Synthesis of a pyrrolidine derivative of a carvotacetone and monoterpenes for anti-methicillin-resistant Staphylococcus aureus and anti-cryptococcal properties

Nat Prod Res. 2022 May;36(9):2321-2328. doi: 10.1080/14786419.2020.1833201. Epub 2020 Oct 24.

Abstract

Monoterpene derivatives are of great biological relevance in the pharmaceutical industry. In the present study, pyrrolidine derivative of a carvotacetone, 3-O-benzylcarvotacetone (1), and selected monoterpenes (3-hydroxy-2-isopropyl-5-methyl-p-benzoquinone (3) and cis-piperitol (5)) were prepared to provide (R)-1-(4-(benzyloxy)-5-isopropyl-2-methylcyclohexa-1,3-dien-1-yl)-pyrrolidine (2), 2-isopropyl-5-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl acetate (4), cis-3-hydroxypiperitone (6) and carvacrol (7). Structure of 2 was determined based on NMR and HRMS spectral data. Compound 4 exhibited activity against fungi Cryptococcus neoformans with an IC50 value of < 0.8 µg/mL. In addition, this compound 4 had an IC50 value of 14.97 µg/mL against methicillin resistant Staphylococcus aureus bacteria. Previous to the current study, both compound 6 and 7 had been reported to have anti-microbial and anti-fungal activities.

Keywords: Anti-MRSA; Anti-cryptococcal; Carvacrol; Cis-3-hydroxypiperitone; Monoterpenes.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Cyclohexanones
  • Methicillin-Resistant Staphylococcus aureus*
  • Microbial Sensitivity Tests
  • Monoterpenes / pharmacology
  • Pyrrolidines

Substances

  • Anti-Bacterial Agents
  • Cyclohexanones
  • Monoterpenes
  • Pyrrolidines
  • carvotacetone
  • pyrrolidine