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Top 10 Most Talked-About Articles on Medicinal Chemistry

Posted on November 21st, 2016 by in Chemistry


Every day, researchers in medicinal chemistry are doing important work in the lab, striving bit by bit to uncover the knowledge that will lead to treatments and potentially even cures for numerous diseases and maladies. Here are some of the most-discussed articles and findings in medicinal chemistry, biological chemistry, and organic chemistry in recent weeks.

1. European Journal of Medicinal Chemistry – Multifunctional diamine AGE/ALE inhibitors with potential therapeutical properties against Alzheimer’s disease 

As a result of this investigation, two compounds are found to have promising therapeutic potential in the treatment of Alzheimer’s disease.

2. Bioorganic Chemistry – Design, synthesis and biological evaluation of coumarin derivatives as novel acetylcholinesterase inhibitors that attenuate H2O2-induced apoptosis in SH-SY5Y cells 

The findings of this study could have implications in the future development of therapy for Alzheimer’s disease.

3. European Journal of Medicinal Chemistry – Synthesis and biological evaluation of novel ferrocene-naphthoquinones as antiplasmodial agents

In this study, 11 new 3-(ferrocenylmethyl)-1,4-naphthoquinone derivatives were synthesized with an on-water methodology.

4. Bioorganic & Medicinal Chemistry Letters – Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: Developing a structure–activity relationship 

In this report, a series of hydroxypyrone- and hydroxythiopyrone-based MMPi with aryl backbones at the 2-, 5-, and 6-positions of the hydroxypyrone ring have been synthesized.

5. European Journal of Medicinal Chemistry – Inhibitory effects of 5-benzylidene barbiturate derivatives on mushroom tyrosinase and their antibacterial activities 

The results of this study demonstrated that some compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM).

6. Bioorganic & Medicinal Chemistry Letters – Synthesis and evaluation of 5-benzylidene(thio)barbiturate-β-d-glycosides as mushroom tyrosinase inhibitors 

This study’s findings demonstrated that most of the compounds had more potent inhibitory activities than arbutin (IC50 8.4 mmol/L), with compound 12b found to be the most potent inhibitor with an IC50 value of 0.05 mmol/L.

7. Bioorganic & Medicinal Chemistry – Design, synthesis and biological evaluation of hydroxy- or methoxy-substituted 5-benzylidene(thio) barbiturates as novel tyrosinase inhibitors 

The results here reveal that several compounds had more potent tyrosinase inhibitory activities than the widely-used tyrosinase inhibitor kojic acid (IC50 = 18.25 μM). 3′,4′-dihydroxylated 1e in particular was found to be the most potent inhibitor with IC50 value of 1.52 μM.

8. Bioorganic & Medicinal Chemistry Letters – Design and synthesis of aloe-emodin derivatives as potent anti-tyrosinase, antibacterial and anti-inflammatory agents 

This study comes from a trio of researchers at the Department of Biology and Chemical Engineering at Shaoyang University in China.

9. European Journal of Medicinal Chemistry – In silico and in vitro validation of serine hydroxymethyltransferase as a chemotherapeutic target of the antifolate drug pemetrexed 

Here the interaction mode of SHMT with pemetrexed, an antifolate drug inhibiting several enzymes involved in folate-dependent biosynthetic pathways, is assessed.

10. Carbohydrate Research – Carbohydrate CuAAC click chemistry for therapy and diagnosis 

This review summarizes the impressive progress that was made over a recent five-year period in CuI-catalyzed azide-alkyne 1,3-dipolar cycloaddition CuAAC “click chemistry” of carbohydrate derivatives, specifically in the context of potential therapeutic and diagnostic tool development.


All opinions shared in this post are the author’s own.

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