Balaji R. Madje

An efficient approach for the synthesis of medicinally important dihydropyrano[2,3- c ]pyrazoles derivatives by using Fe ₃ O ₄ @BTC nanocomposite (NCs) based catalytic system.

A series of fluorinated pyrazoles was synthesized in a straightforward manner without the use of hazardous catalysts, toxic solvents, or extreme reaction conditions, yielding high product efficiency. Fluorinated aldehyde and piperonal underwent a condensation reaction to form a chalcone intermediate, which was subsequently cyclized with hydrazine hydrate to yield the corresponding pyrazole derivatives. The structures of the synthesized compounds were confirmed using IR, ¹H NMR, and mass spectrometry. These compounds were then evaluated for their antibacterial and antitubercular activity. Molecular docking studies revealed high binding affinity scores across the entire series.

In this work, we synthesized a heterogeneous magnetic nanocatalyst using iron oxide (Fe ₃ O ₄ ) surface‐modified with L‐arginine@NiO (Fe ₃ O ₄ @L‐Arg@NiO). Several characterization techniques such as fourier transform infrared (FT‐IR), field emission scanning electron microscopy (FE‐SEM), X‐ray diffraction (XRD), high‐resolution transmission electron microscopy (HR‐TEM), electron dispersion spectra (EDS) and thermogravimetric analysis (TGA) were used to extensively analyze its structural and morphological properties. The Fe ₃ O ₄ @L‐Arg@NiO nanocatalyst was subjected to the one‐pot multi‐component synthesis of 3,4‐dihydropyrimidin‐2‐(1 H )‐ones derivatives under solvent‐free conditions. It was determined that nanocatalyst Fe ₃ O ₄ @L‐Arg@NiO demonstrating desired product 3,4‐dihydropyrimidin‐2‐(1 H )‐ones with 85%–95% yield, in shorter reaction time. Furthermore, simple work‐up, reusability of the catalyst up to five cycles and sustainability of the catalyst are characteristic features of this environment friendly protocol.

Oriental Journal of Chemistry is a peer reviewed quarterly research journal of pure and applied chemistry. It publishes standard research papers in almost all thrust areas of current chemistry of academic and commercial importance. It provides a platform for rapid publication of quality research papers, reviews and chemistry letters. Oriental Journal of Chemistry is abstracted and indexed in almost all reputed National and International agencies.

A novel series of benzene sulfonamide pyrazole oxadiazole derivatives have been synthesized by reaction of 4-(5-(3-fluoro-4-methoxyphenyl)-3-(hydrazinecarbonyl)-1H-pyrazol-1-yl) benzene sulfonamide with different substituted benzoic/pyridinyl/indolyl acids in phosphorous oxychloride, characterized by IR, ¹H NMR, ¹³C NMR, MS analytical data and evaluated for their antimicrobial as well as antitubercular activity. Molecular docking studies against Mycobacterium tuberculosis β-ketoacyl-acyl carrier protein synthase A, (Kas-A) was carried out to understand the possible mode of its inhibition and potential of synthesized compounds as antitubercular agents. Antibacterial activity of compounds 5d (3-Cl) and 5f (2,4-diCl) were found good against E. coli, P. aeruginosa, S. aureus and S. pyogenes as compared to standard Ampicillin. Compound 5d was found active antitubercular agents against M. tuberculosis H₃₇Rv. Graphical Abstract

The saccharine nucleus has long been recognized as a significant component in medicine. A series of Pseudo-saccharine amines derivatives (7a-j) were synthesized and examined for their antibacterial activity. After testing all compounds, the compounds 7b, 7f, 7g, 7i and 7j were found most effective against Escherichia coli, Streptococcus aureus and Bacillus subtilis strains. The MIC of the compound was found from 4.6 to 16.1 μM. Further, compound 7f and 7i exhibited excellent activity against E.coli and Bacillus subtilis with MIC value 4.6 and 4.7 μM respectively. The compound 7b and 7i was found active against all the three bacteria. The zone inhibition was observed at 10 μM against Escherichia coli, Staphylococcus aureus and Bacillus subtilis at 0.9, 1.8, 3.9 respectively for 7b and 1.0, 1.8, and 2.0 cm respectively for 7i.

In the present investigation, a series of 4‐((3‐(trifluoromethyl)‐5,6‐dihydro‐[1,2,4]triazolo[4,3‐a]pyrazin‐7(8H)‐yl)methyl)benzenamine analogs 6a–o were synthesized and characterized by IR, NMR (¹H and ¹³C), and mass spectra. All newly synthesized compounds 6a–o were prepared under conventional and microwave irradiation methods. These compounds obtained in higher yields and in shorter reaction times in the microwave irradiation method when compared with the conventional method. Synthesized compounds 6a–o were inspected for their in vitro antitubercular activity against Mycobacterium tuberculosis H₃₇Ra using an established XTT reduction menadione assay. Among the screened compounds, 6i (IC₅₀: 1.82 μg/mL), 6j (IC₅₀: 1.02 μg/mL), and 6k (IC₅₀: 1.59 μg/mL) showed excellent activity. Furthermore, compound 6i showed MIC₉₀ value of 16.02 μg/mL. In summary, the results indicate the identification of some novel, selective, and specific inhibitors against M. tuberculosis that can be explored further for the potential antitubercular drug.

A novel series of benzene sulfonamide pyrazole linked [1,2,4]-triazolo[3,4-b][1,3,4]thiadiazole derivatives have been synthesized by reaction of 4-(3-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-5- (3-fluoro-4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide with different substituted benzoic/ pyridinyl/indolyl acids in POCl3, characterized by IR, 1H NMR, 13C NMR, MS analytical data and evaluated for their antibacterial as well as antifungal activity. Antibacterial activity of compounds 6c, 6i and 6k were found good against E. coli, P. aeruginosa, S. aureus and S. pyogenes compared to standard ampicillin. Compounds 6b and 6e is having promising antifungal activity against C. albicans as compare to standard griseofulvin.