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The present study mainly focused on synthesizing novel triazolo[1,5‐a]pyrimidine‐6‐carboxamide derivatives using multicomponent reaction. Synthesized derivatives were duly characterized using spectroscopic methods of analysis FT‐IR and mass spectroscopy, and 1H NMR and 13C NMR confirmed the structure of compounds. Further, the potential of the synthesized compounds against Plasmodium falciparum dihydrofolate reductase (Pf‐DHFR) inhibitors was evaluated by in vitro antimalarial activity, and the results of the study showed moderate to good antimalarial profile of synthesized entities. In silico study of all the synthesized compounds was carried out using Schrödinger LLC‐2020‐3 Software to explain the binding mode and interactions between molecules and pf DHFR enzyme. To study the drug likeliness of molecules, 3D QSAR and Pharmacokinetic studies have been carried out, and the results obtained showed a good pharmacokinetics profile of two compounds, namely AMP‐24 and AMP‐28, having good IC50 values concerning standard drugs. Further, the in vitro enzyme inhibition assay results suggested that the synthesized compound interacts nicely with the enzyme and might be used as a potent antimalarial agent. [ABSTRACT FROM AUTHOR]

An optimization and modification of Grimmel's method leading to cyclization and incorporation of glycine linked sulphonamide at position-2 in 4-quinazolin-(3H)-ones was accomplished. Generation of a lipophilic site at position-3 of 4-quinazolinones was explored by synthesis of imines, unfortunately leading to an isomeric mixture of stereoisomers. These stereoisomeric mixtures were further converted to a single isomer utilizing the novel methodology developed by the use of an aprotic solvent system. Moreover, a mixture of (Z)/(E)-isomers and single configuration was identified and ascertained using NMR, HMQC, HMBC and NOESY spectroscopic techniques. The synthesized entities were further screened for their antimalarial efficacy pertaining two active scaffolds 8m and 8s. The active molecules were sent forth for enzyme inhibitory study against presumed receptors h-DHFR and Pf-DHFR computationally as well as in vitro, proving their potency as dihydrofolate reductase inhibitors. The oral bioavailability of these active molecules was also predicted by the study of ADME properties, indicating good bioavailability of the active entities. [ABSTRACT FROM AUTHOR]

Sulfonamide substituted 8-hydroxyquinoline derivatives were prepared using a microwave synthesizer. The interaction of sulfonamide substituted 8-hydroxyquinoline derivatives and their transition metal complexes with Plasmid (pUC 19) DNA and Calf Thymus DNA were investigated by UV spectroscopic studies and gel electrophoresis measurements. The interaction between ligand/metal complexes and DNA was carried out by increasing the concentration of DNA from 0 to 12 μl in UV spectroscopic study, while the concentration of DNA in gel electrophoresis remained constant at 10 μl. These studies supported the fact that, the complex binds to DNA by intercalation via ligand into the base pairs of DNA. The relative binding efficacy of the complexes to DNA was much higher than the binding efficacy of ligands, especially the complex of Cu-AHQMBSH had the highest binding ability to DNA. The mobility of the bands decreased as the concentration of the complex was increased, indicating that there was increase in the interaction between the metal ion and DNA. Complexes of AHQMBSH were excellent for DNA binding as compared to HQMABS. [ABSTRACT FROM AUTHOR]

Cefadroxil drug loaded biopolymeric films of chitosan-furfural schiff base were prepared by reacting chitosan with furfural in presence of acetic acid and perchloric acid respectively for the external use. Prepared films were evaluated for their strength, swelling index, thickness, drug content, uniformity, tensile strength, percent elongation, FTIR spectral analysis and SEM. The results of in vitro diffusion studies revealed that the films exhibited enhanced drug diffusion as compared to the films prepared using untreated chitosan. The films also demonstrated good to moderate antibacterial activities against selective gram positive and gram negative bacteria. [ABSTRACT FROM AUTHOR]

A novel 4-[(8-hydroxyquinolin-5-yl)methyl]aminobenzenesulfonamide (HQMABS) was synthesized by optimized reaction of 4-aminobenzenesulfonamide with 5-chloromethyl-8-hydroxyquinoline hydrochloride (CMHQ). Various oxinates of HQMABS were also prepared using Mn(II), Fe(II), Co(II), Ni(II), Cu(II), and Zn(II) metal salts. All compounds were analyzed by physicochemical, thermogravimetric and spectroscopic techniques. Antimicrobial activity was carried out using agar-plate method against various strains of bacteria (Staphylococcus aureus, Bacillus subtillis, Pseudomonas aerugionsa, and Escherichia coli) and spores of fungi (Aspergillus niger and Aspergillus flavous). The results showed significantly higher antimicrobial activity of HQMABS compared to the parent 8-hydroxyquinoline and sulfonamide, while oxinates of HQMABS showed milder activity.