- Structure-activity study of L-amino acid-based N-type calcium channel blockers
-
Synthesis and structure-activity relationship (SAR) study of L-amino acid-based N-type calcium channel blockers are described. The compounds synthesized were evaluated for inhibitory activity against both N-type and L-type calcium channels focusing on sel
- Seko, Takuya,Kato, Masashi,Kohno, Hiroshi,Ono, Shizuka,Hashimura, Kazuya,Takimizu, Hideyuki,Nakai, Katsuhiko,Maegawa, Hitoshi,Katsube, Nobuo,Toda, Masaaki
-
p. 1901 - 1913
(2007/10/03)
-
- Selective detachment of Boc-protected amino acids and peptides from Merrifield, PAM and Wang resins by trimethyltin hydroxide
-
We describe the development of a new non-acidolytic and non- nucleophilic method for the selective cleavage by trimethyltin hydroxide of amino acids and dipeptides at benzyl ester links attached to resins commonly used in peptide synthesis.
- Furlan, Ricardo L. E.,Mata, Ernesto G.,Mascaretti, Oreste A.,Pena, Clara,Coba, Marcelo P.
-
p. 13023 - 13034
(2007/10/03)
-
- Stable polypeptides having c-AMP production enhancing activity and the use thereof
-
Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof: wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO: 20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.
- -
-
-
- An improved method for the preparation of ω-cyclohexyl esters of aspartic and glutamic acid
-
An improved synthesis of β-cyclohexyl L-aspartate and γ-cyclohexyl L-glutamate and its N-tert-butoxycarbonyl (Boc) derivatives is described.
- Toth,Penke
-
p. 361 - 362
(2007/10/02)
-
- USE OF α-2-CYANOETHYL tert-BUTOXYCARBONYLASPARTATE AS AN INTERMEDIATE FOR SYNTHESIS OF β-ESTERS
-
The use of α-2-cyanoethyl Boc-aspartate is proposed for the first time for the synthesis of β-esters of Boc-aspartic acid.The α-2-cyanoethyl protective group is selectively split out by strong organic bases under hydrolytic conditions without the β-ester bond being affected.Using the α-2-cyanoethyl derivative, β-cyclohexyl, β-benzyl, and β-tert-butyl Boc-aspartates have been synthesized in good yields.
- Kalashnikov, V. V.,Samukov, V. V.
-
p. 196 - 198
(2007/10/02)
-