Current Organic Chemistry - Volume 29, Issue 7, 2025

Andrographis is a member of the family Acantheceae. It contains approximately 44 accepted species. Among them, Andrographis paniculata has been extensively studied during the last decade. The genus contains triterpenoids as the main class of compound, along with carotenoids, flavonoids, glycosides, xanthones, phenolic compounds, and fatty acid compounds. A. paniculata has been reported in Ayurveda, homeopathy, naturopathy, and Siddha. Traditionally, the genus is utilized in treating diarrhea, parasitic problems, liver illness, various skin problems, fever, snake bites, cough and many more. Pharmacological activities like antioxidant, neuroprotective, anti-inflammatory, antimalarial, hepatoprotective, antibacterial antiviral, anticancer, and antidiabetic have been documented in it with scientific evidence. Various components found in this genus show broad biological opportunities for novel medicinal medicines. Andrographolide is the major chemical constituent present in almost all the species. It has been reported for various pharmacological activities, mostly for antioxidant and anticancer. The genus is widely spread among India, China, Southeast Asia, Sri Lanka, Vietnam, Thailand, and basically tropical and subtropical Asia. In India, it is found in Nallamala Hills, Andhra Pradesh, and South India. The present review has provided a critically analyzed vision of phytochemistry, traditional uses, and pharmacological applications of the genus Andrographis. The current information was collected systematically from scientific databases, including Google Scholar, PubMed, ACS Publications, SciFinder, Science Direct, and Web of Science.

A novel series of 4-[3-acetyl-2-(N-alkyl(aryl)acetamido)-1,3,4-thiadiazol-5-yl]-3-(2-oxo-2H-chromen-3-yl)-1-(4-phenylthiazol-2-yl)-1H-pyrazoles (2a-i) and 3 was synthesized in good yields. The methodology was depended on a one-pot four-components reaction of hydrazine hydrate, alkyl(aryl) isothiocyanate, 3-(2-oxo-2H-chromen-3-yl)-1-(4-phenylthiazol-2-yl)-1H-pyrazole-4-carboxaldehyde (1), and acetic anhydride in acetic acid under ultrasound irradiation. The spectral tools confirmed the structures of all synthesized compounds. Using the standard SRB method, the designed compounds were screened for their in vitro cytotoxicity properties against PC3, HepG2, and HCT116 human cancer cell lines. Products 2a and 2c worked best against all cancer cells tested, as well as doxorubicin. Apoptosis and cell cycle analyses were performed for the bioactive products 2a and 2c. Both products strongly impacted all tumor cells in the late apoptotic pathway and significantly inhibited all cancer cell types under investigation in both the S and G2 phases. After that, a molecular docking study was carried out on products 2a and 2c to investigate how they interact with the CDK-8 receptor. The ADMET prediction suggested that these bioactive products may be effective anticancer treatments.

A series of 4-thiazolidinone was synthesized and characterized by means of TLC, melting point, and spectral data like IR, ¹H NMR, and Mass spectra. The anti-inflammatory activity of the synthesized compounds was determined via in vivo studies. The antioxidant properties of the synthesized compounds were determined by carrageenan-induced rat paw edema model. The synthesized compounds (A1-A14) showed significant anti-inflammatory and antioxidant activities. The most promising results for both antioxidant and anti-inflammatory activity were exhibited by compound A8 which may emerge as a potent anti-inflammatory agent with potential free radical scavenging activity. Molecular docking studies were carried out to determine the interaction of compounds into the active site of COX-2 inhibitor (PDB ID: 3LN1), which suggested compound A8 to have the best docking score by showing interactions with ASP483 and LYS478.

In this study, functionalized 2-(trichloromethyl)-1H-benzo[d]imidazole derivative with good yields was synthesized using a copper-catalyzed N-arylation reaction of 2-iodoaniline and trichloroacetonitrile. This reaction was performed by employing the catalytic value of copper (I) and 1,10-phenanthroline as the ligand in tetrahydrofuran solvent at 23°C. In the following, the reaction of the final product with phenylacetylene and sodium azide (Huisgen reaction) using the copper catalyst in water solvent at 23°C led to the synthesis of new (1,2,3-triazol)-1H-benzo[d]imidazole derivatives with the principles of green chemistry and suitable efficiency. The availability of raw materials and suitable catalysts, mild reaction conditions, and easy purification are among the advantages of this method for the synthesis of various multi-substituted benzo[d]imidazole and 1,2,3-triazole derivatives.