8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 23, 2007, Pages 6511-6515

  Fisher, Thorsten E ^a   Kim, Boyoung ^a   Staas, Donnette D ^a   Lyle, Terry A ^a   Young, Steven D ^a   Vacca, Joseph P ^a   Zrada, Matthew M ^a   Hazuda, Daria J ^a   Felock, Peter J ^a   Schleif, William A ^a   Gabryelski, Lori J ^a   Anari, M Reza ^a   Kochansky, Christopher J ^a   Wai, John S ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antiviral; HIV; Integrase inhibitor

Indexed keywords

8 HYDROXY 3,4 DIHYDROPYRROLO[1,2 A]PYRAZINE 1(2H) ONE; INTEGRASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG INHIBITION; DRUG POTENCY; DRUG STRUCTURE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; VIRUS REPLICATION;

CELL LINE, TUMOR; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HUMANS; PYRAZINES; T-LYMPHOCYTES;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 35648967035     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.09.086     Document Type: Article

References (21)

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19. 95) are defined as those which inhibited by ≥ 95% the spread of HIV-1 infection in susceptible cell culture. MT-4 human T-lymphoid cells were maintained in RPMI 1640 medium containing 10% heat inactivated fetal bovine serum. Cells were infected en masse at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24 h. At this time, cells were washed and distributed into 96 well microtiter dishes. Serial two-fold dilutions of inhibitor were added to the wells and the cultures were maintained for three additional days. Virus spread was assessed by HIV-1 p24 core antigen ELISA. Control cultures in the absence of inhibitor were fully infected at 4 days
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