Ryan, Michael C.; Kim, Eunjung; Cao, Xufeng; Reichard, Walter; Ogorek, Tyler J.; Das, Pronay; Jonsson, Colleen B.; Baudry, Jerome; Chung, Donghoon; Golden, Jennifer E. published the artcile< Piperazinobenzodiazepinones: New Encephalitic Alphavirus Inhibitors via Ring Expansion of 2-Dichloromethylquinazolinones>, Related Products of 112-63-0, the main research area is piperazinobenzodiazepinone preparation antialphaviral; dichloromethylquinazolinone ring expansion.
While expanding the pharmacophoric model of antialphaviral amidines prepared via a quinazolinone rearrangement, we discovered that diamine-treated, 2-dihalomethylquinolinones unexpectedly afforded ring-expanded piperazine-fused benzodiazepinones I [R1 = NO2, F, CN; R2 = H, NO2; R3 = H, Br, 2-morpholinyl, etc.; R4 = Me, Bn; R5 = Me, cyclohexyl, Bn; Ar = Ph, 4-MeOC6H4, 4-FC6H4, etc.]. Notably, this new chemotype showed potent, submicromolar inhibition of virus-induced cell death, >7-log reduction of viral yield, and tractable structure-activity relationships across both viruses. Antiviral activity was confirmed in primary human neuronal cells. A mechanistic rationale for product formation is proposed, and key structural elements were comparatively modeled between a similarly substituted antiviral amidine and piperazinobenzodiazepinone prototypes to guide future antiviral development.
ACS Medicinal Chemistry Letters published new progress about Alphavirus (inhibitors). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.
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