132067-41-5Relevant articles and documents
NOVEL AMINOPEPTIDASE INHIBITORS AND METHODS OF USE
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, (2017/02/09)
An aminopeptidase inhibitor compound comprising a biaryl, hydroxamic acid based core of formula: wherein X is a 5 or 6-membered ring, and including pharmaceutically acceptable salts and solvates thereof.
Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions
Drinkwater, Nyssa,Vinh, Natalie B.,Mistry, Shailesh N.,Bamert, Rebecca S.,Ruggeri, Chiara,Holleran, John P.,Loganathan, Sasdekumar,Paiardini, Alessandro,Charman, Susan A.,Powell, Andrew K.,Avery, Vicky M.,McGowan, Sheena,Scammells, Peter J.
, p. 43 - 64 (2016/01/30)
Malaria remains a global health problem, and though international efforts for treatment and eradication have made some headway, the emergence of drug-resistant parasites threatens this progress. Antimalarial therapeutics acting via novel mechanisms are urgently required. Plasmodium falciparum M1 and M17 are neutral aminopeptidases which are essential for parasite growth and development. Previous work in our group has identified inhibitors capable of dual inhibition of PfA-M1 and PfA-M17, and revealed further regions within the protease S1 pockets that could be exploited in the development of ligands with improved inhibitory activity. Herein, we report the structure-based design and synthesis of novel hydroxamic acid analogues that are capable of potent inhibition of both PfA-M1 and PfA-M17. Furthermore, the developed compounds potently inhibit Pf growth in culture, including the multi-drug resistant strain Dd2. The ongoing development of dual PfA-M1/PfA-M17 inhibitors continues to be an attractive strategy for the design of novel antimalarial therapeutics.
TETRAZINE-CONTAINING COMPOUNDS AND SYNTHETIC METHODS THEREOF
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, (2016/08/29)
Described herein are tetrazine derivatives and efficient synthetic methods of synthesis thereof using elimination-Heck cascade reaction. Provided herein is the synthesis of conjugated tetrazines from the tetrazine derivatives. Also provided herein are met
In situ synthesis of alkenyl tetrazines for highly fluorogenic bioorthogonal live-cell imaging probes
Wu, Haoxing,Yang, Jun,Seckute, Jolita,Devaraj, Neal K.
supporting information, p. 5805 - 5809 (2014/06/10)
In spite of the wide application potential of 1,2,4,5-tetrazines, particularly in live-cell and in vivo imaging, a major limitation has been the lack of practical synthetic methods. Here we report the in situ synthesis of (E)-3-substituted 6-alkenyl-1,2,4
NOVEL COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASE
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, (2011/10/03)
The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease
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, (2013/03/26)
The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of formula (1) or (2) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
Synthesis of 4-phosphono- and of 4-(phosphonomethyl)-dl-phenylalanine, two analogues of O-phosphotyrosine
Bayle-Lacoste, Mireille,Moulines, Jean,Collignon, Noel,Boumekouez, Abdelkader,De Tinguy-Moreaud, Eliane,Neuzil, Eugene
, p. 7793 - 7802 (2007/10/18)
:4-Phosphono-DL-phenylalanine 1 was synthetized from 4-bromo-DL-phenylalanine or from 4-(bromomethyl)-bromobenzene ; 4-(phosphonomethyl)-DL-phenylalanine 14 was prepared from methyl p-toluate. The interest of these phosphonic analogues arises from their possible interference in the metabolism of O-phosphotyrosine.