65128-66-7Relevant academic research and scientific papers
General Entry into o-,o′-Heteroatom-Linked N-(Hetero)aryl-Imidazole Motifs by Gold-Catalysed Formal [3+2]-Dipolar Cycloaddition
Garzón, Miguel,Arce, Elsa M.,Reddy, Raju Jannapu,Davies, Paul W.
supporting information, p. 1837 - 1843 (2017/06/09)
A general redox-neutral approach into the o-,o′-heteroatom-linked N-(hetero)aryl-imidazole family of heteroaromatics has been developed. New types of heteroatom substituted carbimidoyl nitrenoids are efficiently realised from robust, bench-stable N-(heteroaryl)-pyridinium-N-aminides by formal gold-catalysed [3+2]-dipolar cycloadditions across ynamides. Broad structural variety and functional group tolerance allows rapid access into diverse functionalised scaffolds, as exemplified by the preparation of 8 different heteroaromatic cores. (Figure presented.).
NOVEL HETEROARYL-AMINO DERIVATIVES
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Page/Page column 32, (2013/05/09)
Disclosed is a compound of formula (I), wherein R1, R2, L, Rm and Rn are as defined herein. The compound of formula (I) may be used in preventing and/or treating acyl CoA-diacylglycerol acyltransferase 1(DGAT-1) related diseases, such as obesity, coronary disease, hypertension, hyperlipidemia, arteriosclerosis, type II diabetes, stroke, hepatitis C, and the like.
COMPOUNDS FOR MODULATING TRPV3 FUNCTION
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Page/Page column 145-146, (2008/06/13)
The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
Non-imidazole histamine H3 ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H3-antagonists
Walczyski, Krzysztof,Zuiderveld, Obbe P.,Timmerman, Henk
, p. 15 - 23 (2007/10/03)
In search for a new lead of non-imidazole histamine H3-receptor antagonists, a series of 1[(2-thiazolopyridine)-4-n-propyl]piperazines, the analogous 1-[(2-oxazolopyridine)-4-npropyl]piperazines, 1-[(2-benzothiazole)-4- n-propyl]piperazine and 1-[(2-benzooxazole)4-n-propyl]piperazine were prepared and in vitro tested as H3-receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). It appeared that by comparison of homologous pairs the thiazolo derivatives have slightly higher activity than their oxazolo analogues. The most potent compound of these series is the 1-(2-thiazolo[4,5-c]pyridine)-4-n-propylpiperazine (3c) with pA2 = 7.25 (its oxazole analogue (4g) showed pA2 = 6.9). The structure-activity relationships for compounds with various positions of the nitrogen in the benzene ring for the thiazoles compared with oxazoles are discussed.
β-lactam compounds and process for producing the same
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, (2008/06/13)
Novel β-lactam compound of the formula [1]: wherein R1is lower alkyl or hydroxy-substituted lower alkyl, R2is H or lower alkyl, X is O or, S, R3is H, metal or protecting group, W is a 6- or 7-membered nitrogen-containing heterocycle optionally being substituted at carbon atoms. Said β-lactam compound shows excellent antibacterial activity against Gram-positive bacteria, particularly against methicillin-resistantStaphylococcus aureusand methicillin-resistant and coagulase-negativeStaphylococcus aureus.
Cephalosporin derivatives
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, (2008/06/13)
A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): STR1 wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.
