40843-78-5Relevant articles and documents
ANTIDIABETIC OXAZOLIDINEDIONES AND THIAZOLIDINEDIONES
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Page/Page column 34, (2010/11/25)
Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia
FUSED AROMATIC COMPOUNDS HAVING ANTI-DIABETIC ACTIVITY
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Page/Page column 39, (2010/11/23)
Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obes
PROCESS FOR THE PRODUCTION OF ANTIDIABETIC OXAZOLIDINEDIONES
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Page/Page column 8; 10, (2008/06/13)
The present invention provides a convergent process for the preparation of a family of antidiabetic phenoxy-substituted phenoxybenzyl oxazolidinediones shown as structure I. The compounds are selective PPAR gamma partial agonists (SPPARM's), which are use
Selective displacement of aryl fluorides with hydroquinone: Synthesis of 4-phenoxyphenols
Marcune, Benjamin F.,Hillier, Michael C.,Marcoux, Jean-Fran?ois,Humphrey, Guy R.
, p. 7823 - 7826 (2007/10/03)
The selective displacement of a variety of aryl fluorides with hydroquinone has been achieved to give substituted 4-phenoxyphenols 3. In some cases the addition of 18-crown-6 resulted in a significant rate enhancement, and the reactions could be carried out at lower temperature. One of these derivatives, 3a (X = Cl) was converted to 2-propyl-4-(4-chlorophenoxy)phenol 2a, a precursor to the PPARγ receptor agonist 1.
ANTIDIABETIC OXAZOLIDINEDIONES AND THIAZOLIDINEDIONES
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Page/Page column 30, (2010/02/13)
Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones of formula (I) are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well
5-Aryl thiazolidine-2,4-diones as selective PPARγ agonists
Koyama, Hiroo,Boueres, Julia K.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,Miller, Daniel J.,Tolman, Richard L.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 1801 - 1804 (2007/10/03)
A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.
5-Aryl thiazolidine-2,4-diones: Discovery of PPAR dual α/γ agonists as antidiabetic agents
Desai, Ranjit C.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 2795 - 2798 (2007/10/03)
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARα/γ agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.
Structure-activity relationship of new growth inhibitors of Trypanosoma cruzi
Cinque, Güendalina M.,Szajnman, Sergio H.,Zhong, Li,Docampo, Roberto,Schvartzapel, Andrea J.,Rodriguez, Juan B.,Gros, Eduardo G.
, p. 1540 - 1554 (2007/10/03)
Several drugs bearing the 4-phenoxyphenoxy skeleton and other closely related structures were designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the etiologic agent of Chagas' disease. The new class of drugs was envisioned by modifying the nonpolar 4-phenoxyphenoxy moiety replacing selected aromatic protons by different groups via electrophilic aromatic substitution reactions as well as introducing a sulfur atom at file polar extreme. Of the designed compounds, sulfur-containing derivatives were shown to be potent antireplicative agents against T. cruzi. Among these drugs, 4-phenoxyphenoxyethyl thiocyanate (compound 56) proved to be an extremely active growth inhibitor of the epimastigote forms of T. cruzi and displayed an IC500 of 2.2 μM. Under the same assay conditions, this drug was much more active than Nifurtimox, one of the drugs currently in clinical use to control this disease. This thiocyanate derivative was also a very active inhibitor against the intracellular form of the parasite at the nanomolar level. Other sulfur derivatives prepared also exhibited very potent antiproliferative action against T. cruzi. The presence of a sulfur atom at the polar extreme for this family of compounds seems to be very important for biological action because this atom was always associated with high inhibition values. 4-Phenoxyphenoxyethyl thiocyanate presents very good prospective not only as a lead drug but also as a potential chemotherapeutic agent.