Thakor Priteshkumar M, Patel Jatin D, Patel Rajesh J, Chaki Sunil H, Khimani Ankurkumar J, Vaidya Yati H, Chauhan Anita P, Dholakia Amit B, Patel Vishant C, Patel Ankitkumar J, Bhavsar Nirav H, Patel Hiteshkumar V
Department of Chemistry, Shri Alpesh N. Patel Post Graduate Institute of Science and Research, Anand, Gujarat 388001, India.
Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Anand, Gujarat 388001, India.
ACS Omega. 2024 Jun 24;9(33):35431-35448. doi: 10.1021/acsomega.4c02007. eCollection 2024 Aug 20.
The current work aims to generate novel Schiff bases by reacting substituted aldehydes with amine derivatives catalyzed by a natural acid. The developed compounds underwent diverse physicochemical analyses including liquid chromatography-mass spectrometry, Fourier transform infrared spectroscopy, scanning electron microscopy, H- and C-nuclear magnetic resonance, and X-ray diffraction. Furthermore, differential thermogravimetric, thermogravimetric, and differential thermal analysis techniques were employed in a nitrogen-free environment to determine kinetic parameters. These data were then used in model-free isoconversional methods (e.g., Friedman, Kissinger-Akahira-Sunose, and Flynn-Wall-Ozawa). The Schiff bases were evaluated for their and α-amylase inhibitory activity. Schiff base-2 displayed the highest inhibition compared with the reference drug acarbose. In comprehensive MTT assay cytotoxicity investigations, both Schiff bases showed strong anticancer capabilities against the human lung cancer cell line (A549). Moreover, this study demonstrated effectiveness of synthetic compounds in screening for anti-Alzheimer's and stress resistance properties. The simplicity of its biology allowed precise evaluation of the effect of compounds on neuronal function and stress response. This research enhances drug discovery efforts for Alzheimer's and stress-related disorders, potentially improving patient outcomes.
当前的工作旨在通过天然酸催化取代醛与胺衍生物反应生成新型席夫碱。所开发的化合物进行了多种物理化学分析,包括液相色谱 - 质谱联用、傅里叶变换红外光谱、扫描电子显微镜、氢和碳核磁共振以及X射线衍射。此外,在无氮环境中采用差示热重、热重和差示热分析技术来确定动力学参数。然后将这些数据用于无模型等转化率方法(例如弗里德曼法、基辛格 - 赤平 - ose法和弗林 - 沃尔 - 小泽法)。对席夫碱的α - 淀粉酶抑制活性进行了评估。与参考药物阿卡波糖相比,席夫碱 - 2表现出最高的抑制作用。在全面的MTT法细胞毒性研究中,两种席夫碱对人肺癌细胞系(A549)均显示出强大的抗癌能力。此外,本研究证明了合成化合物在筛选抗阿尔茨海默病和抗应激特性方面的有效性。其生物学的简单性使得能够精确评估化合物对神经元功能和应激反应的影响。这项研究加强了针对阿尔茨海默病和应激相关疾病的药物研发工作,有可能改善患者的治疗效果。