63469-19-2
Chemical Structure
Apalcillin
Synonym(s): PC-904
- CAS No.: 63469-19-2
- Formula:C25H23N5O6S
- Molecular Weight:521.55
IUPAC Name: (2S,5R,6R)-6-((R)-2-(4-hydroxy-1,5-naphthyridine-3-carboxamido)-2-phenylacetamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
InChIKey: XMQVYNAURODYCQ-SLFBBCNNSA-N
SMILES: O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC([C@H](NC(C3=C(O)C4=NC=CC=C4N=C3)=O)C5=CC=CC=C5)=O)N1C2=O)O
Biological Activity: Apalcillin (PC-904) in combination with Ro 48-1220, a penam sulfone β-lactamase inhibitor, demonstrated broad-spectrum activity against gram-negative aerobic and anaerobic bacteria, excluding Klebsiella oxytoca. It exhibited potent activity against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae, with effective MICs (11 μg/mL). The combination also inhibited Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter species at low MICs (0.25 to 4 μg/mL). However, its efficacy against oxacillin-resistant staphylococci and certain gram-positive organisms was limited. Apalcillin/Ro 48-1220 showed comparable efficacy to piperacillin/tazobactam against some extended-spectrum β-lactamase-producing Escherichia coli but was less effective against SHV-type β-lactamases[1].
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Apalcillin | Apalcillin (PC-904) in combination with Ro 48-1220, a penam sulfone β-lactamase inhibitor, demonstrated broad-spectrum activity against gram-negative aerobic and anaerobic bacteria, excluding Klebsiella oxytoca. It exhibited potent activity against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae, with effective MICs (11 μg/mL). The combination also inhibited Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter species at low MICs (0.25 to 4 μg/mL). However, its efficacy against oxacillin-resistant staphylococci and certain gram-positive organisms was limited. Apalcillin/Ro 48-1220 showed comparable efficacy to piperacillin/tazobactam against some extended-spectrum β-lactamase-producing Escherichia coli but was less effective against SHV-type β-lactamases. | |||||||||||||||||||||
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