Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.
Arylalkylidene rhodanines 2(a-d) inhibit HCV NS3 protease at moderate concentrations. They are better inhibitors of other serine proteases such as chymotrypsin and plasmin. However, the selectivity of arylmethyliden e rhodanines (8a, 9a) with bulkier and more hydrophobic functional groups increases by 13- and 25-fold towards HCV NS3 protease respectively.
Sing
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WT
Medicinal and Combinatorial Chemistry Laboratory, Institute of Molecular and Cell Biology, Singapore.
Lee
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CL
Yeo
S L
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Lim
S P
SP
Sim
M M
MM
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry; D002918:Chymotrypsin / Q000378:metabolism; D020650:Combinatorial Chemistry Techniques; D005341:Fibrinolysin / Q000378:metabolism; D006526:Hepatitis C / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D012236:Rhodanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases
D000998:Antiviral Agents; D002918:Chymotrypsin; D005341:Fibrinolysin; D012236:Rhodanine; D015842:Serine Proteinase Inhibitors; D017361:Viral Nonstructural Proteins; C084422:NS3 protein, hepatitis C virus; D012697:Serine Endopeptidases; D043583:Nucleoside-Triphosphatase; D053487:DEAD-box RNA Helicases; D000085242:Viral Proteases