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Search Results (3)

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Keywords = pimprinine

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14 pages, 3459 KiB  
Article
Design, Synthesis, Antifungal Activity, and Molecular Docking of Streptochlorin Derivatives Containing the Nitrile Group
by Jing-Rui Liu, Ya Gao, Bing Jin, Dale Guo, Fang Deng, Qiang Bian, Hai-Feng Zhang, Xin-Ya Han, Abdallah S. Ali, Ming-Zhi Zhang, Wei-Hua Zhang and Yu-Cheng Gu
Mar. Drugs 2023, 21(2), 103; https://doi.org/10.3390/md21020103 - 31 Jan 2023
Cited by 10 | Viewed by 3329
Abstract
Based on the structures of natural products streptochlorin and pimprinine derived from marine or soil microorganisms, a series of streptochlorin derivatives containing the nitrile group were designed and synthesized through acylation and oxidative annulation. Evaluation for antifungal activity showed that compound 3a could [...] Read more.
Based on the structures of natural products streptochlorin and pimprinine derived from marine or soil microorganisms, a series of streptochlorin derivatives containing the nitrile group were designed and synthesized through acylation and oxidative annulation. Evaluation for antifungal activity showed that compound 3a could be regarded as the most promising candidate—it demonstrated over 85% growth inhibition against Botrytis cinerea, Gibberella zeae, and Colletotrichum lagenarium, as well as a broad antifungal spectrum in primary screening at the concentration of 50 μg/mL. The SAR study revealed that non-substituent or alkyl substituent at the 2-position of oxazole ring were favorable for antifungal activity, while aryl and monosubstituted aryl were detrimental to activity. Molecular docking models indicated that 3a formed hydrogen bonds and hydrophobic interactions with Leucyl-tRNA Synthetase, offering a perspective for the possible mechanism of action for antifungal activity of the target compounds. Full article
(This article belongs to the Special Issue Chemical Modification and Structural Elucidation of Marine Natural Products)
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13 pages, 6890 KiB  
Article
Discovery of Novel Pimprinine and Streptochlorin Derivatives as Potential Antifungal Agents
by Jing-Rui Liu, Jia-Mu Liu, Ya Gao, Zhan Shi, Ke-Rui Nie, Dale Guo, Fang Deng, Hai-Feng Zhang, Abdallah S. Ali, Ming-Zhi Zhang, Wei-Hua Zhang and Yu-Cheng Gu
Mar. Drugs 2022, 20(12), 740; https://doi.org/10.3390/md20120740 - 25 Nov 2022
Cited by 7 | Viewed by 3269
Abstract
Pimprinine and streptochlorin are indole alkaloids derived from marine or soil microorganisms. In our previous study, they were promising lead compounds due to their potent bioactivity in preventing many phytopathogens, but further structural modifications are required to improve their antifungal activity. In this [...] Read more.
Pimprinine and streptochlorin are indole alkaloids derived from marine or soil microorganisms. In our previous study, they were promising lead compounds due to their potent bioactivity in preventing many phytopathogens, but further structural modifications are required to improve their antifungal activity. In this study, pimprinine and streptochlorin were used as parent structures with the combination strategy of their structural features. Three series of target compounds were designed and synthesized. Subsequent evaluation for antifungal activity against six common phytopathogenic fungi showed that some of thee compounds possessed excellent effects, and this is highlighted by compounds 4a and 5a, displaying 99.9% growth inhibition against Gibberella zeae and Alternaria Leaf Spot under 50 μg/mL, respectively. EC50 values indicated that compounds 4a, 5a, 8c, and 8d were even more active than Azoxystrobin and Boscalid. SAR analysis revealed the relationship between 5-(3′-indolyl)oxazole scaffold and antifungal activity, which provides useful insight into the development of new target molecules. Molecular docking models indicate that compound 4a binds with leucyl-tRNA synthetase in a similar mode as AN2690, offering a perspective on the mode of action for the study of its antifungal activity. These results suggest that compounds 4a and 5a could be regarded as novel and promising antifungal agents against phytopathogens due to their valuable potency. Full article
(This article belongs to the Special Issue Chemical Modification and Structural Elucidation of Marine Natural Products)
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16 pages, 2030 KiB  
Article
Genomic and Metabolomic Investigation of a Rhizosphere Isolate Streptomyces netropsis WLXQSS-4 Associated with a Traditional Chinese Medicine
by Songya Zhang, Lingxiao Zhang, Jing Zhu, Hong Chen, Zhicong Chen, Tong Si and Tao Liu
Molecules 2021, 26(8), 2147; https://doi.org/10.3390/molecules26082147 - 8 Apr 2021
Cited by 8 | Viewed by 3366
Abstract
Rhizosphere microorganisms play important ecological roles in promoting herb growth and producing abundant secondary metabolites. Studies on the rhizosphere microbes of traditional Chinese medicines (TCMs) are limited, especially on the genomic and metabolic levels. In this study, we reported the isolation and characterization [...] Read more.
Rhizosphere microorganisms play important ecological roles in promoting herb growth and producing abundant secondary metabolites. Studies on the rhizosphere microbes of traditional Chinese medicines (TCMs) are limited, especially on the genomic and metabolic levels. In this study, we reported the isolation and characterization of a Steptomyces netropsis WLXQSS-4 strain from the rhizospheric soil of Clematis manshurica Rupr. Genomic sequencing revealed an impressive total of 40 predicted biosynthetic gene clusters (BGCs), whereas metabolomic profiling revealed 13 secondary metabolites under current laboratory conditions. Particularly, medium screening activated the production of alloaureothin, whereas brominated and chlorinated pimprinine derivatives were identified through precursor-directed feeding. Moreover, antiproliferative activities against Hela and A549 cancer cell lines were observed for five compounds, of which two also elicited potent growth inhibition in Enterococcus faecalis and Staphylococcus aureus, respectively. Our results demonstrated the robust secondary metabolism of S. netropsis WLXQSS-4, which may serve as a biocontrol agent upon further investigation. Full article
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