Next Article in Journal
On the Use of Iron in Organic Chemistry
Next Article in Special Issue
Composition and Orientation of the Core Region of Novel HIV-1 Entry Inhibitors Influences Metabolic Stability
Previous Article in Journal
Quinolone Complexes with Lanthanide Ions: An Insight into their Analytical Applications and Biological Activity
Previous Article in Special Issue
Quinolinecarboxamides Inhibit the Replication of the Bovine Viral Diarrhea Virus by Targeting a Hot Spot for the Inhibition of Pestivirus Replication in the RNA-Dependent RNA Polymerase
Open AccessCommunication

The Evolution of Pleconaril: Modified O-Alkyl Linker Analogs Have Biological Activity towards Coxsackievirus B3 Nancy

1
Saint-Petersburg Pasteur Institute, Mira str., 14, 197101 Saint Petersburg, Russia
2
Bach Institute of Biochemistry, Research Center of Biotechnology of the Russian Academy of Sciences, Leninsky prospect, 33, build. 2, 119071 Moscow, Russia
3
Collaborations Pharmaceuticals, Inc., 840 Main Campus Drive, Lab 3510, Raleigh, NC 27606, USA
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2020, 25(6), 1345; https://doi.org/10.3390/molecules25061345
Received: 10 February 2020 / Revised: 11 March 2020 / Accepted: 13 March 2020 / Published: 16 March 2020
(This article belongs to the Special Issue Antiviral Agents)
Coxsackieviruses type B are one of the most common causes of mild upper respiratory and gastrointestinal illnesses. At the time of writing, there are no approved drugs for effective antiviral treatment for Coxsackieviruses type B. We used the core-structure of pleconaril, a well-known antienteroviral drug candidate, for the synthesis of novel compounds with O-propyl linker modifications. Some original compounds with 4 different linker patterns, such as sulfur atom, ester, amide, and piperazine, were synthesized according to five synthetic schemes. The cytotoxicity and bioactivity of 14 target compounds towards Coxsackievirus B3 Nancy were examined. Based on the results, the values of 50% cytotoxic dose (CC50), 50% virus-inhibiting dose (IC50), and selectivity index (SI) were calculated for each compound. Several of the novel synthesized derivatives exhibited a strong anti-CVB3 activity (SI > 20 to > 200). These results open up new possibilities for synthesis of further new selective anticoxsackievirus compounds. View Full-Text
Keywords: coxsackievirus; coxsackievirus B3 Nancy; viral myocarditis; antivirals; pleconaril coxsackievirus; coxsackievirus B3 Nancy; viral myocarditis; antivirals; pleconaril
Show Figures

Graphical abstract

MDPI and ACS Style

Volobueva, A.; Egorova, A.; Galochkina, A.; Ekins, S.; Zarubaev, V.; Makarov, V. The Evolution of Pleconaril: Modified O-Alkyl Linker Analogs Have Biological Activity towards Coxsackievirus B3 Nancy. Molecules 2020, 25, 1345.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop