Straightforward Enantioselective Synthesis of (+)‐Ancistrofuran.

Palombo, Elie; Audran, Gérard; Monti, H.

doi:10.1002/chin.200603203

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2015

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“…14 was achieved in a two-step process via the reduction of the corresponding thionocarbonate ester derivative of 9. 22 Ester 12 was the methyl ester derivative of 9. The biological results showed that, nitrile 8 surprisingly exhibited no inhibitory activities (IC 50 > 10 μM and EC 50 > 100 μM) (Table 1).…”

Section: ■ Results and Discussionsupporting

confidence: 65%

Cyanohydrin as an Anchoring Group for Potent and Selective Inhibitors of Enterovirus 71 3C Protease

et al. 2015

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Cyanohydrin derivatives as enterovirus 71 (EV71) 3C protease (3C(pro)) inhibitors have been synthesized and assayed for their biochemical and antiviral activities. Compared with the reported inhibitors, cyanohydrins (1S,2S,2'S,5S)-16 and (1R,2S,2'S,5S)-16 exhibited significantly improved activity and attractive selectivity profiles against other proteases, which were a result of the specific interactions between the cyanohydrin moiety and the catalytic site of 3C(pro). Cyanohydrin as an anchoring group with high selectivity and excellent inhibitory activity represents a useful choice for cysteine protease inhibitors.

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Section: ■ Results and Discussionsupporting

confidence: 65%