Mini Reviews in Medicinal Chemistry - Volume 25, Issue 10, 2025

Schiff bases are an important scaffold for designing drug development. They are characterized by having a carbon-nitrogen double bond. This double bond is synthesized by different synthetic schemes by both the aromatic and aliphatic chains. Bases inspired chemists due to their versatile importance in drug discovery and drug development. A large number of drugs are designed through the heterocyclic Schiff base moieties. This review highlighted the importance of Schiff bases concerning their bioactive importance in drug design. Moreover, amide-iminol tautomerism is a significant tool for the high biological importance of Schiff bases due to the presence of the C=N bond. Furthermore, the reported synthesized heterocyclic scaffolds Schiff bases have a wide range of biological importance. Due to this different biological importance, such as antimicrobial, anticonvulsant, analgesic, antioxidant, antimalarial, anti-inflammatory, anticancer, antidiabetic, and antileishmanial properties, the researcher has shown their interest by synthesizing different heterocyclic Schiff bases. In this review article, biologically active heterocyclic Schiff bases were reviewed intensively concerning drug design and drug development.

Pancreatic cancer (PCa) has a high mortality rate, and early and precision detection is vital to improve the survival rate of PCa. However, current imaging modalities such as ultrasound, CT, MRI, and ¹⁸F-FDG PET/CT are limited in diagnosing distant metastatic lesions and specific visualization. In recent years, small molecule tracers targeting tumor stroma or antigens have made significant progress in preclinical applications for preoperative PCa diagnosis and image-guided intraoperative resection. Tracers targeting integrins (avb6) in tumor stroma and NTR1 in tumor antigens have been undergoing clinical safety validation. This review summarized small-molecule radioactive probes targeting tumor stroma or antigens in PCa, evaluated their imaging characteristics, clinical potential, and the advantages of multi-targeted probe combinations. Additionally, it explored the potential of novel probes for fluorescence imaging-guided intraoperative resection.

Sustainable chemistry and nature-friendly protocols are not only luxury but has become essential requirement for the modern society as it progresses towards a more responsible future. To match the current needs of the community, industries and in particular chemical industry is looking for novel and cheap strategies that have less adverse effects on the environment. Heterocyclic compounds are one particular motif, which is prevalent in nature. It is found in a wide range of synthetic and natural compounds, both established and in development as potent therapeutic candidates. According to the US retail market in 2014-2015, heterocyclic moieties constitute the basic skeletons for 80% of marketed pharmaceuticals. However, majority of the synthetic methodologies still uses classical approaches with toxic solvents, stoichiometric reagents, reactions with less atom economy etc. Thus, there is an urgent need for green, sustainable alternatives of the classical reactions. In recent years, an array of diverse approaches and technologies have been discovered by the scientific community to address the issue of eco-friendly manufacture of various pharmaceutically and medicinally important heterocyclic molecules. In this context, the current review will summarize various reported green pathways to the heterocyclic architecture, particularly O, N, and S-heterocyclic compounds. The methods highlighted in this article includes reaction in environment friendly nonconventional media, solvent-free approaches, heterogeneous catalysis, organocatalysis, electrochemical reactions, microwave-mediated reactions, ultrasound-based reactions, enzymatic reactions, biocatalysis, and others.

Sleep disorders and the resultant sleep deprivation (SD) are very common nowadays, resulting in depressed mood, poor memory and concentration, and various important changes in health, performance and safety. They may provoke further impairment of the cell lining of the blood vessels, as acting as a risk factor for cardiovascular disease (CVD) onset and progression. SD may lead to low neuronal regaining and plasticity, drastically affecting brain function. Thus, SD is a known risk factor for mental, behavioral and developmental disorders. Due to the inflammatory and oxidative stressful nature of SD, immune response modulation and antioxidants could be another therapeutic approach, apart from the already known symptomatic treatment with sedatives. Additionally, many drugs approved for other indications and under investigation, have been revisited due to their wide array of pharmacological activities. This review summarizes the main aspects of SD pathology and SD interrelated comorbidities and presents direct and indirect antioxidant molecules and drugs with multi-targeting potential that could assist in the prevention or management of these factors. A number of research groups have investigated well-known antioxidant compounds with multi-targeting cores, combining structural characteristics with properties including anti-inflammatory, metal chelatory, gene transcription and immune modulatory that may add towards the effective SD and its associated comorbidities treatment.