A helicase-primase inhibitor
BAY 57-1293 is a potent and safe inhibitor of HSV helicase-primase with IC50 value of 12nM [1].
BAY 57-1293 displays anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. In the plaque reduction assay and the conventional cytopathogenicity assay, BAY 57-1293 shows IC50 values of 0.01-0.02μM and 0.01-0.03μM, respectively. Besides that, BAY 57-1293 is active at an IC50 value of 10nM–30nM against all clinical isolates of HSV-1 and HSV-2. Furthermore, BAY 57-1293 is active in vivo. The oral administration of BAY 57-1293 shows 10-fold more potent than valacyclovir in a murine model of disseminated herpes infection. In a rat lethal challenge model, BAY 57-1293 exerts profound antiviral activity without toxic effects. [1, 2]
参考文献:
[1] Kleymann G, Fischer R, Betz U A K, et al. New helicase-primase inhibitors as drug candidates for the treatment of herpes simplex disease. Nature medicine, 2002, 8(4): 392-398.
[2] Betz U A K, Fischer R, Kleymann G, et al. Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293. Antimicrobial agents and chemotherapy, 2002, 46(6): 1766-1772.
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