Bioorganic and Medicinal Chemistry Letters 2006-Jul
Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1.
কেবল নিবন্ধিত ব্যবহারকারীরা নিবন্ধগুলি অনুবাদ করতে পারবেন
প্রবেশ করুন - নিবন্ধন করুন
লিঙ্কটি ক্লিপবোর্ডে সংরক্ষিত হয়েছে
কীওয়ার্ডস
বিমূর্ত
A new class of tumor necrosis factor alpha (TNF-alpha) synthesis inhibitors based on an N-2,4-pyrimidine-N-phenyl-N'-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-alpha production. X-ray co-crystallization studies with mutated p38alpha showed that these trisubstituted ureas interact with the ATP-binding pocket in a pseudo-bicyclic conformation brought about by the presence of an intramolecular hydrogen bonding interaction.