68858-21-9Relevant articles and documents
Synthetic method of p-hydroxymethylphenoxyacetic acid serving as linker
-
Paragraph 0005; 0013, (2017/03/08)
The invention relates to a synthetic method of p-hydroxymethylphenoxyacetic acid serving as a linker and aims at solving the technical problems that a traditional method is higher in cost, is unfavorable for body health and the like. The technical scheme adopted by the invention is that the synthetic method of the p-hydroxymethylphenoxyacetic acid serving as the linker comprises the following steps of condensing p-hydroxy benzaldehyde and chloroacetic acid under the alkaline condition to obtain p-formylphenoxyacetic acid; reducing the p-formylphenoxyacetic acid by using a reducing agent to obtain the p-hydroxymethylphenoxyacetic acid. The synthetic method disclosed by the invention is low in synthetic cost and is suitable for scale production.
Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin
Hidaka, Koushi,Kimura, Tooru,Ruben, Adam J.,Uemura, Tsuyoshi,Kamiya, Mami,Kiso, Aiko,Okamoto, Tetsuya,Tsuchiya, Yumi,Hayashi, Yoshio,Freire, Ernesto,Kiso, Yoshiaki
scheme or table, p. 10049 - 10060 (2009/04/07)
Plasmepsin (Plm) is a potential target for new antimalarial drugs, but most reported Plm inhibitors have relatively low antimalarial activities. We synthesized a series of dipeptide-type HIV protease inhibitors, which contain an allophenylnorstatine-dimethylthioproline scaffold to exhibit potent inhibitory activities against Plm II. Their activities against Plasmodium falciparum in the infected erythrocyte assay were largely different from those against the target enzyme. To improve the antimalarial activity of peptidomimetic Plm inhibitors, we attached substituents on a structure of the highly potent Plm inhibitor KNI-10006. Among the derivatives, we identified alkylamino compounds such as 44 (KNI-10283) and 47 (KNI-10538) with more than 15-fold enhanced antimalarial activity, to the sub-micromolar level, maintaining their potent Plm II inhibitory activity and low cytotoxicity. These results suggest that auxiliary substituents on a specific basic group contribute to deliver the inhibitors to the target Plm.
Peptide Synthesis. Part 2. Procedures for Solid-phase Synthesis using Nα-fluorenylmethoxycarbonylamino-acids on Polyamide Supports. Synthesis of Substance P and of Acyl Carrier Protein 65-74 Decapeptide
Atherton, Eric,Logan, Christopher J.,Sheppard, Robert C.
, p. 538 - 546 (2007/10/02)
Use of base-labile Nα-9-fluorenylmethoxycarbonylamino-acids in combination with acid-labile t-butyl or p-alkoxybenzyl side-chain or carboxy-terminal (resin-linkage) protecting groups enables solid-phase peptide synthesis to be carried out under exceptionally mild reaction conditions.The repetitive and vigorous acidic treatments required in conventional synthesis are avoided.High-yield syntheses of a decapeptide and of an undecapeptide amide (Substance P) are described using this new combination of protecting groups on polyamide supports.
