Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 6, 2014, Pages 1615-1620

  Xiao, Dong ^a   Zhu, Xiaohong ^a   Yu, Younong ^a   Shao, Ning ^a   Wu, Jie ^a   McCormick, Kevin D ^a   Dhondi, Pawan ^a   Qin, Jun ^a   Mazzola, Robert ^a   Tang, Haiqun ^a   Rao, Ashwin ^a   Siliphaivanh, Phieng ^a   Qiu, Hongchen ^a   Yang, Xiaoxin ^a   Rivelli, Maria ^a   Garlisi, Charles G ^a   Eckel, Steve ^a   Mukhopadhyay, Gitali ^a   Correll, Craig ^a   Rindgen, Diane ^a   Aslanian, Robert ^a   Palani, Anandan ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Agonism antagonism switch; Amide isostere; Drug like properties; Isoxazolines; Quality by design (QbD)

Indexed keywords

AMIDE; CRTH2 ANTAGONIST; ISOXAZOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CHIRALITY; DISTRIBUTION VOLUME; DRUG CLEARANCE; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG SOLUBILITY; NONHUMAN; QUALITY BY DESIGN; QUALITY CONTROL; RAT; STRUCTURE ACTIVITY RELATION;

AGONISM/ANTAGONISM SWITCH; AMIDE ISOSTERE; CRTH(2) ANTAGONISTS; DRUG-LIKE PROPERTIES; ISOXAZOLINES; QUALITY BY DESIGN (QBD);

AMIDES; ANIMALS; DOGS; DRUG DESIGN; HALF-LIFE; HAPLORHINI; HUMANS; ISOXAZOLES; QUINAZOLINONES; RATS; RATS, WISTAR; RECEPTORS, IMMUNOLOGIC; RECEPTORS, PROSTAGLANDIN; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84895801226     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.01.043     Document Type: Article

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