Metal-ligand coordination involving hydrogen-bond-functionalized ligands was employed rationally to get an easy access to a series of metallogelators derived from 3-pyridyl derivatives of nonsteroidal anti-inflammatory drugs [e.g., ibuprofen, sulindac, and flurbiprofen designated as 3-pyIBU, 3-pySUL, and 3-pyFLR, respectively] and biogenic metal centers [Zn(II), Cu(II), Mn(II), and Ag(I)]. A total of 13 metallogels (MG1-MG13) were obtained by allowing the ligands and the metal salts to react in dimethyl sulfoxide (DMSO)/water at room temperature. A slightly different solvent system (DMSO/water/MeOH) afforded four crystalline coordination complexes of 3-pyIBU, namely, [{Cu(3-pyIBU)(DMSO)}(NO)] (CC1), [{Ag(3-pyIBU)}(BF)] (CC2), [{Ag(3-pyIBU)}(ClO)] (CC3), and [{Cu(3-pyIBU)(CHOH)}(OTf)] (CC4), which were fully characterized by single-crystal X-ray diffraction. However, none of these coordination complexes produced metallogels-the results corroborated well with the rationale, based on which the metallogelators were obtained. Two selected metallogels (MG3 and MG9) could be leached out from the corresponding metallogels to the bulk solvent to the extent of 51 and 59%, respectively after 24 h of incubation at 37 °C, indicating their plausible use in topical application. Moreover, one of the selected metallogelators, i.e., MG9, displayed anti-inflammatory response and was able to inhibit the migration of highly aggressive human breast cancer cells MDA-MB-231, suggesting its plausible use as anticancer agent.

: Piperazine scaffolds are a group of heterocyclic atoms having pharmacological values and shows significant results in pharmaceutical chemistry. Piperazine has the flexible core structure for the design and synthesis of new bioactive compounds. These flexible heterogenous compounds exhibit various biological roles, primarily anticancer, antioxidant, cognition enhancers, antimicrobial, antibacterial, antiviral, antifungal, anti-inflammatory, anti-HIV-1 inhibitors, antidiabetic, antimalarial, antidepressant, antianxiety and anticonvulsant activities etc. In the past few years, researchers focused on the therapeutic profile of piperazine synthons for different biological targets. The present review highlights the development in designing and pharmacological activities of nitrogen-containing piperazine moiety as a therapeutic agent. The extensive popularity of piperazine as a drug of abuse and their vast heterogeneity research efforts over the last years motivated the new investigators to further explore this area.

Background:: This review elaborates the updated synthetic and pharmacological approaches of a known group of dihydropyrimidinones/thiones from the multi-component reaction like Biginelli reaction was named Pietro Biginelli in 1891. This review consists of the reaction of an aromatic aldehyde, urea and ethyl acetoacetate leading to dihydropyrimidinone/thione. Currently, the scientific movement to develop economically viable green methods using compounds that are reusable, non-volatile, easily obtained, etc. Objective:: This review covers the recent synthesis and pharmacological advancement of dihydropyrimidinones/thiones moiety, along with covering the structure-activity relationship of the most potent compounds, which may prove to become better, more efficacious and safer agents. Thus, this review may help the researchers in drug designing and development of new Dihydropyrimidinones entities. Conclusion:: This review focuses on the wide application of dihydropyrimidinone/thione review reports the design, synthesis and pharmacological activities of nitrogen-sulphur containing dihydropyrimidinone moiety by using multi-component reaction. Dihydropyrimidinones (DHPM) pharmacophore is an important heterocyclic ring in medicinal chemistry. It is derived from multi-component reactions, “Biginelli reaction” and plays critical role as anticancer, antioxidant, antimicrobial, antiinflammatory, anti-HIV-1, antimalarial, anti-inflammatory, antihypertensive and anti-tubercular agents. Exhaustive research has led to the determination of its vast biological profile, with a wide range of therapeutic application.

Dengue fever is prevalent in subtopic regions, producing mortality and morbidity worldwide, which have been of major concern to different governments and World Health Organization. The search of new anti‐dengue agents from phytochemicals was assumed to be highly emergent in past. The phytochemicals have been used in wide distribution of vector ailments such as malaria. The demand of the phytochemicals is based on the medicines which are mostly considered to be safer, less harmful than synthetic drugs and nontoxic. This review mentions majorly about the phytochemicals potentially inhibiting dengue fever around the world. The phytochemicals have been isolated from different species, have potential for the treatment of dengue. Different crude extracts and essential oils obtained from different species showed a broad activity against different phytochemicals. The current studies showed that natural products represent a rich source of medicines toward the dengue fever. Furthermore, ethnobotanical surveys and laboratory investigation established identified natural plants species in the development of drug discovery to control the dengue fever.

Background: Isatin (IST) is a crucial pharmacologically active compound, chemically known as indole-1H-2,3- dione. Development of different IST based analogues acquired significant awareness because of its pronounced therapeutic importance such as analgesic, anticancer, anti-inflammatory, antitubercular, antimicrobial, antifungal, antiviral (effective against SARS coronavirus 3C protease) and many other activities, and represent an important class of heterocyclic compounds that can be used as a precursor for the synthesis of many useful drugs. Objective: Previously many articles were reported on IST synthesis and their different pharmacological activities but herein, we mentioned 59 different synthesis schemes of several IST derivatives/hybrids derived from the substitution of the nitrogen, aromatic ring, the second and third position of IST along with most potent molecule among each of synthesized libraries with their structural activity relationship (SAR). Using these standardized approaches several biological important compounds were developed like sunitinib, nintedanib, indirubin, etc and several studies have been carried out in nowadays to develop newer compounds having fewer side effects and also overcome the problem of resistance. Conclusion: This report critically reviews the different strategies for the designs and synthesis of several IST based compounds having different biological activities with SAR which can favour further investigation and modification for the development of new and more potent entities.