135544-90-0Relevant academic research and scientific papers
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
Synthesis and Superpotent Anticancer Activity of Tubulysins Carrying Non-hydrolysable N-Substituents on Tubuvaline
Sani, Monica,Lazzari, Paolo,Folini, Marco,Spiga, Marco,Zuco, Valentina,De Cesare, Michelandrea,Manca, Ilaria,Dall'Angelo, Sergio,Frigerio, Massimo,Usai, Igor,Testa, Andrea,Zaffaroni, Nadia,Zanda, Matteo
, p. 5842 - 5850 (2017/04/28)
Synthetic tubulysins 24 a–m, containing non-hydrolysable N-substituents on tubuvaline (Tuv), were obtained in high purity and good overall yields using a multistep synthesis. A key step was the formation of differently N-substituted Ile-Tuv fragments 10 b
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines
Moas-Héloire, Valeria,Renault, Nicolas,Batalha, Vania,Arias, Angela Rincon,Marchivie, Mathieu,Yous, Said,Deguine, Noémie,Buée, Luc,Chavatte, Philippe,Blum, David,Lopes, Luisa,Melnyk, Patricia,Agouridas, Laurence
, p. 15 - 25 (2015/11/23)
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolinesg" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy
Lescop, Cyrille,Herzner, Holger,Siendt, Herve,Bolliger, Reto,Henneboehle, Marco,Weyermann, Philipp,Briguet, Alexandre,Courdier-Fruh, Isabelle,Erb, Michael,Foster, Mark,Meier, Thomas,Magyar, Josef P.,Von Sprecher, Andreas
, p. 5176 - 5181 (2007/10/03)
Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50 values down to 25 nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.
Piperizinones as modulators of chemokine receptor activity
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, (2008/06/13)
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Antiretroviral hydrazine derivatives
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, (2008/06/13)
The invention relates to compounds of formula STR1 and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BRADYKININ ANALOGUES WITH Ψ(E,CH=CH) AND Ψ(CH2-NH) ISOSTERIC PEPTIDE BOND REPLACEMENTS
Scarso, A.,Degelaen, J.,Viville, R.,Cock, E. De,Marsenille, M. Van,et al.
, p. 381 - 399 (2007/10/02)
The synthesis of bradykinin analogues is described in which the Gly4-Phe5, Phe5-Ser6 or the Pro7-Phe8 peptide bond has been replaced by a trans carbon-carbon double bond or by a "reduced" peptide bond.Some of the analogues display high potency and prolonged activity in the rat blood pressure test, indicating increased metabolic stability.A clear selectivity is obtained towards the myotropic effect in the guinea pig ileum.
