Synthesis and in vitro activity of novel quaternary ammonium carbapenems: 2-Pyridiniopropyl and 1-pyridinioethyl carbapenems.
- 1 January 1992
- journal article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 45 (6) , 940-953
- https://doi.org/10.7164/antibiotics.45.940
Abstract
The synthesis of new carbapenems having either a pyridiniopropyl group at the 2-position or a pyridinioethyl group at the 1-position is described, along with the preparation of their corresponding hydroxy and acetoxy analogs. The antibacterial activity, susceptibility to dehydropeptidase-I (DHP-I) enzyme and chemical stability of these new carbapenems are also reported. 2-Pyridiniopropyl-carbapenem 4 was found to possess excellent antibacterial activity. It was more stable chemically and less susceptible to the DHP-I enzyme than the thio analog 3. 1-Pyridinioethylcarbapenem 5 showed significantly reduced antibacterial activity as compared to 2-pyridiniopropylcarbapenem 4.Keywords
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