- Hydrazone linker as a useful tool for preparing chimeric peptide/ Nonpeptide bifunctional compounds
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The area of multitarget compounds, joining two pharmacophores within one molecule, is a vivid field of research in medicinal chemistry. Not only pharmacophoric elements are essential for the design and activity of such compounds, but the type and length o
- Dyniewicz, Jolanta,Lipinski, Piotr F. J.,Kosson, Piotr,Lesniak, Anna,Bochynska-Czyz, Marta,Muchowska, Adriana,Tourwe, Dirk,Ballet, Steven,Misicka, Aleksandra,Lipkowski, Andrzej W.
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supporting information
p. 73 - 77
(2017/12/12)
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- Kinetically controlled peptide synthesis mediated by papain using the carbamoylmethyl ester as an acyl donor
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A series of dipeptides were synthesized generally in good yields with carbamoylmethyl (Cam) esters as acyl donors in the presence of a cysteine protease, papain, immobilized on Celite. Several segment condensations were also achieved generally in high yields without danger of racemization and formation of the secondary-hydrolysis product. Moreover, partial sequences of some bioactive peptides were prepared through segment condensations, and aimed-at peptides were obtained generally in high yields without the racemization of C-terminal residues of the carboxyl components. Thus, the superiority of the Cam ester in the kinetically controlled peptide synthesis was once again ascertained in couplings mediated by the cysteine protease as in those catalyzed by the serine proteases reported earlier.
- Miyazawa, Toshifumi,Horimoto, Takao,Tanaka, Kayoko
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p. 371 - 376
(2014/08/18)
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- Evidence of the Preferential Involvement of μ Receptors in Analgesia Using Enkephalins Highly Selective for Peripheral μ or δ Receptors
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In order to study the preferential involvement of μ or δ receptors in the analgesic effects of enkephalins, several peptides which selectively interact with these two kinds of receptors in peripheral organs were synthesized.The inhibitory potency on the e
- Gacel, Gilles,Fournie-Zaluski, Marie-Claude,Fellion, Etienne,Roques, Bernard P.
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p. 1119 - 1124
(2007/10/02)
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- Synthesis and pharmacological study of some enkephalin analogs in relation to the plurality of opiate receptors
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We have synthesized a series of enkephalin analogs and measured their affinity for each type of 'opiate' receptor, the μ receptor and the δ receptor. Furthermore, we have determined their respective antinociceptive activity after intracerebroventricular i
- Audigier,Mazarguil,Gout,Cros
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p. 173 - 177
(2007/10/02)
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