- Ferrocenylethenyl-substituted oxadiazoles with phenolic and nitro anchors as sensitizers in dye sensitized solar cells
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Three new ferrocenyl oxadiazoles, viz. (E)-2-(4-hydroxyphenyl)-5-(2-ferrocenyl-ethen-1-yl)-1,3,4-oxadiazole (D2), (E)-2-(4-nitrophenyl)-5-(2-ferrocenyl-ethen-1-yl)-1,3,4-oxadiazole (D3) and (E)-3-(4-nitrophenyl)-5-[5-(2-ferroceneylethen-1-yl)-1,3,4-oxadia
- Singh, Amita,Kociok-K?hn, Gabriele,Trivedi, Manoj,Chauhan, Ratna,Kumar, Abhinav,Gosavi, Suresh W.,Terashima, Chiaki,Fujishima, Akira
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p. 4745 - 4756
(2019/03/26)
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- Some regularities of the synthesis of ethyl 3-aryl-1,2,4-oxadiazole-5-carboxylates
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Features of amidoximes reactions with ethyl chlorooxalate in a wide range of solvents at the use of a number of bases were investigated. An efficient preparation method for ethyl 3-aryl-1,2,4-oxadiazole-5-carboxylates in acetonitrile in the presence of triethylamine was developed.
- Voronova,Baikov,Krasovskaya,Kolobov,Kofanov
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p. 1683 - 1686
(2015/02/02)
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- Synthesis and biological evaluation of isoxazole, oxazole, and oxadiazole containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors
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Diacylglycerol acyltransferase, DGAT1, is a promising target enzyme for obesity due to its involvement in the committed step of triglyceride biosynthesis. Amino biphenyl carboxylic acids, exemplified by compound 4, are known potent inhibitors of hDGAT1. However the high cLogP and poor solubility of these biphenyl analogs might tend to limit their development. We have synthesized and evaluated compounds containing 3-phenylisoxazole, 5-phenyloxazole, and 3-phenyl-1,2,4-oxadiazole biaryl units for their hDGAT1 inhibition. Our aim in synthesizing such heterocyclic analogs was to improve the cLogP and solubility of these molecules while retaining hDGAT1 potency. Several compounds within the 3-phenylisoxazole series exhibited potent hDGAT1 inhibition when evaluated using an in vitro enzymatic assay. Certain promising compounds were studied for their potential to reduce triglyceride levels using an in vivo fat tolerance test in mice and were also evaluated for any possible improvement to their solubility. Compound 40a (IC50 = 64 nM) with an in vivo plasma triglyceride reduction of 90 percent, and a solubility of 0.43 mg/ml at pH 7.4 may serve as a new lead for developing newer anti-obesity agents.
- Jadhav, Ravindra D.,Kadam, Kishorkumar S.,Kandre, Shivaji,Guha, Tandra,Reddy, M. Mahesh Kumar,Brahma, Manoja K.,Deshmukh, Nitin J.,Dixit, Amol,Doshi, Lalit,Potdar, Nisha,Enose, Arno A.,Vishwakarma, Ram A.,Sivaramakrishnan,Srinivasan, Shaila,Nemmani, Kumar V.S.,Gupte, Amol,Gangopadhyay, Ashok K.,Sharma, Rajiv
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experimental part
p. 324 - 342
(2012/09/07)
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- OXAZOLE, OXADIAZOLE AND THIAZOLE DERIVATIVES AS DIACYLGLYCEROL ACYLTRANFERASE INHIBITORS
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The present invention relates to isoxazole, thiazole and oxidiazole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, in particular to the use of these compounds in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1.
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Page/Page column 123
(2010/04/06)
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- Antiparasitic Agents. 6. Synthesis and Anthelmintic Activities of Novel Isothiocyanatophenyl-1,2,4-oxadiazoles
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The syntheses and anthelmintic activities of 31 3- and 5-(isothiocyanatophenyl)-1,2,4-oxadiazoles are reported.In the primary anthelmintic screen, 3-(4-isothiocyanatophenyl)-1,2,4-oxadiazole (39) showed 100percent nematocidal activity and 3-(2-furanyl)-5-
- Haugwitz, R. D.,Martinez, A. J.,Venslavsky, J.,Angel, R. G.,Maurer, B. V.,et al.
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p. 1234 - 1241
(2007/10/02)
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