跳转至内容

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

摘要

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.

材料

货号

品牌

产品描述

Sigma-Aldrich

苯甲酸, ACS reagent, ≥99.5%

Sigma-Aldrich

水杨酸, ACS reagent, ≥99.0%

Sigma-Aldrich

水杨酸, ≥99%, FG

Sigma-Aldrich

水杨酸, BioXtra, ≥99.0%

Sigma-Aldrich

苯甲酸, ≥99.5%, FCC, FG

Sigma-Aldrich

水杨酸, suitable for plant cell culture

Supelco

Mettler-Toledo 校准物质 ME 18555，苯甲酸, analytical standard, (for the calibration of the melting point system), traceable to primary standards (LGC)

Sigma-Aldrich

苯甲酸, ReagentPlus^®, 99%

Supelco

Melting point standard 121-123°C, analytical standard

Sigma-Aldrich

苯甲酸, meets analytical specification of Ph. Eur., BP, USP, FCC, E210, 99.5-100.5% (alkalimetric)

Sigma-Aldrich

苯甲酸, natural, ≥99.5%, FCC, FG

Supelco

苯甲酸, reference material for titrimetry, certified by BAM, >99.5%

Sigma-Aldrich

水杨酸, puriss. p.a., ≥99.0% (T)

Sigma-Aldrich

水杨酸, meets analytical specification of Ph. Eur., BP, USP, 99.5-100.5% (calc. to the dried substance)

Sigma-Aldrich

水杨酸, ReagentPlus^®, ≥99%

Sigma-Aldrich

苯甲酸, puriss. p.a., ACS reagent, reag. Ph. Eur., ≥99.9% (alkalimetric)

Sigma-Aldrich

苯甲酸, purified by sublimation, ≥99%

Supelco

苯甲酸, Standard for quantitative NMR, TraceCERT^®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland

Supelco

水杨酸, certified reference material, TraceCERT^®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland