Ontology highlight
ABSTRACT:
SUBMITTER: Testa C
PROVIDER: S-EPMC4255721 | biostudies-literature | 2014 Nov
REPOSITORIES: biostudies-literature
Testa Chiara C Scrima Mario M Grimaldi Manuela M D'Ursi Anna M AM Dirain Marvin L ML Lubin-Germain Nadège N Singh Anamika A Haskell-Luevano Carrie C Chorev Michael M Rovero Paolo P Papini Anna M AM
Journal of medicinal chemistry 20141113 22
Side chain-to-side chain cyclizations represent a strategy to select a family of bioactive conformations by reducing the entropy and enhancing the stabilization of functional ligand-induced receptor conformations. This structural manipulation contributes to increased target specificity, enhanced biological potency, improved pharmacokinetic properties, increased functional potency, and lowered metabolic susceptibility. The Cu(I)-catalyzed azide-alkyne 1,3-dipolar Huisgen's cycloaddition, the prot ...[more]