23304-48-5Relevant articles and documents
Structure-guided design of new indoles as negative allosteric modulators (NAMs) of N-methyl-d-aspartate receptor (NMDAR) containing GluN2B subunit
Buemi, Maria Rosa,De Luca, Laura,Ferro, Stefania,Russo, Emilio,De Sarro, Giovambattista,Gitto, Rosaria
, p. 1513 - 1519 (2016)
Negative allosteric modulators (NAMs) of GluN2B-containing NMDARs provide pharmacological tools for the treatment of chronic neurodegenerative diseases. Novel NAMs have been designed on the basis of computational studies focused on the 'hit compound' 3. This series of indoles has been tested in competition assay. Compounds 16 and 17 were the most active ligands (IC50 values of 83 nM and 71 nM, respectively) and they showed a potency close to that of reference compounds ifenprodil (1, IC50 = 47 nM) and 3 (IC50 = 25 nM). Furthermore, docking studies have been performed for active ligand 16 and the results were in a good agreement with biological data.
(phenoxy)alkoxy-1H-indole derivatives or pharmaceutically acceptable salts thereof, preparation method therof and pharmaceutical composition for use in preventing or treating PPARα, PPARγ and PPARδ related diseases containing the same as an active ingredient
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Paragraph 0257-0258, (2017/08/10)
The present invention relates to (phenoxy)alkoxy-1H-indole derivatives or pharmaceutically allowable salts thereof, to a manufacturing method thereof, and to a pharmaceutical composition for preventing or treating PPARandalpha;, PPARandgamma; and PPARanddelta;-related diseases comprising the derivatives or salt thereof as an active ingredient. The (phenoxy)alkoxy-1H-indole derivatives have excellent abilities of activating PPARandalpha;, PPARandgamma; and PPARanddelta;, thereby being used for preventing or treating PPARandalpha;, PPARandgamma; and PPARanddelta;-related diseases of metabolic diseases, cardiovascular system diseases, cancer, inflammation, etc. as a PPAR agonist.COPYRIGHT KIPO 2017
Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists We dedicate this article to Professor Young-Ger Suh on the occasion of his retirement.
Gim, Hyo Jin,Li, Hua,Jeong, Ji Hye,Lee, Su Jeong,Sung, Mi-Kyung,Song, Mi-Young,Park, Byung-Hyun,Oh, Soo Jin,Ryu, Jae-Ha,Jeon, Raok
, p. 3322 - 3336 (2015/08/03)
Abstract A series of alkoxy-3-indolylacetic acid analogs has been discovered as peroxisome proliferator-activated receptor (PPAR) agonists. Structure-activity relationship study indicated that PPARα/γ/δ activities were dependent on the nature of the hydrophobic group, the attachment position of the alkoxy linker to the indole ring, and N-alkylation of indole nitrogen. Some compounds presented significant PPARγ/δ activity and molecular modeling suggested their putative binding modes in the ligand binding domain of PPARγ. Of these, compound 51 was selected for in vivo study via an evaluation of microsomal stability in mouse and human liver. Compound 51 lowered the levels of fasting blood glucose, insulin, and HbA1c without gain in body weight in db/db mice. When compound 51 was treated, hepatic triglycerides level and the size of adipocytes in white adipose tissue of db/db mice were also reduced as opposed to treatment with rosiglitazone. Taken together, compound 51 shows high potential warranting further studies in models for diabetes and related metabolic disorders and may be in use as a chemical tool for the understanding of PPAR biology.
