目前的目标是合成具有生物活性的Isatin衍生物。为此,从Isatin底物合成Isatin衍生物的六个(06)化学实体,例如3a-3c和4a-4c。
借助1H-NMR对纯化合物进行了表征,FT-IR,EIMS光谱技术。在盐水虾生物测定的帮助下,评估了合成的胺3a-3c和腙4a-4c的毒性潜力。
获得的结果表明,3c对卤虫盐藻具有良好的毒性(LD50=1.03×10-5M)。针对四种革兰氏阴性(E.大肠杆菌铜绿假单胞菌,美国伤寒,S.flexneri)和两个革兰氏阳性(B.subtilis,金黄色葡萄球菌)细菌。化合物3a对两种细菌菌株显示出显著的活性;即铜绿假单胞菌,美国伤寒,化合物3c表现出对铜绿假单胞菌的显著活性。化合物4b对伤寒沙门氏菌的活性最高,显示比标准药物更大的抑制区生长直径(GIZ)。化合物4c对铜绿假单胞菌和伤寒沙门氏菌表现出显著的活性。化合物3a-3c和4a-4c对5个菌株中的3个表现出中等至显著的抗菌活性。只有化合物3c对卤虫盐藻具有良好的毒性(LD50=1.03×10-5M)。化合物3a-3c和4a-4c对六种真菌培养物的抗真菌研究;龙氏T.longfusus,C.白色念珠菌,A.黄花,M.卡尼斯,F.solani,和C.glabrata.所有化合物对一种或多种具有抑制作用的病原体具有活性(10-90%)。化合物3a对犬分枝杆菌表现出显著的抑制作用,即90%,70%对T.longfusus,化合物4b进一步显示出对黄曲霉的显著抑制(90%),因此证明是该系列中最活跃的成员。
所有化合物都显示出更好的抗菌性,抗真菌和细胞毒活性,这可能为制备具有更高抗菌活性的增强分子提供了基础。
The current objective was to synthesize biologically active Isatin derivatives. For this purpose, six (06) chemical entities of Isatin derivatives such as 3a-3c and 4a-4c were synthesized from Isatin substrate.
The pure compounds were characterized with the help of 1H-NMR, FT-IR, EIMS spectroscopic techniques. The synthesized amines 3a-3c and hydrazones 4a-4c were evaluated for their toxicity potential with the help of brine shrimp bioassay.
The obtained results revealed that 3c exhibited promising toxicity (LD50 = 1.03 × 10-5 M) against Artemia salina. The pure chemical entities such as compounds 3a-3c and 4a-4c were evaluated against four Gram-negative (E. coli, P. aeruginosa, S. typhi, S. flexneri) and two Gram-positive (B. subtilis, S. aureus) bacteriae. The compound 3a displayed significant activity against two bacterial strains; i.e. P. aeruginosa, S. typhi, compound 3c demonstrated significant activity against P. aeruginosa. Compound 4b was the most active against S. typhi, displaying a greater diameter of the growth of inhibition zone (GIZ) than the standard drug. Compound 4c exhibited significant activity against P. aeruginosa and S. typhi. Compounds 3a-3c and 4a-4c exhibited moderate to significant antibacterial activity against three out of five strains. Only Compound 3c revealed promising toxicity (LD50 = 1.03 × 10-5 M) against Artemia salina. Antifungal studies of the compounds 3a-3c and 4a-4c against six fungal cultures; T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glabrata. All the compounds were active against one or more pathogens having inhibition (10- 90 %). Compound 3a exhibited significant inhibition i.e. 90 % against M. canis, 70 % against T. longifusus, compound 4b further displayed significant inhibition (90 %) against A. flavus and thus proved to be the most active member of the series.
All compounds showed better antibacterial, antifungal and cytotoxic activities, which may provide a ground to prepare enhanced molecules with much higher antibacterial activities.