title: Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.
abstract: 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.
authors.affiliation: Medicinal and Combinatorial Chemistry Laboratory, Institute of Molecular and Cell Biology, Singapore.
authors.forename: W T
authors.initials: WT
authors.lastname: Sing
authors.forename: C L
authors.initials: CL
authors.lastname: Lee
authors.forename: S L
authors.initials: SL
authors.lastname: Yeo
authors.forename: S P
authors.initials: SP
authors.lastname: Lim
authors.forename: M M
authors.initials: MM
authors.lastname: Sim
mesh_terms: 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
chemical_list: 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