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螺吲哚酮类化合物的作用机制研究：一类新型抗疟药。

Mechanistic study of the spiroindolones: a new class of antimalarials.

机构信息

Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, Singapore.

出版信息

Molecules. 2012 Aug 24;17(9):10131-41. doi: 10.3390/molecules170910131.

DOI:10.3390/molecules170910131
PMID:22922283
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6268731/
Abstract

During the synthesis of the new antimalarial drug candidate NITD609, a high degree of diastereoselectivity was observed in the Pictet-Spengler reaction. By isolating both the 4E and 4Z imine intermediates, a systematic mechanistic study of the reaction under both kinetic and thermodynamic conditions was conducted. This study provides insight into the source of the diastereoselectivity for this important class of compounds.

摘要

在新型抗疟药物候选物 NITD609 的合成过程中，Pictet-Spengler 反应表现出高度的非对映选择性。通过分离出 4E 和 4Z 两种烯胺中间体，对动力学和热力学条件下的反应进行了系统的机理研究。该研究深入了解了这一类重要化合物非对映选择性的来源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/0604a02b39e2/molecules-17-10131-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/daec178fdaac/molecules-17-10131-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/7611a776e0ff/molecules-17-10131-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/c35111b141d2/molecules-17-10131-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/977eb3b41727/molecules-17-10131-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/8e93167c6a95/molecules-17-10131-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/0604a02b39e2/molecules-17-10131-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/daec178fdaac/molecules-17-10131-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/7611a776e0ff/molecules-17-10131-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/c35111b141d2/molecules-17-10131-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/977eb3b41727/molecules-17-10131-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/8e93167c6a95/molecules-17-10131-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ee49/6268731/0604a02b39e2/molecules-17-10131-g006.jpg

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Direct and highly enantioselective iso-Pictet-Spengler reactions with α-ketoamides: access to underexplored indole core structures.直接和高对映选择性的异 Pictet-Spengler 反应与 α-酮酰胺：探索较少的吲哚核心结构的途径。
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The Pictet-Spengler Reaction Updates Its Habits.
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A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.一项针对新型咪唑并哌嗪KAF156在健康成年志愿者中进行的首次人体随机、双盲、安慰剂对照、单剂量和多剂量递增口服给药研究，以评估其安全性、耐受性和药代动力学。
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