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).

1 2
3 4
5 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.

7 8

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).

9 10 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.


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