- Development of a method for the synthesis of 2,4,5-trisubstituted oxazoles composed of carboxylic acid, amino acid, and boronic acid
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A novel method for the synthesis of trisubstituted oxazoles via a one-pot oxazole synthesis/Suzuki–Miyaura coupling sequence has been developed. One-pot formation of 5-(triazinyloxy)oxazoles using carboxylic acids, amino acids and a dehydrative condensing reagent, DMT-MM, followed by Ni-catalyzed Suzuki–Miyaura coupling with boronic acids provided the corresponding 2,4,5-trisubstituted oxazoles in good yields.
- Yamada, Kohei,Kamimura, Naoto,Kunishima, Munetaka
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p. 1478 - 1485
(2017/08/02)
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- Novel L-arginine derivatives as aminopeptidase N inhibitors: design, chemistry, and pharmacological evaluation
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Considering the important roles played in tumor, aminopeptidase N has been an appealing target for anti-tumor drug development. Here, a serial of novel aminopeptidase N inhibitors with L-arginine scaffold were designed, synthesized and evaluated for aminopeptidase N inhibitory activities. The preliminary anti-enzyme activity assay demonstrated that compounds 5e, 5h, 11e, 11g, and 11h showed comparable activities with the positive control bestatin, an approved aminopeptidase N inhibitor. In vitro anti-proliferation assay, compound 5f showed excellent activities against four kinds of tumor cells which overexpress aminopeptidase N. In vivo anti-metastasis assay, compounds 5f and 11g exhibited better activities than bestatin. So 5f and 11g should be lead compounds as novel aminopeptidase N inhibitors for further development.
- Mou, Jiajia,Luan, Yepeng,Chen, Danghui,Wang, Qiang
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p. 3015 - 3025
(2017/10/06)
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- Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold l-arginine as amino-peptidase N/CD13 inhibitors
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A series of bi- or tri-peptide analogues with the scaffold l-arginine were designed, synthesized and evaluated for their inhibitory activities against amino-peptidase N (APN) and metalloproteinase-2 (MMP-2). The primary activity assay showed that all the compounds exhibited higher inhibitory activities against APN than MMP-2. Within this series, compounds C6 and C7 (IC50 = 4.2 and 4.3 μM) showed comparable APN inhibitory activities with the positive control bestatin (IC50 = 3.8 μM).
- Mou, Jiajia,Fang, Hao,Liu, Yingzi,Shang, Luqing,Wang, Qiang,Zhang, Lei,Xu, Wenfang
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experimental part
p. 887 - 895
(2010/05/02)
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- Synthesis and aldose reductase inhibitory activity of benzoyl-amino acid derivatives
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A series of N-(4-methoxy, 4-fluoro, 4-trifluoromethyl and 4-nitrobenzoyl)-L-amino acids was synthesized and their inhibitory activity towards bovine lens aldose reductase (ALR2) was tested.
- Benvenuti, Stefania,Severi, Fabio,Costantino, Luca,Vampa, Gabriella,Melegari, Michele
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p. 439 - 442
(2007/10/03)
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- N-TERMINAL SUBSTITUENT AND SIDE-CHAIN INFLUENCES ON THE CHEMICAL SHIFTS OF PROTONS IN MODEL DIPEPTIDE SYSTEMS
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(1)H Chemical shift values of ester methyls in model dipeptide esters have been shown to be sensitive to (a) the nature and configuration of the constituent amino acids and (b) the spatial distance between the N-terminal aryl group and the ester protons.C
- Davies, John S.,Hakeem, Essam
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p. 1387 - 1392
(2007/10/02)
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