Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. the impact of physicochemical properties on ADME and PK

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7429-7434

  Tanis, Steven P ^a   Plewe, Michael B ^a   Johnson, Ted W ^a   Butler, Scott L ^b   Dalvie, Deepak ^a   Delisle, Dorothy ^a   Dress, Klaus R ^a   Hu, Qiyue ^a   Huang, Buwen ^a   Kuehler, Jon E ^a   Kuki, Atsuo ^a   Liu, Wen ^a   Peng, Qinghai ^a   Smith, Graham L ^a   Solowiej, Jim ^a   Tran, Khanh T ^a   Wang, Hai ^a   Yang, Anle ^a   Yin, Chunfeng ^a   Yu, Xiaoming ^a   Zhang, Junhu ^a   Zhu, Huichun ^a   more..

^a PFIZER INC   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

ADME; Antiviral; Azaindole hydroxamates; HIV integrase; LipE; Log D; Physicochemical parameters; PK

Indexed keywords

AZAINDOLE N METHYL HYDROXAMIC ACID DERIVATIVE; ELVITEGRAVIR; GSK 1349572; INTEGRASE INHIBITOR; RALTEGRAVIR; UNCLASSIFIED DRUG;

AEROBIC METABOLISM; ANTIVIRAL ACTIVITY; ARTICLE; CYTOTOXICITY; DRUG STABILITY; GLUCURONIDATION; HUMAN; NONHUMAN; PHYSICAL CHEMISTRY;

ADMINISTRATION, ORAL; ANIMALS; DOGS; HALF-LIFE; HEPATOCYTES; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV-1; HUMANS; HYDROXAMIC ACIDS; INDOLES; STRUCTURE-ACTIVITY RELATIONSHIP;

CANIS FAMILIARIS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 78449293310     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.022     Document Type: Article

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