39124-16-8Relevant academic research and scientific papers
Extended diethylglycine homopeptides formed by desulfurization of their tetrahydrothiopyran analogues
De Zotti, Marta,Clayden, Jonathan
supporting information, p. 2209 - 2212 (2019/04/10)
Diethylglycine (Deg) homopeptides adopt the rare 2.05-helical conformation, the longest three-dimensional structure that a peptide of a given sequence can adopt. Despite this unique conformational feature, Deg is rarely used in peptide design b
A PYRAZOLO[1,5-A]PYRIMIDINE COMPOUND
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Page/Page column 125, (2008/06/13)
The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: -C(=O)- or -SO?2#191-, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C?3-8#191 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
Method for the synthesis of compounds of formula 1 and derivatives thereof
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Page 13, (2008/06/13)
Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).
A new series of cyclic amino acids as inhibitors of S-adenosyl L- methionine synthetase
Lavrador, Karine,Guillerm, Danielle,Guillerm, Georges
, p. 1629 - 1634 (2007/10/03)
Optically active 3-amino-3-(tetrahydrofuranyl) carboxylic acid, 3- amino-3-(tetrahydrothienyl) carboxylic acid and their corresponding six membered ring analogues have been synthesised and examined as potential inhibitors of the enzyme S-adenosylmethionine (AdoMet) synthetase. The kinetic behaviour of these compounds was studied using recombinant rat liver AdoMet synthetase (α-isoform) fractionated from E. coli transformed with the plasmid pSSRL-T7N. All the compounds tested were competitive inhibitors of the enzyme with respect to L-methionine.
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)
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.
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.
