Novel aromatic carboxamide potentially targeting fungal succinate dehydrogenase: Design, synthesis, biological activities and molecular dynamics simulation studies.

Background: Succinate dehydrogenase inhibitors (SDHIs) emerging in fungicide markets are widely used in crop protection. Currently, the structural modification focusing on a structurally diverse 'core' moiety (aryl) of SDHIs is being gradually identified as one of the innovative strategies for developing novel, highly effective and low resistant fungicides.

Results: By optimization of lead compound SCU2028, 30 novel aromatic carboxamides Ia-o and IIa-o without a pyrazol group were designed, synthesized and characterized by H NMR, C NMR and high resolution mass spectrum (HRMS).

Novel Pyrazole Carboxamide Containing a Diarylamine Scaffold Potentially Targeting Fungal Succinate Dehydrogenase: Antifungal Activity and Mechanism of Action.

Succinate dehydrogenase (SDH) is known as an ideal target for the development of novel fungicides. Over the years, a series of novel pyrazole carboxamides containing a diarylamine scaffold have been reported as potent SDH inhibitors (SDHIs) in our laboratory. Among them, compound (EC = 0.

Neochamaejasmin B extracted from Stellera chamaejasme L. induces apoptosis through caspase-10-dependent way in insect neuronal cells.

To explore the toxicity mechanisms of neochamaejasmin B (NCB) extracted from Stellera chamaejasme L., we first evaluated its cytotoxicity in neuronal cells of Helicoverpa zea (AW1 cells). NCB inhibited cell growth and was cytotoxic to AW1 cells in a dose-dependent manner.

Unraveling the polypharmacology of a natural antifungal product, eugenol, against Rhizoctonia solani.

Background: Rice sheath blight caused by Rhizoctonia solani is a devastating disease of rice in China. However, indiscriminate use of chemical fungicides applied to control the disease raise major environmental and food safety issues. Ecofriendly biocontrol alternatives are urgently needed.

Toxicity and physiological actions of biflavones on potassium current in insect neuronal cells.

Stellera chamaejasme L. is a Chinese traditional herb. It has a long history and many medicinal usages.

Synthesis and Biological Evaluation of Novel Benodanil-Heterocyclic Carboxamide Hybrids as a Potential Succinate Dehydrogenase Inhibitors.

In order to discover new antifungal agents, twenty novel benodanil-heterocyclic carboxamide hybrids were designed, synthesized, and characterized by H NMR and HRMS. In vitro, their antifungal activities against four phytopathogenic fungi were evaluated, as well as some of the target compounds at 50 mg/L demonstrated significant antifungal activities against . Especially, compounds (EC = 6.

Mechanism of Action of Novel Pyrazole Carboxamide Containing a Diarylamine Scaffold against .

In the last few decades, causing rice sheath blight has resulted in a lot of economic losses in the world. Therefore, many novel pyrazole carboxamide fungicides have been intensively researched and employed to fight against it. In this regard, in recent years, our group reported a novel pyrazole carboxamide containing a diarylamine scaffold with good antifungal activity against rice sheath blight in the pot test and field trial.

Isochamaejasmin induces toxic effects on Helicoverpa zea via DNA damage and mitochondria-associated apoptosis.

Background: Stellera chamaejasme L. is a poisonous plant with rich resources and is thus highly valuable in terms of new pesticide development. Isochamaejasmin (ICM), one of the main ingredients in S.

AW1 Neuronal Cell Cytotoxicity: The Mode of Action of Insecticidal Fatty Acids.

To explore lead compounds for biological insecticides, nine fatty acids (FAs)' insecticidal activities against (Lepidoptera, Noctuidae) and their cytotoxicity on neuronal cells (AW1 cells) were evaluated. The results showed that FAs at 1000 mg/L had a mortality rate of 10.0-83.

Discovery of N-(4-fluoro-2-(phenylamino)phenyl)-pyrazole-4-carboxamides as potential succinate dehydrogenase inhibitors.

