90111-34-5Relevant academic research and scientific papers
COMPOUNDS AND THEIR USES AS MIF INHIBITORS
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Paragraph 0309, (2022/01/08)
The present invention provides compounds of Formula I which can be used as macrophage migration inhibitory factor (MIF) inhibitors; methods for the production of the compounds of the invention; pharmaceutical compositions comprising the compounds of the i
New Phenolic Compounds from the Roots of Lentil (Lens?culinaris)
?uchowski, Jerzy,Pecio, ?ukasz,Reszczyńska, Emilia,Stochmal, Anna
, p. 674 - 680 (2016/09/20)
While lentil (Lens?culinaris) seeds are phytochemically well characterized, very little is known about secondary metabolites from lentil roots. Our research on lentil roots led to isolation of five phenolic compounds and five group B soyasaponins. Their structures were established using NMR spectroscopy and mass spectrometry. Four phenolics have not been hitherto described in the literature: 4-O-β-d-glucopyranosyl-2-methoxybenzoic acid, (αS)-4,4′-di-O-β-d-glucopyranosyl-α,2′-dihydroxydihydrochalcone, (αS)-4′-O-β-d-glucopyranosyl-α,2′,4-trihydroxydihydrochalcone, and keto-2-hydroxyglycitein. The DPPH?radical-scavenging activity of the purified phenolic compounds was additionally evaluated.
CYP199A4 catalyses the efficient demethylation and demethenylation of para-substituted benzoic acid derivatives
Coleman, Tom,Chao, Rebecca R.,Bruning, John B.,De Voss, James J.,Bell, Stephen G.
, p. 52007 - 52018 (2015/06/25)
The cytochrome P450 enzyme CYP199A4, from Rhodopseudomonas palustris strain HaA2, can efficiently demethylate 4-methoxybenzoic acid via hemiacetal formation and subsequent elimination of formaldehyde. Oxidative demethylation of a methoxy group para to the carboxyl moiety is strongly favoured over reaction at one in the ortho or meta positions. Dimethoxybenzoic acids containing a para-methoxy group were also efficiently demethylated exclusively at the para position. The presence of additional methoxy substituents reduces the substrate binding affinity and the activity compared to 4-methoxybenzoic acid. The addition of the smaller hydroxy group to the ortho or meta positions or of a nitrogen heteroatom in the aromatic ring of the 4-methoxybenzoate skeleton was better tolerated by the enzyme and these analogues were also readily demethylated. There was no evidence of methylenedioxy ring formation with 3-hydroxy-4-methoxybenzoic acid, an activity which is observed with certain plant CYP enzymes with analogous substrates. CYP199A4 is also able to deprotect the methylenedioxy group of 3,4-(methylenedioxy)benzoic acid to yield 3,4-dihydroxybenzoic acid and formic acid. This study defines the substrate range of CYP199A4 and reveals that substrates without a para substituent are not oxidised with any significant activity. Therefore para-substituted benzoic acids are ideal substrate scaffolds for the CYP199A4 enzyme and will aid in the design of optimised probes to investigate the mechanism of this class of enzymes. They also allow an assessment of the potential of CYP199A4 for synthetic biocatalytic processes involving selective oxidative demethylation or demethenylation.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 94; 151, (2015/09/23)
This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
SUBSTITUTED 4-(1H-BENZIMIDAZOL-2-YL)[1,4]DIAZEPANES USEFUL FOR THE TREATMENT ALLERGIC DISEASES
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4] diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases
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, (2008/06/13)
The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Nonpeptide oxytocin antagonists: Potent, orally bioavailable analogs of L-371,257 containing A 1-R-(pyridyl)ethyl ether terminus
Kuo, Michelle S.,Bock, Mark G.,Freidinger, Roger M.,Guidotti, Maribeth T.,Lis, Edward V.,Pawluczyk, Joseph M.,Perlow, Debra S.,Pettibone, Douglas J.,Quigley, Amy G.,Reiss, Duane R.,Williams, Peter D.,Woyden, Carla J.
, p. 3081 - 3086 (2007/10/03)
Structure-activity studies on the oxytocin antagonist 1 (L-371,257) have identified a new series of high affinity, receptor-selective OT antagonists in which the N-acetyl-4-piperidinyl ether terminus in 1 has been replaced with a 1-(aryl)ethoxy group.
N-Tetrazolyl benzamides and anti-allergic use thereof
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, (2008/06/13)
Amides obtained by condensing aminotetrazole with optionally substituted ortho-alkoxybenzoic and ortho-methylthiobenzoic acids are potent anti-allergic agents.
