348086-71-5

BAY 57-1293 is a potent inhibitor of herpes simplex virus (HSV) that target the virus helicase primase complex.

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]

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[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.