161314-89-2Relevant academic research and scientific papers
Synthesis, calpain inhibitory activity, and cytotoxicity of P 2-substituted proline and thiaproline peptidyl aldehydes and peptidyl α-ketoamides
Korukonda, Rajani,Guan, Na,Dalton, James T.,Liu, Jiuyu,Donkor, Isaac O.
, p. 5282 - 5290 (2007/10/03)
Calpain is a cytosolic cysteine endopeptidase that has been implicated in a number of disorders including cancer. We have synthesized and studied the μ-calpain inhibitory activity and cytotoxicity of peptidyl aldehydes and peptidyl α-ketoamides with N-sub
ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACIDS
-
, (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
-
, (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
-
, (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.
