Recently 3-amino-tetrahydrothiophen-1,1-dioxides have drawn significant attention of a major drug developers. A few publications have been released earlier, corroborating rather high potential of this pharmacophoric moiety.
3-Amino-tetrahydrothiophen-1,1-dioxide fragment incorporated into drug candidates have promising effects as antiarthritic remedy (compounds 1-4), but also is included in drug candidates with anticoagulant and factor Xa inhibitor activities (compound 5) and antineoplastic and signal transduction inhibitor activities (compound 6).
Drug candidates with analogous 1-(1,1-dioxidotetrahydrothien-3-yl)piperazine fragment (compounds 7, 8) have antineoplastic, tyrosine - specific protein kinase inhibitor (compound 7) and prostate disorders and LHRH antagonist (compound 8) activities.
Some other drug candidates with 3-amino-tetrahydrothiophen-1,1-dioxide motif included in bicyclic systems have antipsychotic activity (compounds 9, 10) and show potential as agents for chemical delivery system (compounds 10, 11) and substance dependency (compound 11).
Enamine provides library of best-selling Building Blocks with tetrahydrothiophen-1,1-dioxide motif (and particularly 3-amino-tetrahydrothiophen-1,1-dioxides) for use in drug discovery (please refer to example structures below). Compounds are in stock and can be supplied promptly, follow-up and re-supply services are available. Diverse libraries of derivatives of the following reagents are also available from stock upon request.