161315-46-4Relevant academic research and scientific papers
A multidisciplinary approach to probing enthalpy-entropy compensation and the interfacial mobility model
Wilfong, Erin M.,Kogiso, Yuri,Muthukrishnan, Sivaramakrishnan,Kowatz, Thomas,Du, Yu,Bowie, Amber,Naismith, James H.,Hadad, Christopher M.,Toone, Eric J.,Gustafson, Terry L.
supporting information; experimental part, p. 11515 - 11523 (2011/09/16)
In recent years, interfacial mobility has gained popularity as a model with which to rationalize both affinity in ligand binding and the often observed phenomenon of enthalpy-entropy compensation. While protein contraction and reduced mobility, as demonst
Synthesis of MMP inhibitor radiotracers [11C]methyl-CGS 27023A and its analogs, new potential PET breast cancer imaging agents
Fei, Xiangshu,Zheng, Qi-Huang,Hutchins, Gary D.,Liu, Xuan,Stone, K. Lee,Carlson, Kathy A.,Mock, Bruce H.,Winkle, Wendy L.,Glick-Wilson, Barbara E.,Miller, Kathy D.,Fife, Rose S.,Sledge, George W.,Sun, Hui Bin,Carr, Raymond E.
, p. 449 - 470 (2007/10/03)
[11C]Methyl-CGS 27023A (1a) and its analogs [11C]methyl-2-picolyl-CGS 27023A (1b), [11C]methyl-benzyl-CGS 27023A (1c), [11C]methyl-2-nitro-CGS 27023A (1d), [11C]methyl-3-nitro-CGS 27023A (1e), and [11C]methyl-4-nitro-CGS 27023A (1f), novel radiolabeled matrix metalloproteinase (MMP) inhibitors, have been synthesized for evaluation as new potential positron emission tomography (PET) breast cancer imaging agents. The appropriate precursors for radiolabeling were obtained in four to five steps from starting material amino acid D-valine with moderate to excellent chemical yields. Precursors were labeled by [11C]methyl triflate through 11C-O-methylation method at the aminohydroxyl position under basic conditions and isolated by solid-phase extraction (SPE) purification to produce pure target compounds in 40-60% radiochemical yields (decay corrected to end of bombardment), in 20-25 min synthesis time. Copyright
ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACIDS
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, (2008/06/13)
Disclosed are compounds of formula I STR1 wherein R, R 1, R. sub.2 and Ar have meanings as defined; pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions
ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACIDS
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, (2008/06/13)
The invention relates to the compounds of formula I STR1 pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.
ARYLSUFONAMIDO-SUBSTITUTED HYDROXAMIC ACIDS
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, (2008/06/13)
The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I STR1 wherein Ar, R, R 1 and R. sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.
Arylsulfonamido-substituted hydroxamic acids
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, (2008/06/13)
Particularly the invention relates to the compounds of formula I STR1 (a) wherein Ar is carbocyclic or heterocyclic aryl; R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C3 -C7 -cycloalkyl, C3 -C7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl; R1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C3 -C7 -cycloalkyl, C3 -C7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, (carbocyclic or heterocyclic aryl)-lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, (amino, mono- or di-lower alkylamino)-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl, acylamino-lower alkyl, piperidyl or N-lower alkylpiperidyl; R2 is hydrogen or lower alkyl; pharmaceutically acceptable prodrug derivatives; and pharmaceutically acceptable salts thereof.
