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Volumn 1, Issue 1, 2010, Pages 14-18

Discovery of a potent and orally bioavailable CCR2 and CCR5 dual antagonist

Author keywords

CCR2; CCR5; chemokine; dual antagonist

Indexed keywords

CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR2; CHEMOKINE RECEPTOR CCR2 ANTAGONIST; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CCR5 ANTAGONIST; DELAYED RECTIFIER POTASSIUM CHANNEL; PIPERIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 77956621678     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml900009d     Document Type: Article
Times cited : (37)

References (34)
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    • The Merck process chemistry group devised a synthesis of the (4 R)-carboxyphenyl-(3 S)-methyl piperidine subunit starting from pure methyl (S)-(+)-3-hydroxy-2-methylpropionate. They also devised a synthesis of the cis -(3 R,1 S)-cyclopentane core also using starting materials of known absolute stereochemistry. This improved synthesis will be described elsewhere.
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    • note
    • 1/2 of 5 h at 37 °C for CCR2.
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    • note
    • Compound 22 was dosed orally in 5 rhesus at 2 mg/kg and plasma concentration of 22 and MCP-1 whole blood monocyte shape change was determined at various time points postdosing (6, 24, 36, 48, 72 h). % inhibition shape change was determined by comparing postdose values to predose values in the same animals. See also ref 32.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.