Compound ID | 387

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CGP-31608

Class: Beta-lactam (penem)

Spectrum of activity: Gram-positive & Gram-negative
Details of activity: This was less active against MRSA and Pseudomonas than imipenem. Used against MRSA and CAP
Institute where first reported: Novartis, Switzerland
Year first mentioned: 1986
Highest developmental phase: Preclinical
Development status: Inactive
Reason Dropped: The dosage tested in phase I was suggested to be administered 3 or 4 times daily. This inconvenience could be the reason of discontinuation (1). It also had a very short half life (2) Additionally, this appeared to be less potent than ritipenem
Chemical structure(s):
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Molecular weight: 244.27
Iso. SMILES: C[C@H]([C@@H]1[C@@H]2N(C1=O)C(=C(S2)CN)C(=O)O)O
InChI Key: RXCNILVLOHRALM-UWBRJAPDSA-N
Can. SMILES: C[C@H]([C@H]1C(=O)N2C(=C(CN)S[C@H]12)C(=O)O)O
InChI: InChI=1S/C9H12N2O4S/c1-3(12)5-7(13)11-6(9(14)15)4(2-10)16-8(5)11/h3,5,8,12H,2,10H2,1H3,(H,14,15)/t3-,5+,8-/m1/s1
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/129935
Guide to Pharmacology: CGP-31608
Citations:
  • http://jac.oxfordjournals.org/content/20/2/179.full.pdf
  • http://jac.oxfordjournals.org/content/21/1/85.full.pdf+html
  • https://books.google.co.uk/books?id=GgPoCAAAQBAJ&pg=PA308&lpg=PA308&dq=LY173013&source=bl&ots=spuNwNoFKJ&sig=jTjiVJirHIj6GLgqaVt76y91ThA&hl=en&sa=X&ei=4ct2Vc6bLMOBU_e3gHA&ved=0CDcQ6AEwBg#v=onepage&q=LY173013&f=false

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