Current Organic Chemistry - Volume 26, Issue 2, 2022

A review concerning the synthesis and pharmacological properties of pyrazoles obtained from Chalcone described in the literature over the last 5 years (2016-2020) was presented and discussed. Among the synthetic approaches for pyrazoles described so far, the cyclization and acetylation method of α,β-unsaturated chalcones, and substituted hydrazine were selected and analyzed. 105 pyrazole derivatives (3-107) were evaluated as well as their pharmacological activities, namely, antineoplastic, anti-inflammatory, antioxidant, antibacterial, antifungal, antimycobacterial, antiplasmodial, Alzheimer's disease, enzymes inhibition (like acetylcholinesterase, carbonic anhydrase, and malonyl CoA decarboxylase), anticonvulsant, among others. Pyrazolic compounds are widely used in the design of the new drug with a wide spectrum of pharmacological approaches. Therefore, it is relevant to research the synthetic methods and therapeutic properties of different pyrazole derivatives.

Dimethyl sulfoxide (DMSO) is not only a common and cheap aprotic polar solvent with low toxicity but also serves as an efficient and multipurpose reactant, and has widely been used in organic synthesis. DMSO as an important precursor can effectively introduce a broad range of functional fragments into organic molecules, such as -Me, -CH, -CH2, -SMe2, - CH2SMe, -CH2SOMe, -SMe, -SO2Me, -SOMe or O substituents, and serves as a mild oxidant in organic transformations. Many significant achievements based on DMSO as a synthon in synthetic chemistry have rapidly been made over the past several years. To help researchers further understand the recent advances in the field, the review summarizes the applications of DMSO as carbon, sulfur, and oxygen sources and its use as the dual synthon in synthetic transformations.

Functionalized bicyclic pyrimidinones and their derivatives are significant heterocyclic scaffolds being their all-around prevalence in biologically potent compounds. In several attempts to explore the different synthetic methodologies for the construction of bicyclic condensed pyrimidinones, different researchers from all across the globe have reported numerous substantial methods. In the present review, considerable work has been critically compiled on the synthesis of substituted and functionalized bicyclic pyrimidinones from 2000 onwards.

Barbituric acid is a pyrimidine heterocyclic organic compound, which is pharmacologically active. It is important to build structures containing various medicinal activities. This compound attracts the scientific research community in organic synthesis. It can be used in the synthesis of polyheterocyclic, natural, medicinal compounds, and organic sensors. Herein, the utilization of barbituric or thiobarbituric acid in multicomponent reactions is reported from 2016-2021 in this manuscript.

Benzothiazoles have recognized pharmacophores in the field of research, predominantly in synthetic and medicinal chemistry, on account of their significant pharmaceutical properties. This important class of derivatives endows an extensive range of biological activities like anti-inflammatory, antidiabetic, anticancer, anticonvulsant, antibacterial, antiviral, antioxidant, antituberculosis, enzyme inhibitors, etc. Hence, various methodologies have been accomplished to synthesize benzothiazole compounds considering the purity, yield, and selectivity of the products. This review provides different reaction methods that are involved in the synthesis of a variety of benzothiazole derivatives.