Structure-activity relationships for selected sulfur-rich antithrombotic compounds.
We assessed the antithrombotic activity of some simple organosulfur compounds which have some of the functionality found in the disulfide ajoene, a pharmacologically active compound isolated from garlic. The results establish that antithrombotic activity is associated with disulfides directly attached to a phenyl ring and is further enhanced by an alpha-sulfonyl group. CH(3)SO(2)CH(2)SSPh proved to be a potent inhibitor of platelet aggregation with an IC(50) of 5 microM.
MacDonald
J A
JA
Department of Pharmacology, Health Sciences Center, 1300 Jefferson Park Avenue, Charlottesville, Virginia 22908-0735, USA.
Langler
R F
RF
D004220:Disulfides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005343:Fibrinolytic Agents / Q000737:chemistry* / Q000494:pharmacology*; D005737:Garlic / Q000737:chemistry; D006801:Humans; D066298:In Vitro Techniques; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010946:Plants, Medicinal; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013454:Sulfoxides; D013455:Sulfur / Q000737:chemistry; D013917:Thrombin / Q000494:pharmacology
D004220:Disulfides; D005343:Fibrinolytic Agents; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; D013454:Sulfoxides; D013455:Sulfur; C048980:ajoene; D013917:Thrombin