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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 ...
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 ...
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 ...
Elastin is heterogeneously cross-linked
(Amer Soc Biochemistry Molecular Biology, 2018)
Elastin is an essential vertebrate protein responsible for the elasticity of force-bearing tissues such as those of the lungs, blood vessels, and skin. One of the key features required for the exceptional properties of ...
An integrated approach towards the development of novel antifungal agents containing thiadiazole: synthesis and a combined similarity search, homology modelling, molecular dynamics and molecular docking study
(Springeropen, 2018)
BackgroundThis study aims to synthesise and characterise novel compounds containing 2-amino-1,3,4-thiadiazole and their acyl derivatives and to investigate antifungal activities. Similarity search, molecular dynamics and ...
Synthesis, structural characterization, and antiproliferative/cytotoxic effects of a novel modified poly (maleic anhydride-co-vinyl acetate) doxorubicin conjugate
(Springer, 2017)
Drug carrier, poly(maleic anhydride-co-vinyl acetate) (MAVA or poly[MA-co-VA]) copolymer, was traditionally synthesized by free radical chain polymerization reaction, in methyl ethyl ketone (MEK) organic media at 80 A ...
Increased potency and selectivity for group III metabotropic glutamate receptor agonists binding at dual sites
(Amer Chemical Soc, 2018)
A group III metabotropic glutamate (mGlu) receptor agonist (PCEP) was identified by virtual HTS. This orthosteric ligand is composed by an L-AP4-derived fragment that mimics glutamate and a chain that binds into a neighboring ...
Design, synthesis, SAR and molecular modeling studies of novel imidazo [2,1-b][1,3,4] thiadiazole derivatives as highly potent antimicrobial agents
(WILEY, 2018)
In this study, a novel series of phenyl substituted imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized, characterized and explored for antibacterial activity against Gram-negative Escherichia coli, Gram-positive ...
