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Literature summary for 3.4.21.97 extracted from

  • Borthwick, A.D.; Angier, S.J.; Crame, A.J.; Exall, A.M.; Haley, T.M.; Hart, G.J.; Mason, A.M.; Pennell, A.M.; Weingarten, G.G.
    Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 1. The alpha-methyl-trans-lactam template (2000), J. Med. Chem., 43, 4452-4464.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
rel-(3aS,6R,6aR)-3-methyl-2-oxo-hexahydro-pyrrolo-[3,2-b]pyrrolo-1,4-dicarboxylic acid 4-benzyl ester 1-methyl ester 0.5 mM, 7.9% inhibition after 15 min Human betaherpesvirus 5
rel-(3aS,6R,6aR)-4-acetoxyacetyl-6-methyl-5-oxohexahydro-pyrrolo[3,2-b]pyrrolo-1-carboxylic acid benzyl ester IC50: 0.805 mM Human betaherpesvirus 5
rel-(3aS,6R,6aR)-4-acetyl-6-methyl-5-oxo-hexahydropyrrolo[3,2-b]pyrrole-1-carboxylic acid benzyl ester IC50: 1.8 mM, 0.5 mM, 15.4% inhibition after 15 min Human betaherpesvirus 5
rel-(3aS,6R,6aR)-4-methanesulfonyl-6-methyl-5-oxohexahydro-pyrrolo[3,2-b]pyrrole-1-carboxylic acid benzyl ester 0.5 mM, 15% inhibition after 15 min Human betaherpesvirus 5
trans-2-oxo-hexahydro-pyrrolo[3,2-b]pyrrolo-1,4-dicarboxylic acid 4-benzyl ester 1 tert butyl ester 0.5 mM, 6.3% inhibition after 15 min Human betaherpesvirus 5

Organism

Organism UniProt Comment Textmining
Human betaherpesvirus 5
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.805
-
 IC50: 0.805 mM Human betaherpesvirus 5 rel-(3aS,6R,6aR)-4-acetoxyacetyl-6-methyl-5-oxohexahydro-pyrrolo[3,2-b]pyrrolo-1-carboxylic acid benzyl ester
1.8
-
 IC50: 1.8 mM, 0.5 mM, 15.4% inhibition after 15 min Human betaherpesvirus 5 rel-(3aS,6R,6aR)-4-acetyl-6-methyl-5-oxo-hexahydropyrrolo[3,2-b]pyrrole-1-carboxylic acid benzyl ester