Cadazolid

Cadazolid is an oxazolidinone-type antibiotic that has activity against a panel of C. difficile strains, including those resistant to fluoroquinolones and linezolid (Cay-15012, MICs = 0.125-0.5 µg/ml). It inhibits toxin A and B formation in stationary-phase cultures and spore formation in late exponential cultures of the toxigenic C. difficile strain ATCC 9689. Cadazolid inhibits C. difficile protein synthesis (IC50s = 0.08-0.31 µg/ml) without affecting nucleic acid or cell wall synthesis (IC50s = 12-18.6 and >32 µg/ml, respectively). In vivo, cadazolid (1 and 10 mg/kg) increases survival in a mouse model of C. difficile-associated diarrhea (CDAD). It also confers 100% survival in a hamster model of CDAD when administered at doses greater than 3 mg/kg.Formal Name: 1-cyclopropyl-6-fluoro-7-[4-[[2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-3-oxazolidinyl]phenoxy]methyl]-4-hydroxy-1-piperidinyl]-1-4-dihydro-4-oxo-3-quinolinecarboxylic acid. CAS Number: 1025097-10-2. Synonyms: ACT-179811. Molecular Formula: C29H29F2N3O8. Formula Weight: 585.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml, DMSO: 20 mg/ml. lambdamax: 240, 285 nm. SMILES: FC1=C(N2CCC(COC3=C(F)C=C(N4C[C@H](CO)OC4=O)C=C3)(O)CC2)C=C5C(C(C(C(O)=O)=CN5C6CC6)=O)=C1. InChi Code: InChI=1S/C29H29F2N3O8/c30-21-10-19-23(33(16-1-2-16)13-20(26(19)36)27(37)38)11-24(21)32-7-5-29(40,6-8-32)15-41-25-4-3-17(9-22(25)31)34-12-18(14-35)42-28(34)39/h3-4,9-11,13,16,18,35,40H,1-2,5-8,12,14-15H2,(H,37,38)/t18-/m1/s1. InChi Key: XWFCFMXQTBGXQW-GOSISDBHSA-N.