SYNTHESIS AND EVALUATION OF BIOLOGICAL ACTIVITY OF HOMODRIMANE SESQUITERPENOIDS BEARING HYDRAZINECARBOTHIOAMIDE OR 1,2,4-TRIAZOLE UNIT

Authors

  • Lidia Lungu Institute of Chemistry
  • Alexandru Ciocarlan Institute of Chemistry
  • Alic Barba Institute of Chemistry
  • Sergiu Shova Institute of Chemistry “P. Poni” Institute of Macromolecular Chemistry
  • Serghei Pogrebnoi Institute of Chemistry
  • Ionel Mangalagiu “Al. I. Cuza” University of Iasi
  • Costel Moldoveanu “Al. I. Cuza” University of Iasi
  • Nicoleta Vornicu Metropolitan Center of Research T.A.B.O.R
  • Michele D'Ambrosio Università degli Studi di Trento
  • Maria V. Babak National University of Singapore
  • Vladimir B. Arion University of Vienna
  • Aculina Aricu Institute of Chemistry

DOI:

https://doi.org/10.1007/4958

Keywords:

homodrimane sesquiterpenoid, hydrazinecarbothioamide, 1, 2, 4-triazole, antibacterial activity, anticancer activity, antifungal activity, microwave irradiation.

Abstract

Synthesis of novel (+)-sclareolide-based homodrimane sesquiterpenoids bearing hydrazinecarbothioamide or N-substituted 1,2,4-triazole unit has been reported. These heterocyclic compounds demonstrate promising in vitro antifungal and antibacterial activities toward fungal species Aspergillus niger, Fusarium solani, Penicillium chrysogenum, Penicillium frequentans, and Alternaria alternata and bacteria
strains Bacillus sp. and Pseudomonas aeruginosa at minimum inhibitory concentration level of μg/ml. In addition, two homodrimane sesquiterpenoids with hydrazinecarbothioamide fragment show cytotoxicity toward human ovarian carcinoma cells A2780 and A2780cis with half maximal inhibitory concentration values in range of 9–15 μM.

Author Biographies

Lidia Lungu, Institute of Chemistry

Laboratory "Chemistry of natural and viologically active compounds"

Alexandru Ciocarlan, Institute of Chemistry

Laboratory "Chemistry of natural and viologically active compounds"

Alic Barba, Institute of Chemistry

Laboratory "Chemistry of natural and viologically active compounds"

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Published

2019-08-14

Issue

Vol. 55 No. 8 (2019)

Section

Original Papers