- Photoactive chemosensors 3: A unique case of fluorescence enhancement with Cu(II)
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Chemosensor (4a) shows fluorescence enhancement with Cu(II) and can estimate 1-300 μM Cu(II) by using fluorescence (1-20 μM) and UV-Vis (10-300 μM) spectroscopic techniques. Ni(II), Cd(II), Zn(II), Ag(I) and Hg(II) do not interfere in fluorescence studies and only Ag(I) and Hg(II) interfere in UV-Vis studies.
- Kaur, Sukhdeep,Kumar, Subodh
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- Synthesis and structure - Activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis
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The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. In our preceding paper, we have reported on a series of novel and orally active N-hydroxy-α-phenylsulfonylacetamide derivatives. However, these compounds had two drawbacks (moderate selectivity and chirality issues). To circumvent these two problems, a series of novel and orally active N-substituted 4-benzenesulfonylpiperidine-4-carboxylic acid hydroxyamide derivatives have been synthesized. The present paper deals with the synthesis and SAR of these compounds. Among the several compounds synthesized, derivative 55 turned out to be a potent, selective, and an orally active MMP inhibitor in the clinically relevant advanced rabbit osteoarthritis model. Detailed pharmacokinetics and metabolism data are described.
- Aranapakam, Venkatesan,Davis, Jamie M.,Grosu, George T.,Baker, Jannie,Ellingboe, John,Zask, Arie,Levin, Jeremy I.,Sandanayaka, Vincent P.,Du, Mila,Skotnicki, Jerauld S.,DiJoseph, John F.,Sung, Amy,Sharr, Michele A.,Killar, Loran M.,Walter, Thomas,Jin, Guixian,Cowling, Rebecca,Tillett, Jeff,Zhao, Weiguang,McDevitt, Joseph,Xu, Zhang Bao
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p. 2376 - 2396
(2007/10/03)
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- 1,4-(diphenlyalkyl) piperazine derivatives
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This invention relates to novel compounds of the formula [I], STR1 wherein R 1 and R 2 are the same or different and each represents a lower alkoxy group; A and B are the same or different and each represents a lower alkylene group.The compounds of this i
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- (N-phthalimidoalkyl) piperidines useful as treatments for psychosis
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There is described novel (N-phthalimidoalkyl) piperidine compounds which exhibit selective sigma-receptor antagonism and therefore are useful in the treatment of physiological or drug induced psychosis and dyskinesia in a mammal. Also described are pharmaceutical compositions containing sigma selective compounds and methods of using these compositions for treating physiological or drug induced psychosis or dyskinesia in a mammal. Further provided are methods for preparing the compounds of this invention.
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