- Rational Design of Potent and Selective Inhibitors of an Epoxide Hydrolase Virulence Factor from Pseudomonas aeruginosa
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The virulence factor cystic fibrosis transmembrane conductance regulator (CFTR) inhibitory factor (Cif) is secreted by Pseudomonas aeruginosa and is the founding member of a distinct class of epoxide hydrolases (EHs) that triggers the catalysis-dependent
- Kitamura, Seiya,Hvorecny, Kelli L.,Niu, Jun,Hammock, Bruce D.,Madden, Dean R.,Morisseau, Christophe
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p. 4790 - 4799
(2016/06/13)
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- Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor β (TR-β) selective ligands
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Design and synthesis of a novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives are reported and their in vitro thyroid hormone receptor selectivity has been evaluated in the thyroid luciferase receptor assay. The 3-[3,5-dichloro-4-(4-hydroxy-3-isopropylph
- Raval, Saurin,Raval, Preeti,Bandyopadhyay, Debdutta,Soni, Krunal,Yevale, Digambar,Jogiya, Digvijay,Modi, Honey,Joharapurkar, Amit,Gandhi, Neha,Jain, Mukul R.,Patel, Pankaj R.
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scheme or table
p. 3919 - 3924
(2009/04/07)
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- Thyroid receptor ligands. Part 5: Novel bicyclic agonist ligands selective for the thyroid hormone receptor β
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Based on the examination of the crystal structure of rat TRβ complexed with 3,5,3′-triiodo-l-thyronine (2) a novel TRβ-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TRβ over TRα in bi
- Garcia Collazo, Ana-Maria,Koehler, Konrad F.,Garg, Neeraj,Faernegardh, Mathias,Husman, Bolette,Ye, Liu,Ljunggren, Jan,Mellstroem, Karin,Sandberg, Johnny,Grynfarb, Marlena,Ahola, Harri,Malm, Johan
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p. 1240 - 1244
(2007/10/03)
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- Synthesis and Structure-Activity Relationships of Oxamic Acid and Acetic Acid Derivatives Related to L-Thyronine
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Aryloxamic acids 7 and 23, (arylamino)acetic acids 29, arylpropionic acids 33, arylthioacetic acids 37, and (aryloxy)acetic acid 41 related to L-triiodothyronine (L-T3) were prepared and tested in vitro for binding to the rat liver nuclear L-T
- Yokoyama, Naokata,Walker, Gordon N.,Main, Alan J.,Stanton, James L.,Morrissey, Michael M.,et al.
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p. 695 - 707
(2007/10/02)
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- Heteroacetic acid derivatives
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Disclosed are compounds of formula STR1 wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 is halogen, trifluoromethyl or lower alkyl; R2 is halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; or R3 is the radical STR2 wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 represents hydrogen or lower alkyl; or R9 and R10 together represent oxo; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; X is --NR7, S or O; W is O or S; R5 represents hydrogen, lower alkyl or aryl-lower alkyl;and R6 represents hydrogen; or R5 and R6 together represent oxo provided that X represents --NR7; R7 represents hydrogen or lower alkyl; Z represents carboxyl, carboxyl derivatized as a pharmaceutically acceptable ester or as a pharmaceutically acceptable amide; and pharmaceutically acceptable salts thereof; which are useful as hypocholesteremic agents.
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