(FT-IR)、质谱学、核磁共振氢谱和碳谱对其结构进行了表征。用大蒜比色法测定了新合成化合物的抗核分裂活性，计算了有丝分裂指数值。其中，9G(14.0%)和9L(14.5%)的有丝分裂指数与标准药物(14.4%)相近，而其余化合物的有丝分裂指数较低；因此，这些化合物抑制正常的细胞分裂过程，是最有前途的抗有丝分裂药物。根据构效关系，含吸电子基团的化合物具有最大的抑制百分率，显示出增强的抗有丝分裂活性，而含给电子基的化合物如呋喃(9G)和甲基(9L)与标准化合物相当。新合成的化合物也进行了抗菌活性筛选，其中一些化合物显示出显著的活性。
A new series of benzothiazole amide derivatives (9a-l) were synthesized and characterized by Fourier-transform infrared (FT-IR), mass, and H-1 and C-13 nuclear magnetic resonance (NMR) spectroscopic techniques. The antimitotic activity of the newly synthesized compounds was determined by the Allium assay method, from which mitotic index values were calculated. Here, 9g (14.0 %) and 9l (14.5 %) showed mitotic index values most comparable to that of standard drug (14.4 %), while the remaining compounds showed lower mitotic index values; hence, these compounds inhibit the regular cell division process and are the most promising antimitotic agents. Based on the structural activity relationship, the maximum percentage inhibition was observed for compounds containing electron-withdrawing group, revealing enhanced antimitotic activity, while compounds with electron-donating groups such as furan (9g) and methyl (9l) were comparable to standard. The newly synthesized compounds were also screened for antimicrobial activity, with some of them showing remarkable activity.[GRAPHICS].