26452-99-3Relevant academic research and scientific papers
NOVEL TRPV3 MODULATORS
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Paragraph 0408; 0409; 0424, (2013/06/27)
Disclosed herein are modulators of TRPV3 of formula (I) wherein G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
NOVEL TRPV3 MODULATORS
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Page/Page column 77, (2012/03/09)
Disclosed herein are modulators of TRPV3 of formula (I), wherein G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, u, and p are as defined in the specifica
Iminyl, Amidyl, and Carbamyl Radicals from O-Benzoyl Oximes and O-Benzoyl Hydroxamic Acid Derivatives.
Boivin, Jean,Callier-Dublanchet, Anne-Claude,Quiclet-Sire, Beatrice,Schiano, Anne-Marie,Zard, Samir Z.
, p. 6517 - 6528 (2007/10/02)
Oxime benzoates and O-benzoyl hydroxamic acid derivatives react with tributylstannane in the presence of AIBN to give iminyl, amidyl, and carbamyl radicals which can be captured by an internal olefin.
Iminyl radicals by stannane mediated cleavage of oxime esters
Boivin, Jean,Schiano, Anne-Marie,Zard, Samir Z.
, p. 249 - 252 (2007/10/02)
Despite the explosive growth in the use of radical reactions which has swept organic synthesis in the past few years, nitrogen centred radicals and iminyls in particular have not yet attracted the attention they deserve This can be traced to a large extent to a lack of convenient and mild methods for generating such species. As part of a general study of the reactivity and synthetic potential of iminyls, we recently showed that the reaction of sulfenimines with tributystannane or the Barton decarboxylation of O-carboxymethyl oximes represented useful routes to these intermediates. Another promising approach, still in its preliminary stages however, involved the reduction of oxime esters with nickel powder in acetic acid. in this Letter, we describe yet another method based on the cleavage of oxime benzoates with tin centered radicals.
Iminyl radicals: Part II. Ring opening of cyclobutyl- and cyclopentyliminyl radicals
Boivin, Jean,Fouquet, Eric,Zard, Samir Z.
, p. 1757 - 1768 (2007/10/02)
Slow addition of tributylstannane to sulphenylimines 2 give the corresponding cycloiminyl radicals 3 which can undergo ring opening, a process that is easily incorporated into complex reaction sequences.
Antihyperglycemic activity of novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides
Ellingboe,Alessi,Dolak,Nguyen,Tomer,Guzzo,Bagli,McCaleb
, p. 1176 - 1183 (2007/10/02)
A series of substituted 3H-1,2,3,5-oxathiadiazole-2-oxides (6) was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus. The oxathiadiazoles 6 were synthesized by a two-step sequence: treatment of a substituted acetonitrile (4) with hydroxylamine to give the corresponding amidoxime (5) and cyclization with thionyl chloride to yield 6. In terms of potency, the 2-naphthalenylmethyl group (as in compound 3) was found to be the optimal substituent in this series. Compound 3 was approximately 5 times more potent than ciglitazone (1).
Synthesis and Anti-inflammatory Activity of a Few 5-(Indan-1'yl)methyltetrazoles
Roy, A.,Gupta, J. K.,Lahiri, S.C.
, p. 377 - 380 (2007/10/02)
In an attempt to develop relatively less toxic and more potent anti-inflammatory agents than the presently available ones, a few 5-(indan-1'-yl)methyltetrazoles have been synthesised and subjected to anti-inflammatory screening.Two of them showed anti-inflammatory potency close to that of phenylbutazone in both acute (carrageenin-induced edema) and chronic (adjuvant-induced arthritis) animal test models.The compounds have high LD50 and high therapeutic index, and appreciable analgesic and antipyretic activity
