206055-88-1Relevant articles and documents
Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles
Ratcliffe, Paul,Abernethy, Lynn,Ansari, Nasrin,Cameron, Ken,Clarkson, Tom,Dempster, Maureen,Dunn, David,Easson, Anna-Marie,Edwards, Darren,Everett, Katy,Feilden, Helen,Ho, Koc-Kan,Kultgen, Steve,Littlewood, Peter,MacLean, John,McArthur, Duncan,McGregor, Deborah,McLuskey, Hazel,Neagu, Irina,Nimz, Olaf,Nisbet, Lesley-Anne,Ohlmeyer, Michael,Palin, Ronnie,Pham, Quynhchi,Rong, Yajing,Roughton, Andrew,Sammons, Melanie,Swanson, Robert,Tracey, Heather,Walker, Glenn
scheme or table, p. 4652 - 4657 (2011/09/12)
Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted. Substitution of the 4-position with specific polar functionality afforded the requisite balance of potency, solubility and physicochemical properties. Compo
ISOXAZOLE-5-CARBOXAMIDE DERIVATIVES
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Page/Page column 17-18, (2010/08/18)
The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide de
Concise synthesis and antimicrobial activities of new substituted 5-isoxazolpenicillins
Wang, Xi-Zhao,Jia, Jiong,Zhang, Yan,Xu, Wei-Ren,Liu, Wei,Shi, Fang-Niu,Wang, Jian-Wu
, p. 643 - 652 (2008/03/11)
The synthesis of a series of new 5-isoxazolpenicillins is described, which were obtained by coupling substituted isoxazoles with 6-APA. Concise large-scale synthesis of 3,5-disubstituted isoxazoles by 1,3-dipolar cycloaddition using copper(I) as catalyst was also investigated. Representative compounds were assayed for antimicrobial activities, showing satisfactory antimicrobial activities against Gram-negative bacteria.
Substituted tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones as hypoglycemic agents
Aicher, Thomas D.,Balkan, Bork,Bell, Philip A.,Brand, Leonard J.,Cheon,Deems, Rhonda O.,Fell, Jay B.,Fillers, William S.,Fraser, James D.,Gao, Jiaping,Knorr, Douglas C.,Kahle, Gerald G.,Leone, Christina L.,Nadelson, Jeffrey,Simpson, Ronald,Smith, Howard C.
, p. 4556 - 4566 (2007/10/03)
A series of substituted tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones was synthesized from amino alcohols or amino thiols and keto acids. A pharmacological model based on the results obtained with these compounds led to the synthesis and evaluation of a series of isoxazoles and other monocyclic compounds. These were evaluated for their ability to enhance glucose utilization in cultured L6 myocytes. The in vivo hypoglycemic efficacy and potency of these compounds were evaluated in a model of type 2 diabetes mellitus (non-insulin-dependent diabetes mellitus), the ob/ob mouse. 25a(2S) (SDZ PGU 693) was selected for further pharmacological studies.