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1.
Chem Commun (Camb) ; 60(51): 6544-6547, 2024 Jun 20.
Artigo em Inglês | MEDLINE | ID: mdl-38842029

RESUMO

Chemoselective oxidation of aromatic and heteroaromatic aldehydes (>45 examples) to their corresponding carboxylic acids has been developed. Potassium tert-butoxide acts as an oxygen source during this transformation that delivers the corresponding acids without chromatographic purifications. The use of bench-top reagents, operational simplicity, and high level of chemo-selectivity with respect to oxidation of the least preferred aldehyde functionality, in the presence of more susceptible functional groups, are some of the highlights of this strategy.

2.
Org Biomol Chem ; 22(17): 3502-3509, 2024 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-38618907

RESUMO

An expeditious metal free C-3 alkylation of indoles and its NIS-mediated deviation to indolo[2,3-b]quinolines is reported. This protocol, executed in aqueous HFIP has broad substrate scope and is well inclined towards the ideas of sustainable chemistry. Applications of these strategies in accessing bioactive natural products like vibrindole, norcryptotakeine, neocryptolepine and indenoindolone scaffolds has also been demonstrated.

3.
Microb Ecol ; 85(4): 1276-1287, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-35366684

RESUMO

Here we describe the antimicrobial potential of secondary metabolites, fulvic acid (F.A.) and anhydrofulvic acid (AFA), produced by RDE147, an endophyte of Rosa damascena Mill. The endophyte was identified as Cercospora piaropi by ITS and ß-tubulin-based phylogenetic analyses, while chemoprofiling of the endophyte by column chromatography and spectroscopy yielded two pure compounds, F.A. and AFA. The compounds demonstrated different antimicrobial profiles, with AFA suppressing the growth of C. albicans at 7.3 µg ml-1 IC50. Further studies revealed that AFA strongly restricted the biofilm production and hyphae formation in C. albicans by down-regulating several biofilm and morphogenesis-related genes. The time-kill assays confirmed the fungicidal activity of AFA against C. albicans, killing 83.6% of the pathogen cells in 24 h at the MIC concentration, and the post-antibiotic effect (PAE) experiments established the suppression of C. albicans growth for extended time periods. The compound acted synergistically with amphotericin B and nystatin and reduced ergosterol biosynthesis by the pathogen, confirmed by ergosterol estimation and comparative expression profiling of selected genes and molecular docking of AFA with C. albicans squalene epoxidase. AFA also suppressed the expression of several other virulence genes of the fungal pathogen. The study determines the anti-C. albicans potential of AFA and its impact on the biology of the pathogen. It also indicates that Cercospora species may yield potential bioactive molecules, especially fulvic acid derivatives. However, it is imperative to conduct in vivo studies to explore this molecule's therapeutic potential further.


Assuntos
Candida albicans , Rosa , Candida albicans/metabolismo , Fatores de Virulência/metabolismo , Rosa/metabolismo , Cercospora/metabolismo , Simulação de Acoplamento Molecular , Filogenia , Biofilmes , Ergosterol/metabolismo , Proliferação de Células , Antifúngicos/farmacologia , Antifúngicos/metabolismo , Testes de Sensibilidade Microbiana
4.
Nat Prod Res ; 35(3): 471-480, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31282748

RESUMO

In a continuing effort to explore the structural diversity and pharmacological activities of natural products based scaffolds, herein, we report the isolation, synthesis, and structure determination of cannabidiol and its derivatives along with their cytotoxic activities. Treatment of cannabidiol (1) with acid catalyst POCl3 afforded a new derivative 6 along with six known molecules 2 - 5, 7 and, 8. The structure of 6 was elucidated by extensive spectroscopic analyses and DFT calculations of the NMR and ECD data. All the compounds (2 - 8) were evaluated for their cytotoxic potential against a panel of eight cancer cell lines. Compounds 4, 5, 7, and 8 showed pronounced in vitro cytotoxic activity with IC50 values ranging from 5.6 to 60 µM. Out of the active molecules, compounds 4, and 7 were found to be comparable to that of the parent molecule 1 on the inhibition of almost all the tested cancer cell lines.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Canabidiol/química , Cannabis/química , Canabidiol/isolamento & purificação , Canabidiol/farmacologia , Linhagem Celular Tumoral , Teoria da Densidade Funcional , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular
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