23459-38-3Relevant academic research and scientific papers
A JAK/STAT3 phosphorylation inhibitor and its preparation method and use thereof
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Paragraph 0050, (2017/06/02)
The invention provides a JAK/STAT3 phosphorylation inhibitor as well as a preparation method and application thereof. The structural formula of the JAK/STAT3 phosphorylation inhibitor is as shown in a formula I, wherein X is selected from S or O; Y and Z
Substituted pteridines for the treatment of inflammatory diseases
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Page/Page column 6, (2010/11/08)
The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as
Influence of bulky substituents on histamine H3 receptor agonist/antagonist properties
Sasse, Astrid,Ligneau, Xavier,Rouleau, Agnès,Elz, Sigurd,Ganellin, C. Robin,Arrang, Jean-Michel,Schwartz, Jean-Charles,Schunack, Walter,Stark, Holger
, p. 4000 - 4010 (2007/10/03)
Novel derivatives of 3-(1H-imidazol-4-yl)propanol were designed on the basis of lead compounds belonging to the carbamate or ether series possessing (partial) agonist properties on screening assays of the histamine H3 receptor. One pair of enantiomers in the series of α-methyl-branched chiral carbamates was stereoselectively prepared in high optical yields. Enantiomeric purity was checked by Mosher amide derivatives of precursors and capillary electrophoresis of the final compounds with trimethyl-β-cyclodextrin as chiral selector, and was determined to be ≥95%. The novel compounds were investigated in various histamine H3 receptor assays in vitro and in vivo. Some compounds displayed partial agonist activity on synaptosomes of rat brain cortex, whereas others exhibited antagonist properties only. Selected compounds were investigated in [125I]iodoproxyfan binding studies on the human histamine H3 receptor and showed high affinity in the nanomolar concentration range. Under in vivo conditions after oral administration to mice, some of the compounds exhibited partial or full agonist activity in the brain at low dosages. The (S)-enantiomer of one pair of chiral carbamates (9) proved to be the eutomer; thus, the (S)-enantiomer was selected for further pharmacological studies. In a peripheral in vivo test model in rats, measuring the level of inhibition of capsaicin-induced plasma extravasation, (S)-9 again proved its high oral agonist potency with full intrinsic activity (ED50 values of 0.07-0.1 mg/kg depending on tissue).
Branched alkylamino derivatives of thiazole, processes for preparing them and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to the derivatives of formula I: STR1 in which R1 represents a phenyl or naphthyl radical (optionally substituted), R2 represents a hydrogen or halogen atom or an alkyl, hydroxymethyl or formyl radical, R3
Hypoglycemic α cycloalkylphenylmethyl, furanalkyl, and thiophenealkyl lactamimides
Grisar,Claxton,Wiech
, p. 365 - 369 (2007/10/04)
A series of α cycloalkylphenylmethyl lactamimides and a series of furan and thiophenealkyl lactamimides were prepared for biological evaluation as an extension of earlier findings of hypoglycemic activity in lactamimides. Several compounds produced pronouced hypoglycemia after oral administration to fasted, glucose primed rats.
