Matches in SemOpenAlex for { <https://semopenalex.org/work/W2016919782> ?p ?o ?g. }
- W2016919782 endingPage "2211" @default.
- W2016919782 startingPage "2194" @default.
- W2016919782 abstract "Starting with our previously described(20) class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The resulting compound, 32, is a potent and selective antagonist of CCR3. SAR studies showed that the 3-acetylphenyl urea of 32 could be replaced with heterocyclic ureas or heterocyclic-substituted phenyl ureas and still maintain the potency (inhibition of eotaxin-induced chemotaxis) of this class of compounds in the low-picomolar range (IC(50) = 10-60 pM), representing some of the most potent CCR3 antagonists reported to date. The potency of 32 for mouse CCR3 (chemotaxis IC(50) = 41 nM) and its oral bioavailability in mice (20% F ) were adequate to assess the efficacy in animal models of allergic airway inflammation. Oral administration of 32 reduced eosinophil recruitment into the lungs in a dose-dependent manner in these animal models. On the basis of its overall potency, selectivity, efficacy, and safety profile, the benzenesulfonate salt of 32, designated DPC168, entered phase I clinical trials." @default.
- W2016919782 created "2016-06-24" @default.
- W2016919782 creator A5000577175 @default.
- W2016919782 creator A5003290621 @default.
- W2016919782 creator A5004945278 @default.
- W2016919782 creator A5008465197 @default.
- W2016919782 creator A5012636274 @default.
- W2016919782 creator A5013375925 @default.
- W2016919782 creator A5024851679 @default.
- W2016919782 creator A5025403167 @default.
- W2016919782 creator A5026686512 @default.
- W2016919782 creator A5026919411 @default.
- W2016919782 creator A5027338053 @default.
- W2016919782 creator A5031917567 @default.
- W2016919782 creator A5041230347 @default.
- W2016919782 creator A5041737648 @default.
- W2016919782 creator A5044857121 @default.
- W2016919782 creator A5048051155 @default.
- W2016919782 creator A5050194203 @default.
- W2016919782 creator A5052413109 @default.
- W2016919782 creator A5057427778 @default.
- W2016919782 creator A5060895438 @default.
- W2016919782 creator A5064365336 @default.
- W2016919782 creator A5068506060 @default.
- W2016919782 creator A5085891803 @default.
- W2016919782 creator A5089299226 @default.
- W2016919782 date "2005-01-14" @default.
- W2016919782 modified "2023-10-12" @default.
- W2016919782 title "Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency" @default.
- W2016919782 cites W1499870879 @default.
- W2016919782 cites W1938165519 @default.
- W2016919782 cites W1966101832 @default.
- W2016919782 cites W1973190148 @default.
- W2016919782 cites W1973677690 @default.
- W2016919782 cites W1997444277 @default.
- W2016919782 cites W1999068577 @default.
- W2016919782 cites W2011160302 @default.
- W2016919782 cites W2016234945 @default.
- W2016919782 cites W2025617572 @default.
- W2016919782 cites W2041794561 @default.
- W2016919782 cites W2043219898 @default.
- W2016919782 cites W2045468346 @default.
- W2016919782 cites W2048988599 @default.
- W2016919782 cites W2055203083 @default.
- W2016919782 cites W2063541345 @default.
- W2016919782 cites W2067714902 @default.
- W2016919782 cites W2073310243 @default.
- W2016919782 cites W2073646596 @default.
- W2016919782 cites W2089237353 @default.
- W2016919782 cites W2095422531 @default.
- W2016919782 cites W2096018298 @default.
- W2016919782 cites W2096973404 @default.
- W2016919782 cites W2100756644 @default.
- W2016919782 cites W2113736505 @default.
- W2016919782 cites W2127160263 @default.
- W2016919782 cites W2129788952 @default.
- W2016919782 cites W2137664573 @default.
- W2016919782 cites W2139783705 @default.
- W2016919782 cites W2157340183 @default.
- W2016919782 cites W2166858952 @default.
- W2016919782 cites W2170441532 @default.
- W2016919782 cites W2412504878 @default.
- W2016919782 cites W2949995906 @default.
- W2016919782 doi "https://doi.org/10.1021/jm049530m" @default.
- W2016919782 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15771462" @default.
- W2016919782 hasPublicationYear "2005" @default.
- W2016919782 type Work @default.
- W2016919782 sameAs 2016919782 @default.
- W2016919782 citedByCount "61" @default.
- W2016919782 countsByYear W20169197822012 @default.
- W2016919782 countsByYear W20169197822013 @default.
- W2016919782 countsByYear W20169197822014 @default.
- W2016919782 countsByYear W20169197822015 @default.
- W2016919782 countsByYear W20169197822016 @default.
- W2016919782 countsByYear W20169197822017 @default.
- W2016919782 countsByYear W20169197822020 @default.
- W2016919782 countsByYear W20169197822021 @default.
- W2016919782 countsByYear W20169197822022 @default.
- W2016919782 crossrefType "journal-article" @default.
- W2016919782 hasAuthorship W2016919782A5000577175 @default.
- W2016919782 hasAuthorship W2016919782A5003290621 @default.
- W2016919782 hasAuthorship W2016919782A5004945278 @default.
- W2016919782 hasAuthorship W2016919782A5008465197 @default.
- W2016919782 hasAuthorship W2016919782A5012636274 @default.
- W2016919782 hasAuthorship W2016919782A5013375925 @default.
- W2016919782 hasAuthorship W2016919782A5024851679 @default.
- W2016919782 hasAuthorship W2016919782A5025403167 @default.
- W2016919782 hasAuthorship W2016919782A5026686512 @default.
- W2016919782 hasAuthorship W2016919782A5026919411 @default.
- W2016919782 hasAuthorship W2016919782A5027338053 @default.
- W2016919782 hasAuthorship W2016919782A5031917567 @default.
- W2016919782 hasAuthorship W2016919782A5041230347 @default.
- W2016919782 hasAuthorship W2016919782A5041737648 @default.
- W2016919782 hasAuthorship W2016919782A5044857121 @default.
- W2016919782 hasAuthorship W2016919782A5048051155 @default.
- W2016919782 hasAuthorship W2016919782A5050194203 @default.
- W2016919782 hasAuthorship W2016919782A5052413109 @default.
- W2016919782 hasAuthorship W2016919782A5057427778 @default.