Time filter

Source Type

Waltham, MA, United States

Green O.M.,Infection Innovative Medicines Unit | McKenzie A.R.,Infection Innovative Medicines Unit | Shapiro A.B.,Infection Innovative Medicines Unit | Otterbein L.,Valeocon Management Consulting | And 6 more authors.
Bioorganic and Medicinal Chemistry Letters

A novel arylsulfonamide-containing series of compounds represented by 1, discovered by highthroughput screening, inhibit the acetyltransferase domain of N-acetylglucosamine-1-phosphate-uridyltransferase/glucosamine-1-phosphate- acetyltransferase (GlmU). X-ray structure determination confirmed that inhibitor binds at the site occupied by acetyl-CoA, indicating that series is competitive with this substrate. This letter documents our early hit-to-lead evaluation of the chemical series and some of the findings that led to improvement in in-vitro potency against Gram-negative and Gram-positive bacterial isozymes, exemplified by compound 40. © 2012 Elsevier Ltd. All rights reserved. Source

Discover hidden collaborations