Carboxamide: New Potent Antiviral Against Cytomegalovirus

N-benzyl hydroxypyridone carboxamide could be the novel potent antiviral hit (8a) inhibiting Human Cytomegalovirus (HCMV) in submicromolar range.

N-benzyl hydroxypyridone carboxamide could be the novel potent antiviral agent inhibiting Human Cytomegalovirus (HCMV) in submicromolar range.

Researchers describe the structure–activity relationship (SAR) for 8a, and the characterization of potent analogs for cytotoxicity/cytostatic property, the preliminary mechanism of action, and the absorption, distribution, metabolism and excretion (ADME) properties in the new study.

‘New research validates N-benzyl hydroxypyridone carboxamide as a viable agent for potent and mechanistically distinct antivirals against HCMV.’
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It revealed pharmacophore features adding optimal antiviral profile, including the 5-OH, the N-1 benzyl, at least one –CH2− in the linker, and a di-halogen substituted phenyl ring in the amide moiety.

Various analogs were found with sub-micromolar antiviral potency and good selectivity index. The preliminary mechanism of action characterization used a pUL89-C biochemical endonuclease assay, a virus entry assay, a time-of-addition assay, and a compound withdrawal assay.

ADME profiling measuring aqueous solubility, plasma and liver microsomal stability, and parallel artificial membrane permeability assay (PAMPA) permeability demonstrated largely favorable drug-like properties.

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These studies validate the N-benzyl hydroxypyridone carboxamide as a viable chemotype for potent and mechanistically distinct antivirals against HCMV.

Source-Medindia