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Deprecated: Implicit conversion from float 219.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ChemMedChem 2010 ; 5 (12): 2072-8 Nephropedia Template TP
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Polycyclic N-benzamido imides with potent activity against vaccinia virus #MMPMID20967819
Torres E; Duque MD; Camps P; Naesens L; Calvet T; Font-Bardia M; Vazquez S
ChemMedChem 2010[Dec]; 5 (12): 2072-8 PMID20967819show ga
The synthesis and antiviral activity of a series of novel polycyclic analogues of the orthopoxvirus egress inhibitor tecovirimat (ST-246) is presented. Several of these compounds display sub-micromolar activity against vaccinia virus, and were more potent than cidofovir (CDV). The more active compounds were about 10-fold more active than CDV, with minimum cytotoxic concentrations above 100 muM. Chemical manipulations of the two carbon-carbon double bonds present in the compounds were carried out to further explore the structure-activity relationships of these new polycyclic imides. Hydrogenation of the two carbon-carbon double bonds decreases antiviral activity, whereas either cyclopropanation or epoxidation of the double bonds fully eliminates the antiviral activity.