21888-30-2Relevant academic research and scientific papers
α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment
Zhang, Linlin,Lin, Daizong,Kusov, Yuri,Nian, Yong,Ma, Qingjun,Wang, Jiang,Von Brunn, Albrecht,Leyssen, Pieter,Lanko, Kristina,Neyts, Johan,De Wilde, Adriaan,Snijder, Eric J.,Liu, Hong,Hilgenfeld, Rolf
, p. 4562 - 4578 (2020/03/05)
The main protease of coronaviruses and the 3C protease of enteroviruses share a similar active-site architecture and a unique requirement for glutamine in the P1 position of the substrate. Because of their unique specificity and essential role in viral po
Convenient green preparation of dipeptides using unprotected α-amino acids
Ezawa, Tetsuya,Jung, Seunghee,Kawashima, Yuya,Noguchi, Takuya,Imai, Nobuyuki
, p. 75 - 83 (2017/01/10)
Dipeptides and amides were obtained in high yields from N-carbobenzyloxy α-amino acids and 3-phenylpropanoic acid with unprotected α-amino acids via the corresponding mixed carbonic carboxylic anhydrides using ethyl chloroformate and triethylamine by an ecological and convenient method in which the protection of C-terminals is not needed.
Convenient peptide synthesis without protection of C-Terminals
Noguchi, Takuya,Tehara, Naoka,Uesugi, Yuki,Jung, Seunghee,Imai, Nobuyuki
scheme or table, p. 42 - 43 (2012/03/11)
Condensation of carboxylic acids 1 and 5 with unprotected α-amino acids 2 via activation by ethyl chloroformate and triethylamine proceeded effectively to afford the corresponding amides in 5099% yields. Tripeptide 7c was obtained in 42% yield from the dipeptide 6c in a similar manner.
Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors
Shang, Luqing,Fang, Hao,Zhu, Huawei,Wang, Xuejian,Wang, Qiang,Mu, Jiajia,Wang, Binghe,Kishioka, Shiroh,Xu, Wenfang
experimental part, p. 2775 - 2784 (2009/08/15)
Aminopeptidase N (APN), belonged to metalloproteinase, is an essential peptidase involved in the process of tumor invasion and metastasis. A series of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine were designed, synthesized and evaluate
PROCESS FOR THE SEPARATION OF RACEMIC MIXTURES
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Page 6, (2008/06/13)
The present invention relates to a process for the separation of racemic mixtures comprising development of a denser molecular imprint on silica with a desired enantiomer by sol-gel-protocol comprising hydrolytic control polymerization of a silica source as the monomer and amino alkylsilane as a functional monomer in the presence of the desired enantiomer, capping of surface OH groups and desorption of ancapsulated enantiomer from the silica.
4-SUBSTITUTED -3-[1 OR 2 AMINO ACID RESIDUE]-AZETIDIN-2-ONE DERIVATIVES USEFUL AS CYSTEINE PROTEINASE INHIBITOR
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, (2008/06/13)
Disclosed herein are azetidin-2-one compounds which exhibit excellent cysteine proteinase inhibitory activity. The compounds are 4-substituted-3-{1 or 2 amino acid residue}-azetidin-2-ones of forumula I STR1 wherein AAR is a 1 or 2 acid residue, and R 1 and R 2 are as defined herein. The compounds can be used in the treatment of various diseases such as muscular dystrophy, bone resorption disorders, myocardial infarction and cancer metastasis.
Inhibition of peptidylglycine α-amidating monooxygenase by N-substituted homocysteine analogs
Erion,Tan,Wong,Jeng
, p. 4430 - 4437 (2007/10/02)
C-terminal amidation is a posttranslational modification found in many neuropeptides. Peptidylglycine α-amidating monooxygenase (PAM) catalyzes the synthesis of the biologically essential C-terminal amide from a glycine- extended precursor peptide. Report
Selectivity in the Trimethylsilylation and Acylation of Peptide Bonds, and its Application to Modification of the Enkephalins
Davies, John S.,Merritt, Raymond K.,Treadgold, Richard C.,Morley, John S.
, p. 2939 - 2948 (2007/10/02)
N.m.r. spectra of N-acylated peptides, formed by reaction of protected peptides with silylating agents followed by acylation, have provided a means for assessing selectivity in the acylation of amide bonds.Amino-acids such as valine and phenylalanine prev
