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2022 ◽  
Vol 372 ◽  
pp. 131214
Author(s):  
Fernanda de Oliveira ◽  
Inês L.D. Rocha ◽  
Diana Cláudia Gouveia Alves Pinto ◽  
Sónia P.M. Ventura ◽  
André Gonzaga dos Santos ◽  
...  
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ARKIVOC ◽  
2022 ◽  
Vol 2022 (2) ◽  
Author(s):  
Shushanik Shamir Dashyan ◽  
Ruzanna Garnik Paronikyan ◽  
Suren Sergey Mamyan ◽  
Ervand Garnik Paronikyan

Marine Drugs ◽  
2022 ◽  
Vol 20 (1) ◽  
pp. 75
Author(s):  
Elisabete Lima ◽  
Jorge Medeiros

The incidence of neurodegenerative diseases, such as Alzheimer’s disease (AD), increases continuously demanding the urgent development of anti-Alzheimer’s agents. Marine organisms (MO) have to create their own defenses due to the adverse environment where they live and so synthesize several classes of compounds, such as akaloids, to defend themselves. Therefore, the identification of marine natural products with neuroprotective effects is a necessity. Being that AD is not only a genetic but also an environmental complex disease, a treatment for AD remains to discover. As the major clinical indications (CI) of AD are extracellular plaques formed by β-amyloid (Aβ) protein, intracellular neurofibrillary tangles (NFTs) formed by hyper phosphorylated τ-protein, uncommon inflammatory response and neuron apoptosis and death caused by oxidative stress, alkaloids that may decrease CI, might be used against AD. Most of the alkalolids with those properties are derivatives of the amino acid tryptophan mainly with a planar indole scaffold. Certainly, alkaloids targeting more than one CI, multitarget-directed ligands (MTDL), have the potential to become a lead in AD treatment. Alkaloids to have a maximum of activity against CI, should be planar and contain halogens and amine quaternization.


Science ◽  
2022 ◽  
Vol 375 (6577) ◽  
pp. 161-167
Author(s):  
Julien Sourimant ◽  
Carolin M. Lieber ◽  
Megha Aggarwal ◽  
Robert M. Cox ◽  
Josef D. Wolf ◽  
...  

Preparing antiviral defenses Antiviral drugs are an important tool in the battle against COVID-19. Both remdesivir and molnupiravir, which target the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) polymerase, were first developed against other RNA viruses. This highlights the importance of broad-spectrum antivirals that can be rapidly deployed against related emerging pathogens. Sourimant et al . used respiratory syncytial virus (RSV) as a primary indication in identifying further drugs that target the polymerase enzyme of RNA viruses. The authors explored derivatives of molnupiravir and identified 4′ fluorouridine (EIDD-2749) as an inhibitor of the polymerase of RSV and SARS-CoV-2. This drug can be delivered orally and was effective against RSV in mice and SARS-CoV-2 in ferrets. —VV


2022 ◽  
Vol 7 (1) ◽  
pp. 123-128
Author(s):  
Tatiana Ďurčeková ◽  
Ján Mocák ◽  
Jozef Lehotay ◽  
Jozef Čižmárik

Anaesthetical activity of 113 morpholinoethyl-, piperidinoethyl-, piperidinopropyl- and azepanoethyl- ester derivatives of alkoxyphenylcarbamic acid was characterized by several chemometrical techniques. The surface anaesthetical activity, A, and the infiltration anaesthetical activity, B, were correlated to lipophilicity, (expressed by the logarithm of the HPLC retention factor, log k), the length of the side alkoxy chain (represented by the number n of carbon atoms), molar mass M as well as the ester type. Principal component analysis and cluster analysis were used for predicting both types of the anaesthetic activity of the alkoxyphenylcarbamic acid esters.


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