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Curr Trop Med Rep. 2021;8(2):121-132. doi: 10.1007/s40475-021-00232-7. Epub 2021 Mar 17.
2
[3 + 2]-Dipolar Cycloaddition of Aldehyde-Tethered Alkynamides and Trimethylsilyl Amino Esters: A Gateway to Uniquely Functionalized Polycyclic N-Heterocycles via Post-Ugi Functionalization.醛基封端炔丙酰胺和三甲基硅基氨基酯的[3 + 2]-偶极环加成：通过 Ugi 后官能化构建独特官能化的多环 N-杂环化合物的途径。
J Org Chem. 2020 Dec 4;85(23):14890-14904. doi: 10.1021/acs.joc.0c01539. Epub 2020 Nov 2.
3
Synthesis of β- and γ-lactam fused dihydropyrazinones from Ugi adducts a sequential ring construction strategy.β-和γ-内酰胺稠合二氢吡嗪酮的 Ugi 加合物合成：一种连续环构建策略。
Chem Commun (Camb). 2020 Oct 22;56(84):12789-12792. doi: 10.1039/d0cc04415f.
4
Construction of Highly Functionalized Piperazinones via Post-Ugi Cyclization and Diastereoselective Nucleophilic Addition.通过 Ugi 后环化和非对映选择性亲核加成构建高功能化的哌嗪酮。
J Org Chem. 2020 Jun 5;85(11):6910-6923. doi: 10.1021/acs.joc.0c00108. Epub 2020 May 12.
5
Cutaneous leishmaniasis a neglected tropical disease: community knowledge, attitude and practices in an endemic area, Northwest Ethiopia.皮肤利什曼病是一种被忽视的热带病：在埃塞俄比亚西北部的一个流行地区的社区知识、态度和实践。
BMC Infect Dis. 2019 Oct 16;19(1):855. doi: 10.1186/s12879-019-4506-1.
6
β-Amino acid derivatives as mitochondrial complex III inhibitors of L. donovani: A promising chemotype targeting visceral leishmaniasis.β-氨基酸衍生物作为 L. donovani 的线粒体复合物 III 抑制剂：一种有前途的针对内脏利什曼病的化学型。
Eur J Med Chem. 2019 Nov 15;182:111632. doi: 10.1016/j.ejmech.2019.111632. Epub 2019 Aug 20.
7
Synthesis, Biological Evaluation, Structure-Activity Relationship, and Mechanism of Action Studies of Quinoline-Metronidazole Derivatives Against Experimental Visceral Leishmaniasis.喹啉-甲硝唑衍生物的合成、生物评价、构效关系及抗实验内脏利什曼病作用机制研究。
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8
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10
Visceral leishmaniasis elimination targets in India, strategies for preventing resurgence.印度内脏利什曼病消除目标，防止复发的策略。
Expert Rev Anti Infect Ther. 2018 Nov;16(11):805-812. doi: 10.1080/14787210.2018.1532790. Epub 2018 Oct 10.

发现2,3-二氢-1-吡咯并[3,4-]喹啉-1-酮衍生物可能作为抗利什曼原虫药物。

Discovery of 2,3-dihydro-1-pyrrolo[3,4-]quinolin-1-one derivatives as possible antileishmanial agents.

作者信息

Seth Anuradha, Ghoshal Anirban, Dewaker Varun, Rani Ankita, Singh Sangh Priya, Dutta Mukul, Katiyar Shivani, Singh Sandeep Kumar, Rashid Mamunur, Wahajuddin Muhammad, Kar Susanta, Srivastava Ajay Kumar

机构信息

Molecular Microbiology and Immunology Division, CSIR-Central Drug Research Institute Lucknow-226031 Uttar Pradesh India

Academy of Scientific and Innovative Research (AcSIR) Ghaziabad-201002 Uttar Pradesh India.

出版信息

RSC Med Chem. 2022 May 11;13(6):746-760. doi: 10.1039/d2md00078d. eCollection 2022 Jun 22.

DOI:10.1039/d2md00078d
PMID:35814931
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9215122/
Abstract

A series of uniquely functionalized 2,3,-dihydro-1-pyyrolo[3,4-]quinolin-1-one derivatives were synthesized in one to two steps by utilizing a post-Ugi modification strategy and were evaluated for antileishmanial efficacy against visceral leishmaniasis (VL). Among the library compounds, compound 5m exhibited potential antileishmanial activity (CC = 65.11 μM, SI = 7.79, anti-amastigote IC = 8.36 μM). antileishmanial evaluation of 5m demonstrated 56.2% inhibition in liver and 61.1% inhibition in spleen parasite burden in infected Balb/c mice (12.5 mg kg, i.p.). pharmacokinetic study ascertained the stability of 5m in both simulated gastric fluid and simulated intestinal fluid. All the active compounds passed the PAINS filter and showed no toxicity in predictions.

摘要

通过采用乌吉反应后修饰策略，在一到两步反应中合成了一系列具有独特功能化的2,3-二氢-1-吡咯并[3,4-c]喹啉-1-酮衍生物，并对其抗内脏利什曼病（VL）的抗利什曼原虫疗效进行了评估。在该化合物库中，化合物5m表现出潜在的抗利什曼原虫活性（CC = 65.11 μM，SI = 7.79，抗无鞭毛体IC = 8.36 μM）。对5m的抗利什曼原虫评估表明，在感染的Balb/c小鼠（12.5 mg/kg，腹腔注射）中，肝脏寄生虫负荷抑制率为56.2%，脾脏寄生虫负荷抑制率为61.1%。药代动力学研究确定了5m在模拟胃液和模拟肠液中的稳定性。所有活性化合物均通过了PAINS筛选，预测显示无毒性。