G.V.P. Chandramouli

An Efficient One-Pot Three-Component Synthesis of Novel Sulfanyl Tetrazoles Using Ionic Liquids

An efficient, simple, and environmentally benign method for the synthesis of novel sulfanyl tetrazoles has been achieved by one-pot three-component reaction of phenacyl bromides/3-(2-bromoacetyl)coumarins with KSCN and NaN3 using [Bmim]BF4 ionic liquid. It could be reused and recycled for four runs without significant loss of product yield.

Design, synthesis and evaluation of novel pyrazolo-pyrimido[4,5-d]pyrimidine derivatives as potent antibacterial and biofilm inhibitors

An efficient four-component reaction of 6-amino-1,3-dimethyluracil, N,N-dimethylformamide dimethylacetal, 1-phenyl-3-(4-substituted-phenyl)-4-formyl-1H-pyrazoles and aromatic amines was conducted in the presence of [Bmim]FeCl4 ionic liquid as a promoting medium. This strategy provided a convenient route without any additional catalyst or metal salt under mild conditions. All the synthesized pyrazolo-pyrimido[4,5-d]pyrimidines derivatives were evaluated for their antibacterial, minimum bactericidal concentration (MBC), biofilm inhibition, intracellular ROS accumulation and protein leakage activities. The results revealed that among all the screened derivatives, the compounds 5c, 5i, 5l and 5m were quite promising with MIC values ranging between 3.9 and 15.6μg/mL, while the MBC values were 2-fold the antibacterial activity values. The biofilm inhibition activity revealed that the compounds 5l and 5m exhibited promising activity with IC50 values ranging between 1.8 and 8.2μg/mL. It was observed that at a concentration of 0.5μg/mL, the compound 5l treated biofilms of Micrococcus luteus showed increased levels of intracellular ROS accumulation. Further, the protein leakage study revealed that the Micrococcus luteus cells treated with compound 5l caused membrane permeability which resulted in protein leakage and subsequent bacterial cell death.

α-Glucosidase inhibitory activity, molecular docking, QSAR and ADMET properties of novel 2-amino-phenyldiazenyl-4H-chromene derivatives

α-Glucosidase inhibitory activity, molecular docking, QSAR and ADMET properties of novel 2-amino-phenyldiazenyl-4H-chromene derivatives Onkara Perumal, Sagar Vijay Kumar Peddakotla, Lingala Suresh, G.V.P. Chandramouli* and Y. Pydisetty* Department of Biotechnology, National Institute of Technology, Warangal 506 004, Telangana, India; Department of Chemistry, National Institute of Technology, Warangal 506 004, Telangana, India; Department of Chemical Engineering, National Institute of Technology, Warangal, 506 004, Telangana, India

Design, Synthesis, and In Vitro Antimicrobial Evaluation of Fused Pyrano[3,2-e]tetrazolo[1,5-c]pyrimidines and Diazepines

A series of novel pyranochromene-containing tetrazoles fused with pyrimidinethiones, pyrimidines, and diazepines 3a–f, 4a–f, and 5a–f were synthesized by condensation of the corresponding tetrazoles 2a–f with carbon disulfide, benzaldehyde, and 4-methoxy phenacyl bromide, respectively. The compound 2a–f was obtained by reaction of pyrano[3,2-c]chromenes 1a–f with sodium azide. The structures of the newly synthesized compounds 2a–f to 5a–f were established on the basis of their elemental analyses, IR, 1H NMR, 13C NMR, and mass spectral data. All of the title compounds were subjected to in vitro antibacterial testing against four pathogenic strains and antifungal screening against two fungi. Preliminary results indicate that some of them exhibited promising activities and that they deserve more consideration as potential antimicrobials.

An efficient one-pot three-component synthesis of imidazol-2-ones using [Bmim]BF4 ionic liquid

A mild and efficient method was developed for preparation of imidazol-2-ones via one-pot three-component condensation of 1,3-cyclic diketones, aryl glyoxals and urea using [Bmim]BF4 ionic liquid. Excellent yields, short reaction time, simple work-up, and reusability of IL are advantages of this procedure.