- Efficient methyl esterification using methoxyl silica gel as a novel dehydrating reagent
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Methoxyl silica gel was prepared readily by the treatment of silica chloride with methanol. By using methoxyl silica gel as a dehydrating agent, carboxylic acids reacted with methanol in the presence of a protonic acid such as 12-phosphotungstic acid afforded the corresponding methyl esters in excellent yields.
- Li, Jian-Guo,Peng, Yan-Qing
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experimental part
p. 305 - 308
(2011/04/22)
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- Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors
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Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling non-regulated necrosis. This form of cell death can be induced in an array of cell types in apoptotic deficient conditions with death receptor family ligands. A series of [1,2,3]thiadiazole benzylamides was found to be potent necroptosis inhibitors (called necrostatins). A structure-activity relationship study revealed that small cyclic alkyl groups (i.e. cyclopropyl) and 2,6-dihalobenzylamides at the 4- and 5-positions of the [1,2,3]thiadiazole, respectively, were optimal. In addition, when a small alkyl group (i.e. methyl) was present on the benzylic position all the necroptosis inhibitory activity resided with the (S)-enantiomer. Finally, replacement of the [1,2,3]thiadiazole with a variety of thiophene derivatives was tolerated, although some erosion of potency was observed.
- Teng, Xin,Keys, Heather,Jeevanandam, Arumugasamy,Porco Jr., John A.,Degterev, Alexei,Yuan, Junying,Cuny, Gregory D.
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p. 6836 - 6840
(2008/03/14)
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- Compounds for the treatment of ischemia
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A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia
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