Nain Sumitra, Mathur Garima, Anthwal Tulika, Sharma Swapnil, Paliwal Sarvesh
Department of Pharmacy, Banasthali Vidyapith, Banasthali, Rajasthan 304022 India.
Pharm Chem J. 2023;57(2):196-203. doi: 10.1007/s11094-023-02867-4. Epub 2023 May 9.
1H-indol-2,3-dione (isatin) class of biologically active compounds have analgesic, anti-microbial, anti-inflammatory, anti-tubercular, anti-proliferative properties, and is also useful for the treatment of SARS-CoV. Schiff bases containing isatin moiety are known to have broad spectrum of biological activities like anti-viral, anti-tubercular, anti-fungal, and anti-bacterial. In this work, several Schiff base derivatives have been synthesized using two methods (synthetic and microwave) by reacting isatin with -phenylenediamine. The synthesized compounds were structurally characterized and their antimicrobial activity was tested against Gram-negative and Gram-positive bacteria using the inhibition zone method. Several newly synthesized isatin derivatives were found effective as antimicrobial agents and showed good potency (compounds , , , , ). Compound displayed higher antimicrobial activity than standard drug (Amoxicillin) against at higher concentration (16 μg/mL) and against at lower concentration (1 μg/mL).
1H-吲哚-2,3-二酮（异吲哚酮）类生物活性化合物具有镇痛、抗微生物、抗炎、抗结核、抗增殖特性，还可用于治疗严重急性呼吸综合征冠状病毒（SARS-CoV）。已知含异吲哚酮部分的席夫碱具有广泛的生物活性，如抗病毒、抗结核、抗真菌和抗菌。在本研究中，通过异吲哚酮与对苯二胺反应，采用两种方法（合成法和微波法）合成了几种席夫碱衍生物。对合成的化合物进行了结构表征，并使用抑菌圈法测试了它们对革兰氏阴性菌和革兰氏阳性菌的抗菌活性。发现几种新合成的异吲哚酮衍生物作为抗菌剂有效且显示出良好的效力（化合物 、 、 、 、 ）。化合物 在较高浓度（16 μg/mL）下对 显示出比对标准药物（阿莫西林）更高的抗菌活性，在较低浓度（1 μg/mL）下对 也具有更高活性。
