Shehaj, Livia published the artcileSmall-Molecule Inhibitors of Haemophilus influenzae IgA1 Protease, SDS of cas: 30165-97-0, the publication is ACS Infectious Diseases (2019), 5(7), 1129-1138, database is CAplus and MEDLINE.
Newly identified, nontypable Haemophilus influenzae (H. influenza) strains represent a serious threat to global health. Due to the increasing prevalence of antibiotic resistance, virulence factors have emerged as potential therapeutic targets that would be less likely to promote resistance. IgA1 proteases are secreted virulence factors of many Gram-neg. human pathogens. These enzymes play important roles in tissue invasion as well as evasion of the immune response, yet there has been limited work on pharmacol. inhibitors. Here, we report the discovery of the first small mol., nonpeptidic inhibitors of H. influenzae IgA1 proteases. We screened over 47 000 compounds in a biochem. assay using recombinant protease and identified a hit compound with micromolar potency. Preliminary structure-activity relationships produced addnl. inhibitors, two of which showed improved inhibition and selectivity for IgA protease over other serine proteases. We further showed dose-dependent inhibition against four different IgA1 protease variants collected from clin. isolates. These data support further development of IgA protease inhibitors as potential therapeutics for antibiotic-resistant H. influenza strains. The newly discovered inhibitors also represent valuable probes for exploring the roles of these proteases in bacterial colonization, invasion, and infection of mucosal tissues.
ACS Infectious Diseases published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C17H19N3O6, SDS of cas: 30165-97-0.
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