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A computational insight into acetylcholinesterase inhibitory activity of a new lichen depsidone
(Taylor & Francis Ltd, 2015)
Acetylcholinesterase (AChE) inhibitors are yet the best drugs currently available for the management of Alzheimer's disease. The recent phytochemical investigation has led to the isolation of a new depsidone 1 with moderate ...
Design strategies, structures and molecular interactions of small molecule src inhibitors
(Bentham Science Publ Ltd, 2016)
In recent years, several small molecules approved by FDA for clinical studies are promising anti-cancer agent. Among the kinases, Abelson Leukaemia (Abl), sarcoma (Src), epidermal growth factor receptor (EGFR) and vascular ...
Synthesis, structure elucidation and biological activities of some novel 4(3H)-quinazolinones as anti-biofilm agents
(Bentham Science Publishers, 2019)
Background: Pseudomonas aeruginosa is an opportunistic pathogen that causes chronic infections in immunocompromised patients. The inhibition of Quorum Sensing (QS) system has been recognized as an attractive strategy for ...
In vitro antibacterial and antifungal activity and computational evaluation of novel indole derivatives containing 4-substituted piperazine moieties
(Bentham Science Publ Ltd, 2018)
Background: Lack of specificity and occurence of resistance to current antibacterial and antifungal agents are major shortcomings for the treatment of microbial diseases. Finding novel antimicrobial agents is therefore ...
SAHAquines, novel hybrids based on SAHA and primaquine motifs, as potential cytostatic and antiplasmodial agents
(ChemPubSoc Europe, 2018)
We report the synthesis of SAHAquines and related primaquine (PQ) derivatives. SAHAquines are novel hybrid compounds that combine moieties of suberoylanilide hydroxamic acid (SAHA), an anticancer agent with weak antiplasmodial ...
Identification of bichalcones as natural product sirtuin inhibitors by virtual screening and in vitro testing
(Amer Chemical Soc, 2018)
Sirtuins are nicotinamide adenine dinucleotide (NAD+ )-dependent class III histone deacetylases, which have been linked to the pathogenesis of numerous diseases, including HIV, metabolic disorders, neurodegeneration and ...
Synthesis, characterization, preliminary SAR and molecular docking study of some novel substituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives as antifungal agents
(Springer Birkhauser, 2017)
The aim of this study was to synthesize imidazo [2,1-b] [1,3,4] thiadiazole derivatives, characterize them with various spectroscopic methods and investigate their antifungal activities. 2- Imino - 1,3,4 - thiadiazole ...
The effects of 1,3,5-trisubstituted indole derivatives on cell growth, apoptosis and MMP-2/9 mRNA expression of MCF-7 human breast cancer cells
(Bentham Science Publ Ltd, 2017)
Background: Matrix metalloproteinases are known as extracellular matrix degrading enzymes and have important role on tumor progression. Objective: This study reports the effects of 1,3,5-trisubstituted indole derivatives ...
Synthesis and antioxidant activity of indole derivatives containing 4-substituted piperazine moieties
(Bentham Science Publ Ltd, 2017)
Background: Oxidative stress caused by reactive oxygen species (ROS) plays a significant role in many human disorder such as cancer, rheumatoid arthritis, atherosclerosis, stroke, neurodegeneration, and diabetes as well ...
Towards more effective acetylcholinesterase inhibitors: a comprehensive modelling study based on human acetylcholinesterase protein–drug complex
(Taylor and Francis Ltd., 2019)
Alzheimer's disease is a progressive neurodegenerative disorder and as the exact cause of the disease remains unknown, it still has no cure to date. Due to the fact that, until recently, there has been no crystal structure ...
