Herein, a highly efficient and environmentally benign protocol for the synthesis of biologically important pyrimido[4,5-b]quinolinone-2,4-diones from aromatic amines, barbituric acid and aryl aldehyde is reported. This process takes place at room temperature under direct irradiation from a UV₃₆₅ light source in the absence of a photocatalyst. The reported approach has several advantages such as high yield, clean reaction conditions, chromatography-free synthesis and the use of a cheap water–glycerol solvent system, which is also an environmentally friendly solvent. The applicability of this protocol for the large-scale synthesis of pyrimido[4,5-b]quinolinone-2,4-diones without wasting any expensive chemicals is an added advantage.

The potential of glutathione as a catalyst for carbon–oxygen ring cyclization was investigated experimentally as well as computationally. The glutathione molecules were immobilized on superparamagnetic iron-oxide nanoparticle so as to improve the efficiency of the catalyst and to augment magnetically aided recyclability. Ultrasound was also exploited for thorough dispersion of the nanoparticles in the aqueous medium so that contact between the catalyst and the reactants are enhanced. This nano-organocatalyst was synthesized and characterized by the following analytical techniques: TEM, scanning electron microscope, EDS, powder X-ray diffraction, vibrating sample magnetometry, FTIR, TGA, DTA. Its catalytic prowess in the synthesis of several indolyl chromenes, pyrrolyl chromenes, and indoloxanthenes were meticulously investigated. The synthetic protocol was found to be efficient, economical, and environment benign. Quantum chemical studies were performed to study the effect of the catalyst on C–O ring cyclization using Gaussian program viz. B3LYP.

The activity of sodium glucose co-transporter 2 (SGLT2) has always been an important parameter influencing chronic kidney disease in type-2 diabetic patients. Herein, we have meticulously designed, synthesized, and evaluated several novel steroidal pyrimidine molecules that possess the capability to successfully bind to the SGLT2 protein and inhibit its activity, thereby remedying kidney-related ailments in diabetic patients. The lead steroidal pyrimidine compounds were selected after virtually screening from a library of probable N-heterocyclic steroidal scaffolds. A nano-catalyzed synthetic route was also explored for the synthesis of the steroidal pyrimidine analogs demonstrating an environmentally benign protocol. Extensive in vitro investigations encompassing SGLT2 screening assays and cell viability assessments were conducted on the synthesized compounds. Among the steroidal pyrimidine derivatives evaluated, compound 9a exhibited the highest SGLT2 inhibition activity and underwent further scrutiny. Western blot analysis was employed to determine the impact of 9a on inflammatory and fibrotic proteins, aiming to elucidate its mechanism of action. Additionally, in silico analyses were performed to illuminate the structural dynamics and molecular interaction mechanism of 9a. The overall investigation is crucial for advancing the development of the next generation of anti-diabetic drugs.