2,7-二氨基庚酸 在
腺嘌呤黄素 、 catalase Pseudomonas putida N-methyl-L-amino acid dehydrogenase 、 T. viride L-lysine oxidase 、 Tris buffer 作用下,
以
various solvent(s) 为溶剂,
反应 2.0h,
生成 (S)-Perhydroazepine-2-carboxylic acid
参考文献:
名称:
Enzymatic synthesis of cyclic amino acids by N-methyl-l-amino acid dehydrogenase from Pseudomonas putida
摘要:
A new enzymatic system for the synthesis of enantiomerically pure cyclic amino acids (CAA) from the corresponding diamino acids or racemic CAA is described. alpha,omega-Diamino acids were oxidized to alpha-keto acids with amino acid oxidases (AAO). The alpha-keto acids were spontaneously transformed into cyclic imino acids in the reaction medium. The resulting imines were reduced to the L-form CAA with N-methyl-L-amino acid dehydrogenase (NMAADH) from Pseudomonas putida ATCC12633 using NADPH as a cofactor. L-Form CAA were also obtained from racemic CAA using D-amino-acid oxidase and NMAADH. Using this method, a new compound [1,4]thiazepane-3-carboxylic acid (Fig. 1) was synthesized from aminopropylcystein. (c) 2006 Published by Elsevier Ltd.
[EN] BACKBONE-CYCLIZED PEPTIDOMIMETICS<br/>[FR] PEPTIDOMIMÉTIQUES À SQUELETTE CYCLISÉ
申请人:POLYPHOR AG
公开号:WO2016162127A1
公开(公告)日:2016-10-13
Novel backbone-cyclized peptidomimetics of the general formula cyclo[-P1-P2-P3-P4-P5-P6-P7-P8-T1-T2-] (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
[EN] BETA-HAIRPIN PEPTIDOMIMETICS<br/>[FR] PEPTIDOMIMÉTIQUES EN ÉPINGLE À CHEVEUX BÊTA
申请人:POLYPHOR AG
公开号:WO2016150576A1
公开(公告)日:2016-09-29
Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiellapneumoniae and/or Acinetobacter baumannii and/or Escherichia coli and/or Pseudomonas aeruginosa. They ca n be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
The present invention relates to novel peptide compounds which are effective in modulating one or more melanocortin receptor types, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of obesity as well as a variety of diseases or conditions associated with obesity.
TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVITY
申请人:Jung Francoise
公开号:US20120283168A1
公开(公告)日:2012-11-08
Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
Beta-hairpin peptidomimetics of the general formula (I), cyclo[P
1
-p
2
-p
3
-p
4
-p
5
-p
6
-p
7
-p
8
p
9
-p
10
-p
11
-p
12
-T
1
-T
2
], and pharmaceutically acceptable salts thereof, with P
1
to P
12
, T
1
and T
2
being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as
Klebsiella pneumoniae
and/or
Acinetobacter baumannii
and/or
Escherichia coli
. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.