Synthesis and screening of clerodane diterpene analogues from 16 hydroxycleroda 3,13(14)-Z-diene 15,16-olide for potential anti-mycobacterial activity.

Autor: Sony Priya K; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India., Sruthi Sri B; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India., Patrick F K; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India., Sangeeta G; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India., Suvarna B P; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India., Murali Krishna K M; Pharmaceutical Chemistry Research Laboratory, Andhra university, Visakhapatnam, India.
Jazyk: angličtina
Zdroj: Natural product research [Nat Prod Res] 2023 Nov 06, pp. 1-9. Date of Electronic Publication: 2023 Nov 06.
DOI: 10.1080/14786419.2023.2275270
Abstrakt: In recent years, clerodane diterpenes, a class of bioactive compounds, have come into the spotlight due to their amazing bioactivities. Three novel clerodane diterpene analogues were obtained by synthesising 16-hydroxycleroda-3,13(14)-Z-diene-15,16-olide (Lactone) with primary amines. Anti-tubercular activity was determined using Microplate Alamar Blue Assay. Among all the synthesised compounds from methanolic extract of seeds, results clearly showed that compounds 3 and 5 have significant anti TB activity with an MIC of 1.56 µg/ml against the Mycobacterium tuberculosis MTB H37Rv bacilli strain than the gold standard drugs pyrazinamide (3.13 µg/ml), ciprofloxacin (3.13 µg/ml), streptomycin (6.25 µg/ml) and rifampicin (6.25 µg/ml). Compound 5 exhibited significant antibacterial activity with zone of inhibition of 10.8 mm with Gram + ve and 7.95 mm with Gram -ve bacteria at a conc of 50 µg/ml respectively. In the current investigation, three novel heterocycles (compounds 3-5) of the diterpenoid were prepared, in high yield, using one-pot, efficient approach.
Databáze: MEDLINE