- A new somatostatin analog with optimized ring size inhibits neointima formation induced by balloon injury in rats without altering growth hormone release
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We report on the synthesis and pharmacological properties of a new series of somatostatin analogs. Two lower homologs of lysine, 2,3-diaminopropanoic acid and 2,4-diaminobutyric acid, were prepared and used for cyclization via amide formation with the side chain of aspartic or glutamic acid in place of natural cystine present in many somatostatin analogs. One resulting compound, although having low binding affinities for somatostatin receptors, displayed a strong potency in inhibiting neointima formation induced by balloon injury in rats at the dose of 100 μg·kg-1·d-1. This dissociation of the antiproliferative effect from the endocrine effect seems to indicate that myointimal growth is not related to a change in growth hormone secretion.
- Thurieau,Janiak,Krantic,Guyard,Pillon,Kucharczyk,Vilaine,Fauchere
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- COMPOUND FOR PREPARATION OF ANTIBODY-PAYLOAD CONJUGATE AND USE THEREOF
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The present application relates to a novel linker for use in bioconjugation, comprising two or more electrophilic carbon atoms of a carbonyl group, and a click chemistry functional group and, more specifically, to a linker through which a compound, a peptide, and/or a protein can be directly and/or indirectly linked by a substitution reaction to a desired target molecule, that is, a target molecule.
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- A Nα-fluorenylmethyloxycarbonyl-Nγ-tert-butoxy carbonyl-L-2,4-diamino-butyric acid synthetic method (by machine translation)
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This invention involves a kind of Nα-fluorenylmethyloxycarbonyl-Nγ-tert-butoxy carbonyl-L-2,4-diamino-butyric acid synthetic method. Mainly solves the problems that the prior method for preparing more existent steps of and avoid the use of palladium carbon cause very difficult problems of processing technology. The technical scheme of the invention is:a kind of Nα-fluorenylmethyloxycarbonyl-Nγ-tert-butoxy-carbonyl-L-2,4-diamino-butyric acid synthetic method, a Nα-fluorenylmethyloxycarbonyl-Nγ-tert-butoxy-carbonyl-L-2,4-diamino-butyric acid synthetic method, its characteristic is to include the following steps: 1st-step reaction, suspension Fmoc-Gln-OH with acetonitrile, ethyl acetate and water mixed solvent, adding diethyla acid iodophenylamino reaction post-processed to obtain Fmoc-Dab-OH; 2nd-step reaction, acetone and Fmoc-Dab-OH under the condition of the water by adding (Boc) 2 O, for adjusting NaOH pH= 7.5-8, by treatment after reaction Fmoc-Dab (Boc)-OH. The present invention provides large-scale production method for Fmoc-Dab (Boc)-OH. (by machine translation)
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Paragraph 0020
(2016/10/09)
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- Practical and efficient synthesis of orthogonally protected α-2,3-diaminopropionic acid (2,3-Dap), 2,4-diaminobutanoic acid (2,4-Dab), and their N-methylated derivatives
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The synthesis of orthogonally protected Fmoc-Dap/Dab (Boc/Z/Alloc)-OH starting from Fmoc-Asp/Glu has been described. The salient features of our synthetic strategy involved formation of Fmoc-Asp/Glu-5-oxazolidinone acids, conversion of acid function to acyl azides, Curtius rearrangement, and hydrolysis of the oxazolidinone group. Copyright Taylor & Francis Group, LLC.
- Rao, R. V. Ramana,Tantry, Subramanyam J.,Babu, Vommina V. Suresh
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p. 2901 - 2912
(2007/10/03)
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- The contribution of the N-terminal structure of polymyxin B peptides to antimicrobial and lipopolysaccharide binding activity
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To elucidate the N-terminal structure-activity relationships of polymyxin B peptides, seven polymyxin B component peptides, the structures of which having been elucidated, and seven N-terminal fatty acid and/or amino acid deletion analogs were synthesized, and their antimicrobial activities determined. The lipopolysaccharide (LPS) binding activities of synthetic peptides were evaluated using [Dab(Dansyl-Gly)1]-polymyxin B3 (Dab; L-α,γ-diaminobutyric acid) as a fluorescent probe. The results indicated that the fatty acyl moiety was not indispensable for LPS binding, but the C9 fatty acyl groups of polymyxin B peptides contributed to the binding affinity to a slightly greater extent than C8 or C 7. The fatty acyl moieties of polymyxin B contributed greatly to the antimicrobial activity, while the distinct N-terminal structures of polymyxin B1-B6, bearing normal-, iso-, or anteiso-fatty acids, or 3-hydroxy-fatty acid with chain lengths between C7 and C9, did not affect bactericidal potency.
- Sakura, Naoki,Itoh, Tatsuya,Uchida, Yoshiki,Ohki, Kazuhiro,Okimura, Keiko,Chiba, Kenzo,Sato, Yuki,Sawanishi, Hiroyuki
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p. 1915 - 1924
(2007/10/03)
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