Current Organic Chemistry - Volume 29, Issue 17, 2025

Metformin is a popular biguanide medicine because of its efficacy and inexpensive cost. Over time, other applications of metformin were found, and the advantages of metformin for diverse conditions such as anticancer, anti-inflammatory, anticoagulant, antimicrobial, and many more were studied. Although the underlying mechanism of these numerous benefits remains unknown, repurposing it is a smart concept, as it offers several advantages, including reduced development and research costs. However, taking it as-is may result in unwanted pharmacokinetics and mild to severe adverse effects. To overcome these, several researchers experimented and reported modified metformin derivatives that had better pharmacological potential, favorable pharmacokinetics, and fewer side effects. This review, therefore, sheds light on the current therapeutic expansion of non-metal derivatives of metformin along with their synthesis methods and evaluated outcomes. This will support researchers studying these modified or replaced metformins in the scientific community.

This review examines the reactivity of bis(α-cyanoacetamides) attached to various spacers in producing heterocyclic and macrocyclic molecules. Bis(α-cyanoacetamides) contain two electrophilic and three nucleophilic sites, allowing for multiple coupling reactions. They are regarded as potent chemical reagents capable of producing various heterocyclic derivatives with potential biological applications. The current review covers all reports where bis(α-cyanoacetamides) are used to prepare heterocycles with mono-, bi-, and tricyclic rings. The review is divided into sections based on the type of annulation system and the number of heteroatoms present. We reviewed all available papers on synthesizing macrocyclic molecular systems using bis(α-cyanoacetamide). The mechanistic postulates of some complex procedures are highlighted.

Kojic Acid (KA) is an oxygen-based heterocycle of natural occurrence and is chemically known as 5-hydroxy-2-(hydroxymethy1)-4H-pyran-4-one. This review has been designed to lighten up the various biological potentials, including the tyrosinase inhibition potential and depigmenting action of KA and its derivatives. KA has very interesting physical and chemical properties and has many applications in the medicinal and cosmetic industries, like antimicrobial, antifungal, antitumor, anti-inflammatory, and depigmentation activities. Despite its medicinal importance, KA possesses a fascinating structure with multiple reactive centers, making it valuable in various chemical transformations. Therefore, a variety of KA derivatives have been/may be prepared with improved stability and with more effective and interesting biological activities than KA itself. Here, in this review, we have briefly described the biological activities of some potent KA derivatives with a brief introduction to the physical and chemical properties of KA. This review would bridge the gap between basic research and applied science, offering value to both scientific and industrial communities.

Organic reactions involve the breaking and formation of bonds, particularly sigma bonds (single bonds) and pi bonds (double and triple bonds). Organic chemists are often more interested in how a reaction works than in why it occurs. With foreknowledge and experience of the reaction details, chemists can generate new compounds and provide a sequential description of each step in the transformations that result in new products. Reaction mechanisms may consist of many steps, including intermediates (like carbocations, carbanions, free radicals, or other species) or transition states between reactants and products. This article will cover 50 key named organic reactions, including every step in each reaction, and their products. In addition, more information on reaction discovery and applications will be discussed. This list represents just a small percentage of the many chemical reactions known in organic chemistry.

Several studies have reported that aldol condensation of various cyclic and acyclic ketones with aromatic aldehydes leads to the formation of symmetrical bisarylidene derivatives, while efficient synthesis of mono- and dissymmetric bisarylidenes is not very common and only a limited number of related reports are available. In the present work, a new one-pot method is designed and performed to synthesize dissymmetric bisarylidene derivatives of tetrahydro-4H-pyran-4-one heterocyclic system. Under the optimized conditions, the first aldehyde reacts with the starting ketone to give the corresponding monoarylidene. This monoarylidene can be either isolated as product 2 or used as the intermediate for a subsequent condensation with the second aldehyde to produce the respective derivative of 3. Both steps can take place in one pot, and high yields of either the monoarylidene intermediates or the final dissymmetric bisarylidene products would be obtained in short time intervals. The method is amenable to the synthesis of both mono- and dissymmetric bisarylidenes of the target compounds. New products of the reaction are fully characterized based on their ¹H NMR, ¹³C NMR, IR, and mass spectroscopic data. The purity of these products is confirmed by elemental analyses. The results are promising to expand the outcome by applying the conditions to the synthesis of the respective derivatives of other heterocyclic systems.

Gossypol has been shown to be a promising natural product for the anticancer drug development for treating leukemia, lymphoma, colon carcinoma, breast cancer, and other malignant disease. It is known that the conversion of aldehyde groups of gossypol into iminofragments by the treatment of various amines can reduce the toxicity of the derivative and simultaneously increase their pharmacological efficacy. This article describes the preparation and screening of antiproliferative properties of a conjugate of gossypol with antitumor antibiotic doxorubicin. It has been shown that the reaction of the amino group of doxorubicin with the aldehyde groups of gossypol gives the condensation product in which two pharmacophores are linked via enamine–enamine moieties. However, this conjugation decreased the antiproliferative activity of paternal doxorubicin and gossypol against chronic myeloid leukemia cells K562 and led to dramatic loss of potency against MDR-subline K-562/4 with expression of Р-glycoprotein (Р-gp).

Using ultrasound, the synthesis of substituted 2-amino (or 2-alkoxy) benzimidazoles through a multi-component, one-pot reaction of 2-iodoaniline and amine (or alcohol)-trichloroacetonitrile (CCl3CN) adduct with the help of a catalytic amount of copper(I) iodide in dimethylformamide at room temperature has been presented. Using basic materials, simple and available reagents, gentle copper-catalyzed reaction conditions, easy purification with the help of solvent, decent efficiency, applying a simple and efficient sonochemical method, reacting in the shortest time, and finally, the synthesis of 18 new heterocycle compounds are appreciable features of this protocol.