Inhibition of bacterial plasmid replication by stereoselective binding by tricyclic psychopharmacons

J. Molnár, M. Gálfi, A. Lozsa, M. J. Nakamura

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

Several dibenzoazepines, thioxanthene, and phenothiazine stereoisomers were studied for their abilities to inhibit plasmid replication, intracellular transfer of R-plasmid, bacterial ATP-ase, and mouse serum cholinesterase isoenzymes. Partially saturated derivative of desipramine inhibited plasmid replication and transfer, but the fully saturated derivative was inactive. The inhibition of plasmid curing and transfer patterns did not correlate with the inhibition of ATP-ase and cholinesterase. Trans-clopenthixol was more effective in plasmid elimination than the cis-isomer. On the other hand, the cis-isomer inhibited ATPase and cholinesterase more than the trans-isomer. The levo- and dextro-methoxytrimeprazine also inhibited plasmid replication and enzyme activity. We believe that the tricyclic configuration of the drugs tested for stereospecific binding to bacterial receptors is more important than its side chain orientation. We believe that there is a similarity between bacterial receptor sites and neural receptor sites. Therefore, this model may be useful in the study of neuropharmacological agents as potential antibacterial agents.

Original languageEnglish
Pages (from-to)235-249
Number of pages15
JournalResearch Communications in Chemical Pathology and Pharmacology
Volume43
Issue number2
Publication statusPublished - 1984

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Plasmids
Cholinesterases
Isomers
Thioxanthenes
Clopenthixol
Adenosine Triphosphate
Derivatives
Stereoisomerism
Desipramine
R Factors
Enzyme activity
Sensory Receptor Cells
Isoenzymes
Adenosine Triphosphatases
Curing
Anti-Bacterial Agents
Enzymes
Serum
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Cite this

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abstract = "Several dibenzoazepines, thioxanthene, and phenothiazine stereoisomers were studied for their abilities to inhibit plasmid replication, intracellular transfer of R-plasmid, bacterial ATP-ase, and mouse serum cholinesterase isoenzymes. Partially saturated derivative of desipramine inhibited plasmid replication and transfer, but the fully saturated derivative was inactive. The inhibition of plasmid curing and transfer patterns did not correlate with the inhibition of ATP-ase and cholinesterase. Trans-clopenthixol was more effective in plasmid elimination than the cis-isomer. On the other hand, the cis-isomer inhibited ATPase and cholinesterase more than the trans-isomer. The levo- and dextro-methoxytrimeprazine also inhibited plasmid replication and enzyme activity. We believe that the tricyclic configuration of the drugs tested for stereospecific binding to bacterial receptors is more important than its side chain orientation. We believe that there is a similarity between bacterial receptor sites and neural receptor sites. Therefore, this model may be useful in the study of neuropharmacological agents as potential antibacterial agents.",
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AB - Several dibenzoazepines, thioxanthene, and phenothiazine stereoisomers were studied for their abilities to inhibit plasmid replication, intracellular transfer of R-plasmid, bacterial ATP-ase, and mouse serum cholinesterase isoenzymes. Partially saturated derivative of desipramine inhibited plasmid replication and transfer, but the fully saturated derivative was inactive. The inhibition of plasmid curing and transfer patterns did not correlate with the inhibition of ATP-ase and cholinesterase. Trans-clopenthixol was more effective in plasmid elimination than the cis-isomer. On the other hand, the cis-isomer inhibited ATPase and cholinesterase more than the trans-isomer. The levo- and dextro-methoxytrimeprazine also inhibited plasmid replication and enzyme activity. We believe that the tricyclic configuration of the drugs tested for stereospecific binding to bacterial receptors is more important than its side chain orientation. We believe that there is a similarity between bacterial receptor sites and neural receptor sites. Therefore, this model may be useful in the study of neuropharmacological agents as potential antibacterial agents.

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