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Introduction:Three novel macrolactams, FW8-1 (1), FW8-4 (2), and FW60-20 (3), were isolated from a culture of Micromonospora sp. The structures of these compounds were elucidated using Mass Spectrometry (MS) and comprehensive Nuclear Magnetic Resonance (NMR) analyses.Methods:The relative configurations of compounds 1-3 were assigned through theoretical calculations of their NMR spectra.objective:The objective is to obtain PMLs with novel structures and to characterize and evaluate them.Results:The isolation and determination of the relative configurations of these macrolactams have provided fresh perspectives on the biosynthetic pathways, leading to the formation of polyene macrolactams.Conclusion:Further, virtual screening and bioactivity predictions have suggested compounds 1-3 to possess potential anti-tumor, anti-inflammatory, and neuroprotective properties.

10 Oct 2024·The Natural Products Journal

Antimicrobial Macrolide Levantilide D from Rare Marine Micromonospora sp.

Author: Jiang, Hong ; Lin, Ru ; Zhou, Jian ; Wu, Bin ; Jiang, Honglei ; Zhao, Wei ; Zhao, Meilu ; Zhou, Jingming ; Ge, Yichao

Introduction:One new levantilide D (2) with a 20-membered macrolide, along with one known levantilide C (1), was isolated from a rare marine actinomycetes Micromonospora sp. (FIMYZ52).Method:The structural elucidation of the compounds was based on integrated analyses involving 1D and 2D NMR spectroscopy and HR-ESI-MS.Result:The relative and absolute configurations of compounds 1 and 2 were ascertained by integrating multispectral ROESY and NOESY information from analogs in conjunction with theoretical TDDFT-ECD calculations. Levantilide D (2) exhibited antibacterial activity against Staphylococcus aureus.Conclusion:A plausible biosynthetic pathway of the macrolide compounds (1-2) was proposed.conclusion:The structure of levantilide D in this study is characterized by a 20-membered macrolide structure with moderately long branched aliphatic chains containing hydroxyl or ketone groups. Macrolides are a class of antibiotics that are widely used to treat a variety of bacterial infections. This structure is crucial for their antibacterial activity. The variations in the lactone ring structure and the attached fatty chains have given rise to different generations of macrolides with varying properties, including antibacterial activity.

01 Jun 2024·Fitoterapia

Antimicrobial spiroketal macrolides and dichloro-diketopiperazine from Micromonospora sp. FIMYZ51

Article

Author: Jiang, Hong ; Wang, Yinuo ; Zhou, Chengzeng ; Wu, Bin ; Ge, Yichao ; Xie, Yang ; Zhou, Jian ; Ma, Yihan ; Zhao, Wei

Four compounds (1-4) featuring with an _L-rhodinose and spiroketal, possess uncommon continuous hydroxy groups in the macrolide skeleton, and a dichloro-diketopiperazine (5) were isolated from a marine derived Micromonospora sp. FIMYZ51. The determination of the relative and absolute configurations of all isolates was achieved by extensive spectroscopic analyses, single-crystal X-ray diffraction analysis, and ECD calculations. According to structural characteristic and genomic sequences, a plausible biosynthetic pathway for compound 1-4 was proposed and a spirocyclase was inferred to be responsible for the formation of the rare spirocyclic moiety. Compounds 1-4 exhibited potent antifungal activities which is equal to itraconazole against Aspergillus niger. Compounds 1-5 exhibited different degree of inhibitory activities against opportunistic pathogenic bacteria of endocarditis (Micrococcus luteus) with MIC values ranging from 0.0625 μg/mL to 32 μg/mL. Compounds 2 and 3 showed moderate cytotoxicity against drug-resistant tumor cell lines (Namalwa and U266). The result not only provides active lead-compounds, but also reveal the potential of the spirocyclase gene resources from Micromonospora sp., which highlights the promising potential of the strain for biomedical applications.

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Pipeline Snapshot as of 05 Mar 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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