Synthesis and biological evaluation of a new substituted 4-carboxy benzamide derivative to provide new therapeutic strategy for diabetes mellitus

2018 ◽  
Vol 07 ◽  
Author(s):  
Sandhya Jain ◽  
Ashish Patel
Keyword(s):  
Diabetes Mellitus ◽  
Therapeutic Strategy ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Hydroxylated Monocarbonyl Curcumin Derivatives as Potential Inducers of Neprilysin Activity

Biomedicines ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 955
Author(s):  
Dimitris Matiadis ◽  
See-Ting Ng ◽  
Eric H.-L. Chen ◽  
Georgia Nigianni ◽  
Veroniki P. Vidali ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Therapeutic Strategy ◽  
Specific Inhibitor ◽  
Biological Evaluation ◽  
Lead Compound ◽  
Cleavage Activity ◽  
Curcumin Derivatives ◽  
Aβ Clearance ◽  
Activity Enhancement ◽  
Synthesis And Biological Evaluation

Background: Alzheimer’s disease (AD) involves impairment of Aβ clearance. Neprilysin (NEP) is the most efficient Aβ peptidase. Enhancement of the activity or expression of NEP may provide a prominent therapeutic strategy against AD. Aims: Ten hydroxylated monocarbonyl curcumin derivatives were designed, synthesized and evaluated for their NEP upregulating potential using sensitive fluorescence-based Aβ digestion and inhibition assays. Results: Compound 4 was the most active one, resulting in a 50% increase in Aβ cleavage activity. Cyclohexanone-bearing derivatives exhibited higher activity enhancement compared to their acetone counterparts. Inhibition experiments with the NEP-specific inhibitor thiorphan resulted in dramatic cleavage reduction. Conclusion: The increased Aβ cleavage activity and the ease of synthesis of 4 renders it an extremely attractive lead compound.

Design, synthesis and biological evaluation of novel pteridinone derivatives possessing a sulfonyl moiety as potent dual inhibitors of PLK1 and BRD4

2021 ◽  
Author(s):  
Fei Chen ◽  
Yu Wang ◽  
Zhanfeng Gao ◽  
Shihui Wang ◽  
Jiuyu Liu ◽  
...  
Keyword(s):  
Single Molecule ◽  
Therapeutic Strategy ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Effective Therapeutic Strategy ◽  
Dual Inhibitors ◽  
Simultaneous Inhibition ◽  
Synthesis And Biological Evaluation

The simultaneous inhibition of PLK1 and BRD4 by a single molecule could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and...

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.

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