Al-Shareef Hossa F, Elhady Heba A, Aboellil Amany H, Hussein Essam M
Department of Chemistry, Faculty of Applied Sciences, Umm Al-Qura University, Makkah, Saudi Arabia.
Department of Chemistry, Faculty of Applied Sciences, Umm Al-Qura University, Makkah, Saudi Arabia ; Department of Chemistry, Faculty of Science (Girl's), Al-Azhar University, Cairo, Egypt.
Springerplus. 2016 Jun 24;5(1):887. doi: 10.1186/s40064-016-2458-0. eCollection 2016.
Indolinone and spiro-indoline derivatives have been employed in the preparation of different important therapeutic compounds required for treatment of anticonvulsants, antibacterial, Antitubercular, and anticancer activities. Schiff bases have been found to possess various pharmacological activities such as antitubercular, plant growth inhibiting, insecticsidal, central nerve system depressant, antibacterial, anticancer, anti-inflammatory, and antimicrobial. Mannich bases have a variety of biological activities such as antibacterial and antifungal activities.
In this study, a green, rapid and efficient protocol for the synthesis of a new series of Schiff bases from spiro[indoline-3,4'-pyran]-3'-carbonitrile derivatives using ammonium chloride as a very inexpensive and readily available reagent. The prepared compounds were assessed in vitro for their antimicrobial activity. Also, the cytotoxic activity of the prepared compounds was assessed in vitro against human cells line MCF7 breast cancer.
Good activity was distinguished for Schiff bases from spiro[indoline-3,4'-pyran]-3'-carbonitriles, with some members recorded higher antimicrobial and anti-breast cancer activities.Graphical abstractNovel Schiff bases from spiro[indoline-3,4'-pyran]-3'-carbonitriles.
吲哚啉酮和螺吲哚啉衍生物已被用于制备治疗抗惊厥、抗菌、抗结核和抗癌活性所需的不同重要治疗化合物。已发现席夫碱具有多种药理活性,如抗结核、抑制植物生长、杀虫、中枢神经系统抑制、抗菌、抗癌、抗炎和抗菌活性。曼尼希碱具有多种生物活性,如抗菌和抗真菌活性。
在本研究中,使用氯化铵作为一种非常廉价且易于获得的试剂,开发了一种绿色、快速且高效的方法,用于从螺[吲哚啉-3,4'-吡喃]-3'-腈衍生物合成一系列新的席夫碱。对所制备的化合物进行了体外抗菌活性评估。此外,还对所制备的化合物针对人MCF7乳腺癌细胞系进行了体外细胞毒性活性评估。
螺[吲哚啉-3,4'-吡喃]-3'-腈类席夫碱表现出良好的活性,一些成员具有更高的抗菌和抗乳腺癌活性。
图形摘要
来自螺[吲哚啉-3,4'-吡喃]-3'-腈的新型席夫碱。