- 8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters (2007-10-13)
Thorsten E Fisher, Boyoung Kim, Donnette D Staas, Terry A Lyle, Steven D Young, Joseph P Vacca, Matthew M Zrada, Daria J Hazuda, Peter J Felock, William A Schleif, Lori J Gabryelski, M Reza Anari, Christopher J Kochansky, John S Wai
PMID17931865
ABSTRACT
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 12 is active against replication of HIV-1 in cell culture with a CIC(95) of 0.31microM. Further SAR exploration led to the preparation of pseudosymmetrical tricyclic pyrrolopyrazine inhibitors 23 and 24 with further improvement in antiviral activity.
MATERIALS
Product Number
Brand
Product Description
Supelco
Salicylic acid, certified reference material, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland
Sigma-Aldrich
Salicylic acid, meets analytical specification of Ph. Eur., BP, USP, 99.5-100.5% (calc. to the dried substance)
Supelco
Mettler-Toledo Calibration substance ME 18555, Benzoic acid, analytical standard, (for the calibration of the melting point system), traceable to primary standards (LGC)
Sigma-Aldrich
Benzoic acid, meets analytical specification of Ph. Eur., BP, USP, FCC, E210, 99.5-100.5% (alkalimetric)
Supelco
Benzoic acid, Standard for quantitative NMR, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland