Reddy Cherkupally Sanjeeva, Dasari Chandrashekar Rand, Yakub Vookanti, Nagaraj Adki
Acta Chim Slov. 2010 Dec;57(4):798-807.
A new series of bis(pyrazolo[3,4-d][1,3]thiazoles) 7a-j has been synthesized and characterized via IR, 1H NMR, 13C NMR, MS and elemental analyses. All the newly synthesized compounds 7a-j have been assayed for their nematicidal activity against Ditylenchus myceliophagus and Caenorhabditis elegans by aqueous in vitro screening technique. The screened data reveal that the compound 7e is most effective against D. myceliophagus and C. elegans with LD50 of 160 and 180 ppm respectively and is almost equal to the activity of the standard levamisole. The compounds 7h and 7j are also most active against C. elegans with LD50 of 190 ppm and D. myceliophagus with LD50 of 180 ppm, respectively. Further, 7a-j were screened for their antibacterial activity. Most of these new compounds showed potent activity against the test bacteria and emerged as potential molecules for further development.
通过红外光谱、1H核磁共振、13C核磁共振、质谱和元素分析，合成并表征了一系列新的双（吡唑并[3,4-d][1,3]噻唑）7a-j。采用水相体外筛选技术，对所有新合成的化合物7a-j进行了杀线虫活性测试，以检测其对食菌茎线虫和秀丽隐杆线虫的活性。筛选数据表明，化合物7e对食菌茎线虫和秀丽隐杆线虫最有效，其半数致死剂量（LD50）分别为160 ppm和180 ppm，几乎与标准左旋咪唑的活性相当。化合物7h和7j对秀丽隐杆线虫也具有最强活性，LD50为190 ppm，对食菌茎线虫的LD50为180 ppm。此外，还对7a-j进行了抗菌活性筛选。这些新化合物中的大多数对测试细菌显示出强效活性，并成为进一步开发的潜在分子。
