alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists.

alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists. Research Abstract Details 

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alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists. Abstract Text:

Michael R Wood,Kathy M Schirripa,June J Kim,Scott D Kuduk,Ronald K Chang,Christina N Di Marco,Robert M DiPardo,Bang-Lin Wan,Kathy L Murphy,Richard W Ransom,Raymond S L Chang,Marie A Holahan,Jacquelynn J Cook,Wei Lemaire,Scott D Mosser,Rodney A Bednar,Cuyue Tang,Thomayant Prueksaritanont,Audrey A Wallace,Qin Mei,Jian Yu,Dennis L Bohn,Frank C Clayton,Emily D Adarayn,Gary R Sitko,Yvonne M Leonard,Roger M Freidinger,Douglas J Pettibone,Mark G Bock,Michael R Wood,Kathy M Schirripa,June J Kim,Scott D Kuduk,Ronald K Chang,Christina N Di Marco,Robert M Dipardo,Bang-Lin Wan,Kathy L Murphy,Richard W Ransom,Raymond S L Chang,Marie A Holahan,Jacquelynn J Cook,Wei Lemaire,Scott D Mosser,Rodney A Bednar,Cuyue Tang,Thomayant Prueksaritanont,Audrey A Wallace,Qin Mei,Jian Yu,Dennis L Bohn,Frank C Clayton,Emily D Adarayn,Gary R Sitko,Yvonne M Leonard,Roger M Freidinger,Douglas J Pettibone,Mark G Bock,

Antagonism of the bradykinin B(1) receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating alpha-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B(1) receptor and good bioavailability in the rat and dog. In addition, these functionally active compounds show high passive permeability and low susceptibility to phosphoglycoprotein mediated efflux, predictive of good CNS exposure.

alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists. Publishing Authors By Initials

MR Wood,KM Schirripa,JJ Kim,SD Kuduk,RK Chang,CN Di Marco,RM DiPardo,BL Wan,KL Murphy,RW Ransom,RS Chang,MA Holahan,JJ Cook,W Lemaire,SD Mosser,RA Bednar,C Tang,T Prueksaritanont,AA Wallace,Q Mei,J Yu,DL Bohn,FC Clayton,ED Adarayn,GR Sitko,YM Leonard,RM Freidinger,DJ Pettibone,MG Bock,MR Wood,KM Schirripa,JJ Kim,SD Kuduk,RK Chang,CN Di Marco,RM Dipardo,BL Wan,KL Murphy,RW Ransom,RS Chang,MA Holahan,JJ Cook,W Lemaire,SD Mosser,RA Bednar,C Tang,T Prueksaritanont,AA Wallace,Q Mei,J Yu,DL Bohn,FC Clayton,ED Adarayn,GR Sitko,YM Leonard,RM Freidinger,DJ Pettibone,MG Bock,

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alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 716-20

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 19

MONTH: 11

YEAR: 2007

alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists.

AFFILIATION: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA.

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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• alpha-Hydroxy amides as a novel class of bradykinin B(1) selective antagonists.