Design, synthesis and biological evaluation of a hybrid compound of berberine and magnolol for improvement of glucose and lipid metabolism

RSC Advances ◽  
2016 ◽  
Vol 6 (85) ◽  
pp. 81924-81931 ◽  
Author(s):  
Yan Li ◽  
Xiao Yuan ◽  
Xianglu Rong ◽  
Ying Gao ◽  
Zhibin Qiu ◽  
...  
Keyword(s):  
Lipid Metabolism ◽  
Research And Development ◽  
Biological Evaluation ◽  
New Drugs ◽  
Main Task ◽  
Hybrid Compound ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Glucose And Lipid Metabolism ◽  
Synthesis And Biological Evaluation

The discovery and structural optimization of lead compounds is the main task in the research and development of new drugs.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

scholarly journals Design Synthesis and Biological Evaluation of NovelN-Nitro Acid Amide Derivatives as Lead Compounds of Herbicide

2016 ◽  
Vol 2016 ◽  
pp. 1-6
Author(s):  
Xiaojuan Qi ◽  
Wenjie Tang ◽  
Shan Gao ◽  
Min Gao ◽  
Changshui Chen ◽  
...  
Keyword(s):  
Acid Amide ◽  
Biological Evaluation ◽  
Herbicidal Activity ◽  
Acetohydroxyacid Synthase ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Amide Derivatives ◽  
Sorghum Sudanense ◽  
Synthesis And Biological Evaluation

A series ofN-nitro acid amide derivatives compounds were synthesized based on the active site of target acetohydroxyacid synthase (AHAS, EC: 2.2.1.6) enzyme. All the structures of newly prepared compounds were thoroughly characterized by satisfied IR and1H NMR spectra. The IC50values against AHAS enzyme and EC50values for herbicidal activity againstAmaranthus mangostanus L.andSorghum sudanenseof all synthesized target compounds were determined. The compoundsII-10,II-21, andII-22with IC50values of 7.09 mg/L, 9.07 mg/L, and 9.11 mg/L and the compoundsII-8andII-22with EC50values of 9.87 mg/L and 19.88 mg/L against root ofAmaranthus mangostanus L.andSorghum sudanensewere illustrated, respectively. Meanwhile, the possible reasons for the lower activity of compounds were analyzed by molecular docking prediction.

Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents

2021 ◽  
Author(s):  
Guddeti Dileep Kumar ◽  
Bandi Siva ◽  
Sravanthi Vadlamudi ◽  
Surendar Reddy Bathula ◽  
Hashnu Dutta ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Traditional Medicinal Plants ◽  
Aloe Emodin ◽  
Synthesis And Biological Evaluation

In connection with our continuous efforts to generate new derivatives from lead compounds isolated from traditional medicinal plants, a series of aloe-emodin derivatives were synthesized and assessed for potential anticancer activity against a panel of cancer cell lines.

scholarly journals Novel Carboline Derivatives as Potent Antifungal Lead Compounds: Design, Synthesis, and Biological Evaluation

2014 ◽  
Vol 5 (5) ◽  
pp. 506-511 ◽  
Author(s):  
Shengzheng Wang ◽  
Yan Wang ◽  
Wei Liu ◽  
Na Liu ◽  
Yongqiang Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

The Discovery and Development of Oxalamide and Pyrrole Small Molecule Inhibitors of gp120 and HIV Entry - A Review

2019 ◽  
Vol 19 (18) ◽  
pp. 1650-1675 ◽  
Author(s):  
Damoder Reddy Motati ◽  
Dilipkumar Uredi ◽  
E. Blake Watkins
Keyword(s):  
Small Molecule ◽  
Viral Entry ◽  
Biological Evaluation ◽  
New Drugs ◽  
Design Synthesis ◽  
Mortality And Morbidity ◽  
Glycoprotein Gp120 ◽  
Hiv Entry ◽  
Immunodeficiency Syndrome ◽  
Hiv 1

Human immunodeficiency virus type-1 (HIV-1) is the causative agent responsible for the acquired immunodeficiency syndrome (AIDS) pandemic. More than 60 million infections and 25 million deaths have occurred since AIDS was first identified in the early 1980s. Advances in available therapeutics, in particular combination antiretroviral therapy, have significantly improved the treatment of HIV infection and have facilitated the shift from high mortality and morbidity to that of a manageable chronic disease. Unfortunately, none of the currently available drugs are curative of HIV. To deal with the rapid emergence of drug resistance, off-target effects, and the overall difficulty of eradicating the virus, an urgent need exists to develop new drugs, especially against targets critically important for the HIV-1 life cycle. Viral entry, which involves the interaction of the surface envelope glycoprotein, gp120, with the cellular receptor, CD4, is the first step of HIV-1 infection. Gp120 has been validated as an attractive target for anti-HIV-1 drug design or novel HIV detection tools. Several small molecule gp120 antagonists are currently under investigation as potential entry inhibitors. Pyrrole, piperazine, triazole, pyrazolinone, oxalamide, and piperidine derivatives, among others, have been investigated as gp120 antagonist candidates. Herein, we discuss the current state of research with respect to the design, synthesis and biological evaluation of oxalamide derivatives and five-membered heterocycles, namely, the pyrrole-containing small molecule as inhibitors of gp120 and HIV entry.

Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties

2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Hybrid Molecules ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of
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