Identification of arylsulfonamides as ExoU inhibitors
ExoU is a potent virulence factor of Pseudomonas aeruginosa and is considered a potential therapeutic target. In order to discover novel ExoU inhibitors, we screened an in-house chemical library utilizing a yeast-based screening system. Some sulfonamides displayed significant activity without nonspecific cytotoxicity. We describe a series of sulfonamides as novel ExoU inhibitors, along with a brief structure-activity relationship.
Kim, Doran,Baek, Jihae,Song, Jiho,Byeon, Hyeyoung,Min, Hyeyoung,Min, Kyung Hoon
supporting information
p. 3823 - 3825
(2014/09/03)
From sensors to silencers: Quinoline- and benzimidazole-sulfonamides as inhibitors for zinc proteases
Derived from the extensive work in the area of small molecule zinc(II) ion sensors, chelating fragment libraries of quinoline- and benzimidazole- sulfonamides have been prepared and screened against several different zinc(II)-dependent matrix metalloproteinases (MMPs). The fragments show impressive inhibition of these metalloenzymes and preferences for different MMPs based on the nature of the chelating group. The findings show that focused chelator libraries are a powerful strategy for the discovery of lead fragments for metalloprotein inhibition.
Rouffet, Matthieu,De Oliveira, Cesar Augusto F.,Udi, Yael,Agrawal, Arpita,Sagi, Irit,McCammon, J. Andrew,Cohen, Seth M.
supporting information; experimental part
p. 8232 - 8233
(2010/08/05)
More Articles about upstream products of 712271-18-6