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Literature summary for 3.4.21.98 extracted from

  • Kirschberg, T.A.; Squires, N.H.; Yang, H.; Corsa, A.C.; Tian, Y.; Tirunagari, N.; Sheng, X.C.; Kim, C.U.
    Novel, sulfonamide linked inhibitors of the hepatitis C virus NS3 protease (2014), Bioorg. Med. Chem. Lett., 24, 969-972.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-15-oxo-1,2,3,7,8,9,10,12a,13,14,15,15a-dodecahydrocyclopropa[f]pyrrolo[1,2-b][1,2,5]thiadiazacyclotetradecine-13a(6H)-carboxamide 5,5-dioxide most potent inhibitor of the series with sulfonamide linkage. The microsomally predicted clearance numbers is 0.17/0.7 L/h/kg (h/r) Hepacivirus C
(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-5,15-dioxo-1,2,3,5,6,7,8,9,10,12a,13,14,15,15a-tetradecahydro-13aH-cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclotetradecine-13a-carboxamide inhibitor with proline amide linkage, slightly more potent than inhibitors with sulfonamide linkage. The microsomally predicted clearance number is 0.17/0.82 L/h/kg (h/r) Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
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-
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000004
-
 pH not specified in the publication, temperature not specified in the publication Hepacivirus C (11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-5,15-dioxo-1,2,3,5,6,7,8,9,10,12a,13,14,15,15a-tetradecahydro-13aH-cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclotetradecine-13a-carboxamide
0.0000029
-
 pH not specified in the publication, temperature not specified in the publication Hepacivirus C (11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-15-oxo-1,2,3,7,8,9,10,12a,13,14,15,15a-dodecahydrocyclopropa[f]pyrrolo[1,2-b][1,2,5]thiadiazacyclotetradecine-13a(6H)-carboxamide 5,5-dioxide