1782-38-3Relevant academic research and scientific papers
IDO inhibitors
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Page/Page column 328; 331; 332, (2018/09/02)
Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
Chiral integrated catalysts composed of bifunctional thiourea and arylboronic acid: Asymmetric aza-Michael addition of α,β-unsaturated carboxylic acids
Hayama, Noboru,Azuma, Takumi,Kobayashi, Yusuke,Takemoto, Yoshiji
, p. 704 - 717 (2016/07/19)
The first intermolecular asymmetric Michael addition of nitrogen-nucleophiles to α,β-unsaturated carboxylic acids was achieved through a new type of arylboronic acid equipped with chiral aminothiourea. The use of BnONH2 as a nucleophile gives a range of enantioenriched β-(benzyloxy)amino acid derivatives in good yields and with high enantioselectivity (up to 90% yield, 97% enantiomeric excess (ee)). The obtained products are efficiently converted to optically active β-amino acid and 1,2-diamine derivatives.
2-[(arylmethoxy)imino]imidazolidines with potential biological activities
Saczewski, Jaroslaw,Hudson, Alan L.,Rybczynska, Apolonia
experimental part, p. 671 - 680 (2010/07/04)
A series of 2-[(arylmethoxy)imino]imidazolidines was synthesized by reacting 2-chloro-4,5-dihydroimidazole with corresponding O- arylmethylhydroxylamines and evaluated for their α1-, α2-adrenergic and imidazoline I1, I2 receptor binding affinities. The most potent 2-[(naphthalen-1-ylmethoxy)imino] imidazolidine showed a high selectivity and good affinity for the [ 3H]prazosin-labeled α1-adrenoceptors (Ki = 107 nM). Representative compounds of this series were also tested in vivo for possible circulatory effects in rats after intravenous administration.
N-and o-substituted 4-[2-( diphenylmethoxy) -ethyl]-1- (phenyl) methyl) piperidine analogs and methods of treating cns disorders therewith
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Page 10, (2008/06/13)
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the
Structure - Activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: Evaluation of behavioral activity of O- and N-analogues and their binding to monoamine transporters
Dutta,Fei,Beardsley,Newman,Reith
, p. 937 - 948 (2007/10/03)
In our effort to develop a pharmacotherapy for the treatment of cocaine addiction, we embarked on synthesizing novel molecules targeting the dopamine transporter (DAT) molecule in the brain as DAT has been implicated strongly in the reinforcing effect of
Factors Affecting the Stability and Equilibria of Free Radicals. XIII. N-Alkoxy- and N-Aralkoxypicrylamines and ESR Spectra of the Corresponding Capto-Dative Persistent Aminyls
Stanciuc, Gabriela,Caproiu, M. Teodor,Caragheorgheopol, Agneta,Caldararu, Horia,Balaban, Alexandru T.,Walter, Robert I.
, p. 63 - 72 (2007/10/02)
Five O-alkylhydroxylamines and three aralkylhydroxylamines have been picrylated to give O-alkyl-N-picrylhydroxylamines.These were converted to the corresponding N-(ar)alkoxy-picryl-aminyl radicals in toluene solution, and the ESR spectra were recorded.Simulations of the spectra with reasonable parameters and g values confirm the expected radical structures.Hyperfine coupling constants for nuclei in the picryl (acceptor) ring are smaller than those for the (ar)alkoxy group.This indication of competitive electron pair delocalization to the picryl ring, together with the long lifetimes of these radicals (compared with the symmetrically substituted diphenylaminyls), both support the concept of captodative stabilization.
