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Molecular Docking, Synthesis And Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines Derivatives As Non-Β-Lactam Β-Lactamases Inhibitors, Joseph Osamudiamen Osazee
Molecular Docking, Synthesis And Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines Derivatives As Non-Β-Lactam Β-Lactamases Inhibitors, Joseph Osamudiamen Osazee
Electronic Theses and Dissertations
Our research aim was to design, synthesize, and study the competitive enzyme inhibition kinetics of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives as potential non-²-lactam ²-lactamase inhibitors. All compounds (1-13) passed the Lipinski’s rule of 5 test and were docked into the active site of TEM-1 ²-lactamase. PBD derivatives 1-7 were synthesized in high yields and tested for their potency against TEM-1 and P99 ²-lactamases. Kinetic data showed that compounds 1, 4, 5, and 7 possessed inhibitory activity against TEM-1 ranging from 4-34 %. Docking results revealed significant interactive spanning of the active site of TEM-1 by PBDs. …
Synthesis, Characterization And Biological Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines For Cytotoxicity And Serine Β-Lactamases Inhibition, Joel K. Annor-Gyamfi
Synthesis, Characterization And Biological Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines For Cytotoxicity And Serine Β-Lactamases Inhibition, Joel K. Annor-Gyamfi
Electronic Theses and Dissertations
Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives possess cancerostatic and anti-infective properties thus making them candidates of possible antibacterial agents. ²-lactam antibiotics are vital weapons for the treatment of bacterial infections, but their existence and effectiveness has been faced with resistance from ²-lactamases. Therefore, the need for new effective antimicrobial drugs is very crucial. In this work, we synthesized in high yields, PBD analogs 1−3, 5 and 7−9 in three to four synthetic steps from commercially available L-proline and isatoic anhydride. MTT Assay was employed to test the in vitro cytotoxicity of PBD analogs 1, 2, 5 …