55023-79-5Relevant academic research and scientific papers
Highly Chemoselective gem-Difluoropropargylation of Aliphatic Alcohols
Okamura, Toshitaka,Egoshi, Syusuke,Dodo, Kosuke,Sodeoka, Mikiko,Iwabuchi, Yoshiharu,Kanoh, Naoki
, p. 16002 - 16006 (2019/11/19)
Despite the potential of α-fluoroethers in medicinal chemistry, their synthetic methods, especially etherification of aliphatic alcohols, have been limited. Herein, we developed two- and three-step gem-difluoropropargylation of aliphatic alcohols includin
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB 1 receptor
Piscitelli, Francesco,Ligresti, Alessia,La Regina, Giuseppe,Coluccia, Antonio,Morera, Ludovica,Allarà, Marco,Novellino, Ettore,Di Marzo, Vincenzo,Silvestri, Romano
supporting information; experimental part, p. 5627 - 5631 (2012/08/28)
We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modulators of the CB1 receptor. The presence of the carboxamide functionality was required in order to obtain a stimulatory effect. The maximum stimulatory activity on CB1 was exerted by carboxamides 13 (EC50 = 50 nM) and 21 (EC50 = 90 nM) bearing a dimethylamino or piperidinyl group, respectively, at position 4 of the phenethyl moiety and a chlorine atom at position 5 of the indole.
IMIDAZOLE DERIVATIVES AS IDO INHIBITORS
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Page/Page column 156-157, (2011/06/11)
Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
A new paradigm for biohydroxylation by Beauveria bassiana ATCC 7159
Holland, Herbert L.,Morris, Terence A.,Nava, Phillip J.,Zabic, Mirjana
, p. 7441 - 7460 (2007/10/03)
The biohydroxylation of a series of amides and related amino, keto and hydrocarbon substrates by the fungal biocatalyst Beauveria bassiana ATCC 7159 has been examined. The product distributions, together with data obtained from selective inhibition experiments using the cyt.P-450 inhibitors isosafrole, 1-aminobenzotriazole and phenylacetylene, suggest that B. bassiana contains a range of hydroxylase enzymes with different substrate specificities. A paradigm is presented for the interpretation of the results of microbial hydroxylation and for the application of existing active site models for B. bassiana.
Biooxidations of some N-Arylpiperidines and Related Compounds using Beauveria sulfurescens
Floyd, Nicholas,Munyemana, Francois,Roberts, Stanley M.,Willetts, Andrew J.
, p. 881 - 882 (2007/10/02)
Beauveria sulfurescens ATCC 7159 oxidized the N-arylamines 3, 4, 7, 13, 18, 20, 22 at the 4-position with good selectivity and in 34 - 66percent yield.
Potential antiinflammatory compounds. I. Antiinflammatory phenylpiperidine derivatives
Hicks,Smith,Williamson,Day
, p. 1460 - 1464 (2007/10/05)
The syntheses of a number of amines and their derivatives, based on the phenylpiperidine nucleus, are described. Their activities on the rat paw carrageenan test are also reported. Activities comparable to that of phenylbutazone were obtained for some of
