Compound ID | 546

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CI-990

Synonym(s): PD 131112 (Prodrug of PD 131628)  |  PD 131628

Class: Fluoroquinolone

Spectrum of activity: Gram-positive  &  Gram-negative
Details of activity: Mice infected with P. aeruginosa were treated with a number of different quinolones. 50 of 60 mice recovered with the treatment of CI-990 whereas 54 of 60 mice recovered from lomefloxacin; more active against Gram positives than Gram negatives; more active against Gram positives than Gram negatives
Description: Brook I and Ledney GD. Quinolone therapy in the prevention of endogenous and exogenous infection after irradiation. 32nd-Intersci-Conf-Antimicrobial-Agents-Chemother 1992; 239.
Institute where first reported: Pfizer, USA; Parke-Davis Pharmaceutical
Year first mentioned: 1990
Highest developmental phase: Preclinical
Development status: Experimental
Reason Dropped: Most of the early potent Gram positive favoring fluoroquinolones showed genotoxicity (LS)
Chemical structure(s):
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Molecular weight: 332.33
Iso. SMILES: C1CN(C[C@H]1N)C2=C(C=C3C(=O)C(=CN(C3=N2)C4CC4)C(=O)O)F
InChI Key: MUKSDTOOLRNSIO-QMMMGPOBSA-N
Can. SMILES: C1CC1N2C=C(C(=O)C3=C2N=C(C(=C3)F)N4CC[C@@H](C4)N)C(=O)O
InChI: InChI=1S/C16H17FN4O3/c17-12-5-10-13(22)11(16(23)24)7-21(9-1-2-9)14(10)19-15(12)20-4-3-8(18)6-20/h5,7-9H,1-4,6,18H2,(H,23,24)/t8-/m0/s1
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/72448
Citations:
  • https://pubmed.ncbi.nlm.nih.gov/17588022/
  • https://journals.asm.org/doi/10.1128/aac.35.1.141

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