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10.1002/cmdc.201000306

http://scihub22266oqcxt.onion/10.1002/cmdc.201000306
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20967819!7162373!20967819
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suck abstract from ncbi


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pmid20967819      ChemMedChem 2010 ; 5 (12): 2072-8
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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.
  • |Antiviral Agents/chemical synthesis/*chemistry/pharmacology[MESH]
  • |Benzamides/chemical synthesis/*chemistry/pharmacology[MESH]
  • |Crystallography, X-Ray[MESH]
  • |Drug Design[MESH]
  • |Imides/chemical synthesis/*chemistry/pharmacology[MESH]
  • |Isoindoles/chemical synthesis/chemistry/pharmacology[MESH]
  • |Molecular Conformation[MESH]
  • |Polycyclic Compounds/*chemistry[MESH]
  • |Structure-Activity Relationship[MESH]


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