Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 1, 2011, Pages 262-266

  Skerlj, Renato ^a   Bridger, Gary ^a   McEachern, Ernie ^a   Harwig, Curtis ^a   Smith, Chris ^a   Wilson, Trevor ^a   Veale, Duane ^a   Yee, Helen ^a   Crawford, Jason ^a   Skupinska, Krystyna ^a   Wauthy, Rossana ^a   Yang, Wen ^a   Zhu, Yongbao ^a   Bogucki, David ^a   Di Fluri, Maria ^a   Langille, Jonathon ^a   Huskens, Dana ^b   De Clercq, Erik ^b   Schols, Dominique ^b  

^a GENZYME CORPORATION   (United States)

^b REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

AMD070; Chemokine receptor; CXCR4; HIV

Indexed keywords

CHEMOKINE RECEPTOR CXCR4 ANTAGONIST;

ANTIVIRAL ACTIVITY; ARTICLE; CALCIUM SIGNALING; CALCIUM TRANSPORT; CELL MEDIATED CYTOTOXICITY; DOG; DRUG BIOAVAILABILITY; DRUG SYNTHESIS; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VIRUS REPLICATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-HIV AGENTS; CALCIUM SIGNALING; DOGS; HETEROCYCLIC COMPOUNDS, 1-RING; HIV-1; HUMANS; RATS; RECEPTORS, CXCR4; STRUCTURE-ACTIVITY RELATIONSHIP; VIRUS REPLICATION;

CANIS FAMILIARIS; HUMAN IMMUNODEFICIENCY VIRUS 1; RATTUS;

EID: 78650514584     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.023     Document Type: Article

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18. 3) δ 3.99 (s, 3H), 4.96 (s, 2H), 7.61 (d, 1H, J = 8.1 Hz), 7.77 (dd, 1H, J = 8.1, 1.8 Hz), 8.27 (d, 1H, J = 1.8 Hz).
19. 3) δ 1.74 (m, 10H), 1.99 (m, 2H), 2.29 (m, 1H), 2.74 (m, 2H), 3.86 (s, 3H), 4.22 (d, 1H, J = 17 Hz), 4.33 (m, 1H), 4.36 (d, 1H, J = 17 Hz), 4.59 (d, 1H, J = 14 Hz), 4.65 (d, 1H, J = 14 Hz), 6.98 (dd, 1H, J = 8.0, 4.7 Hz), 7.25 (m, 3H), 7.33 (dd, 1H, J = 8.1, 1.8 Hz), 7.50 (m, 1H), 7.68 (m, 2H), 8.11 (d, 1H, J = 8.1 Hz), 8.41 (m, 1H).
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