69182-96-3Relevant academic research and scientific papers
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity
Yadav, Rakesh,Bansal, Ranju,Kachler, Sonja,Klotz
, p. 327 - 335 (2014/03/21)
A new series of 8-(p-substituted-phenyl/benzyl)xanthines has been synthesized and evaluated in vitro for adenosine receptor binding affinity and in vivo for bronchospasmolytic effects. It was observed that the nature of substituent at para-position of 8-phenyl/benzyl group on the xanthine scaffold remarkably affects the binding affinity and selectivity of xanthine derivatives for various adenosine receptor subtypes and also their bronchospasmolytic effects. Newly synthesized 8-phenylxanthines displayed potent binding affinity and significant selectivity for A2A receptors and also produced potent bronchospasmolytic effects. Replacement of phenyl ring with benzyl moiety at C8 of xanthine skeleton resulted in notable reduction in adenosine receptor affinity and broncholytic effects.
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor
Bowers, Simeon,Truong, Anh P.,Neitz, R. Jeffrey,Neitzel, Martin,Probst, Gary D.,Hom, Roy K.,Peterson, Brian,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.,Tóth, Gergley,Pan, Hu,Yao, Nanhua,Artis, Dean R.,Brigham, Elizabeth F.,Quinn, Kevin P.,Sauer, John-Michael,Powell, Kyle,Ruslim, Lany,Ren, Zhao,Bard, Frédérique,Yednock, Ted A.,Griswold-Prenner, Irene
scheme or table, p. 1838 - 1843 (2011/05/05)
The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the 4-position of the thiophene we obtained single digit nanomolar compounds, such as 47, which demonstrated an in vivo effect on JNK activity when dosed orally in our kainic acid mouse model as measured by phospho-c-jun reduction.
INHIBITORS OF JUN N-TERMINAL KINASE
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Page/Page column 121, (2010/08/18)
The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.
Synthesis and biological evaluation of phenylacetyl derivatives having low central nervous system permeability as potent and selective M2 muscarinic receptor antagonists
Watanabe, Toshihiro,Kakefuda, Akio,Tanaka, Akihiro,Takizawa, Kenji,Hirano, Seiko,Shibata, Hiroshi,Yamagiwa, Yoko,Yanagisawa, Isao
, p. 53 - 68 (2007/10/03)
A series of phenylacetyl derivatives containing the 5,10-dihydro-11H- dibenzo[b,e][1,4]diazepin-11-one or 5,11-dihydro-6H-pyrido[2,3- b][1,4]benzodiazepin-6-one skeleton was prepared and evaluated for their binding affinities to muscarinic receptors in vitro and for antagonism of bradycardia, salivation and tremor in vivo. Among them, compounds 56 and 66 had high affinity for M2 muscarinic receptors in the heart (pK(i) = 8.7 and 8.9, respectively) with low affinity for M3 muscarinic receptors in the submandibular gland. A structure-activity relationship (SAR) study suggested that the high M2 selectivity over the M3 muscarinic receptors of 56 may be attributed to the direction of the carboxamide carbonyl group. In in vivo studies, 56 and 66 antagonized oxotremorine-induced bradycardia in rats on both intravenous and oral administration, and their heart rate increasing effect in dogs with nocturnal bradycardia was about 3-fold greater than that of AF-DX 116. Furthermore, they had almost no influence on oxotremorine- induced tremor in mice, presenting no evidence of central transfer.
Synthesis and Antiallergy Activity of 4-(Diarylhydroxymethyl)-1-piperidines and Structurally Related Compounds
Walsh, David A.,Franzyshen, Stephen K.,Yanni, John M.
, p. 105 - 118 (2007/10/02)
A series of 4-(diarylhydroxymethyl)-1-piperidines was synthesized and evaluated for antiallergy activity.Several analogues had potent activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity.In particular 1--1-piperidinyl>propoxy>-3-methoxyphenyl>ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.
Synthesis of Amino Derivatives of 5-Aralkylidene-3-pyrrolin-2-ones
Adembri, G.,Anselmi, C.,Camparini, A.,Rossetti, M. G.,Scotton, M.
, p. 1019 - 1022 (2007/10/02)
Preparation of some derivatives of 5-aralkylidene-3-pyrrolin-2-ones is reported.Compounds with an amino group on the phenyl ring at the 3-position of the pyrrolinone ring showed suitable properties as potential UV-A filters.Some of the compounds were quat
