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Tetrahydrothiophen-1,1-dioxides

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 [1, 2, 3] remedy (compounds 1-4), but also is included in drug candidates with anticoagulant and factor Xa inhibitor activities (compound 5) [4] and antineoplastic and signal transduction inhibitor activities (compound 6) [5].

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Drug candidates with analogous 1-(1,1-dioxidotetrahydrothien-3-yl)piperazine fragment (compounds 7, 8) have antineoplastic [6, 7], tyrosine - specific protein kinase inhibitor (compound 7) [6] and prostate disorders and LHRH antagonist (compound 8) [7] activities.

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Some other drug candidates with 3-amino-tetrahydrothiophen-1,1-dioxide motif included in bicyclic systems have antipsychotic activity (compounds 9, 10) [8, 9] and show potential as agents for chemical delivery system (compounds 10, 11) and substance dependency (compound 11) [9].

91011


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). Complete library could be downloaded here. 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.

EN300-08033 EN300-13006
EN300-13307 EN300-13060
EN400-14002 EN300-13178
EN300-08024 EN300-05512
EN300-08032 EN300-06886
EN300-09231 EN300-07743
EN300-07920 EN300-07925
EN300-10627 EN300-08670
EN300-07603 EN300-10414
EN300-07926 EN300-11080
EN300-09040 EN300-13032
EN300-10673 EN300-13183
EN300-12347 EN300-13187
EN300-13083 EN300-14271
EN300-05841 EN300-14663
EN300-07896 EN300-27131

 

[1] Astrazeneca; WO 0046199; 20000810
[2] Bristol-Myers; WO 0302542; 20030109
[3] Merck & Co.; WO 2005009949; 20050203
[4] Astrazeneca; WO 9729104; 970814
[5] Merck & Co.; WO 0441164; 20040521
[6] Merck & Co.; WO 0245652; 20020613
[7] Astrazeneca; WO 0418480; 20040304
[8] Eli Lilly; WO 1997018199; 19970522
[9] Eli Lilly; WO 2003104217; 20031218



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