264254-47-9Relevant academic research and scientific papers
4-aryl-1-oxa-9-thia-cyclopenta (b) fluorenes
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Page column 19, (2008/06/13)
This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1is hydrogen, alkyl of 1-6 carbon atoms, —CH
Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes
Wrobel, Jay,Li, Zenan,Sredy, Janet,Sawicki, Diane R.,Seestaller, Laura,Sullivan, Donald
, p. 1535 - 1538 (2007/10/03)
Novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes were designed, synthesized, and evaluated as inhibitors of the protein tyrosine phosphatase, PTP1B. Compounds 3 (IC50 = 284 nM) and 4 (IC50 = 74 nM), showed nanomolar potency against PTP1B (TRDI(P)YETD(P)YRK as substrate). Compound 4 also lowered insulin in the diabetic ob/ob mouse at a dose of 10 mg/kg/day, po. (C) 2000 Elsevier Science Ltd. All rights reserved.
4-aryl-1-oxa-9-thia-cyclopenta[b]fluorenes
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, (2008/06/13)
This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, -CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; R1 is hydrogen, alkyl of 1-6 carbon atoms, -CH(R2)W, -C(CH3)2CO2R3, 5-thiazolidine-2,4-dione, -CH(R4)CH2CO2R3, -COR3, or -PO3(R3)2; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, -CH2(1H-imidazol-4-yl), -CH2(3-1H-indolyl), -CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), -CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or -CH2(3-pyridyl); W is -CO2R3, -CONH2, -CONHOH, -CN, CONH(CH2)2CN, 5-tetrazole, or -PO3(R3)2; R3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
