Química medicinal

New Microbial Collagenase Inhibitors Discovered

Abstract

Georgiana Nitulescu*

Antimicrobial resistance is spreading globally, making healthcare specialists fear "a return to the dark age of medicine". Great efforts are being made to develop new antimicrobials or to repurpose discontinued or shelved drugs to be used against resistant "superbugs". Antibiotic resistance develops in part because the antibiotics we use kill the bacteria. However, this creates a strong selection pressure: a resistant bacterium multiplies while its non-resistant competitors die. As a result, resistance will emerge quickly in the presence of that antibiotic. Another option is to simply disable bacteria, reducing their ability to infect the host. In other words, rather than inhibiting bacterial viability, Bacterial pathogenesis and infectivity are mediated by virulence factors. Collagenases are virulence factors produced by a variety of bacteria, including Clostridium, Bacillus, Vibrio, and Pseudomonas. These enzymes are among the most efficient collagen degraders, and they play an important role in host colonisation. Because of their critical roles in the infection process, they are an important target for the development of new anti-infective agents. The inhibitory activity of 77 compounds on collagenase A was experimentally evaluated using a fluorescence resonance energy-transfer assay in a primary screening.