Herein we report the synthesis and biological evaluation of a new series of thiazolidin-4-one derivatives. The C4 and C5 functionalized, 5-arylidene/alkylidene, 5-bromo, 5-pyridinium, and 4-arylimino analogs of thiazolidine-4-one were prepared efficiently using appropriate synthetic routes and characterized by IR, NMR and Mass spectrometry. Results of antimicrobial evaluation showed that compounds 4 and 8 had significant antibacterial activity comparable to that of the reference drug gentamicin. Compound 5a showed promising antifungal activity compared to amphotericin B as a reference drug. The antitumor activity revealed that compound 4 was the most active analog among the tested series with IC50 values of 28.4 and 12.6 µg/mL against both HCT-116 and HepG-2 cell lines, respectively, compared to standard drug doxorubicin. Results from the biological evaluation, in-silico molecular docking studies, and ADMET analyses confirmed that thiazolidin-4-one is a promising scaffold that can be used to design potential lead compounds for the antibacterial and antitumor agents.
This work highlighted the proficient and naturally safe methodology for the phenol synthesis using biocatalyst lipase. The development of sustainable synthetic protocol for various organic transformations is an important area of research attracts researchers to avoid use of volatile and hazardous organic solvents in reaction for greener and eco-friendly protocols. Lipase is subclass of esterase enzymes and acts as biocatalyst with industrial significance. They carry out biochemical transformation in non-aqueous and aqueous phases quickly. To further make the process more specific Design Expert software was used for the optimization of synthesize phenol for maximum % Yield and % Purity. Effect of temperature, Concentration of Catalyst, and Volume of Water was selected as an independent factor to get the maximum % Yield and % Purity of the phenol. The results confirmed the mathematical model robustness and justify experimental design. Therefore, the current protocol for synthesis of phenols from phenylboronic acid is greenest and environmentally benign alternative. The current convention has many benefits, like phenomenal product yields, reduced time of reaction, simple procedure to work up, and extensive substrate scope, cost-effective and also lipase was recuperated and reused multiple times without significant loss of its catalytic activity.
The N-methyl pyridinium tosylate (NMPyTs) ionic liquid is used as an efficient, homogeneous, and recyclable catalyst for the synthesis of tetrahydropyridine derivatives via one-pot multi-component condensation of aromatic aldehyde, anilines, and β-ketoesters under ultrasonic irradiations. This protocol was successfully pertinent to a wide range of structurally diverse aromatic aldehydes, substituted anilines, and β-ketoesters. The major characteristics of this technique include operational simplicity, short reaction times, mild reaction conditions, and high yield. Importantly, NMPyTs can undergo up to three recycle runs without any noticeable loss of catalytic activity.
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：