Succinate dehydrogenase (SDH), an essential component of cellular respiratory chain and tricarboxylic acid (or Krebs) cycle, has been identified as one of the most significant targets for pharmaceutical and agrochemical. Herein, with the aim of discovery of new antifungal lead structures, a class of novel N-(4-fluoro-2-(phenylamino)phenyl)-pyrazole-4-carboxamides were designed, synthesized and evaluated for their biological activities. They were bioassayed against seven phytopathogenic fungi, Rhizoctonia solani, Phytophthora infestans, Fusarium oxysporum f.

Neochamaejasmin A extracted from Stellera chamaejasme L. induces apoptosis involving mitochondrial dysfunction and oxidative stress in Sf9 cells.

To explore the toxicity mechanisms of neochamaejasmin A (NCA), extracted from Stellera chamaejasme L., we first evaluated its cytotoxicity on the Spodoptera frugiperda (Sf9) cell line. The results confirmed that NCA inhibited Sf9 cell survival in both a dose- and time-dependent manner.

N-[2-[(3-Chlorophenyl)amino]-phenyl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide: Synthesis, Crystal Structure, Molecular Docking and Biological Activities.

In continuation of our previous research on the development of novel pyrazole-4-carboxamide with potential antifungal activity, compound SCU2028, namely N-[2-[(3-chlorophenyl)amino]phenyl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide, was synthesized by new method, structurally characterized by IR, HR-ESI-MS, H- and C-NMR spectra and further identified by single-crystal X-ray diffraction. In pot tests, compound SCU2028 showed good in vivo antifungal activity against Rhizoctonia solani (R. solani) and IC value of it was 7.

Design, Synthesis, and Antifungal Activities of Novel Aromatic Carboxamides Containing a Diphenylamine Scaffold.

A series of novel N-(2-(phenylamino)-4-fluorophenyl)-pyrazole-4-carboxamides 1-15 and aromatic carboxamides with a diphenylamine scaffold 16-29 were designed, synthesized, and evaluated for their antifungal activities. In vitro experiments showed that compound 6 (EC = 0.03 mg/L) was superior to bixafen (EC = 0.

Design, synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors.

Sixteen novel pyrazole carboxamides with diarylamines scaffold were designed, synthesized and characterized in detail via H NMR, C NMR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good antifungal activity against Rhizoctonia solani, Fusarium oxysporum, Phytophthora infestans and Fusarium graminearum. Among them, compound 1c exhibited the highest antifungal activities against R.

Investigation of novel pyrazole carboxamides as new apoptosis inducers on neuronal cells in Helicoverpa zea.

Novel pyrazole carboxamides with a diarylamine-modified scaffold were modified based on the bixafen (Bayer) fungicide, which has excellent activity against Rhizoctonia solani, Rhizoctonia cerealis and Sclerotinia sclerotiorum. To discover the potential insecticidal activity of these novel pyrazole carboxamides, the present study explored their possible cytoactivity on the insect neuronal cells (RP-HzVNC-AW1) in Helicoverpa zea. The preliminary bioassays showed that some of the target compounds exhibited good cytoactivity against AW1 cells.

Synthesis of novel fenfuram-diarylether hybrids as potent succinate dehydrogenase inhibitors.

Twelve novel fenfuram-diarylether hybrids were designed, synthesized and characterized by H NMR and MS. Their in vitro antifungal activities were evaluated against five phytopathogenic fungi by mycelial growth inhibition method. Most compounds showed significant antifungal effect on Rhizoctonia solani and Sclerotinia sclerotiorum.

Design, synthesis and antifungal activity of novel fenfuram-diarylamine hybrids.

Ten novel fenfuram-diarylamine hybrids were designed and synthesized. And their antifungal activities against four phytopathogenic fungi have been evaluated in vitro and most of the compounds demonstrated a significant antifungal activities against Rhizoctonia solani and Sclerotinia sclerotiorum. Compound 5e exhibited the most potent antifungal activity against R.

Discovery of the molecular mechanisms of the novel chalcone-based inhibitor C1 using transcriptomic profiling and co-expression network analysis.

Background: In our previous studies, we discovered a series of chalcone-based phytopathogenic fungus inhibitors. However, knowledge of their effects, detailed targets and molecular mechanisms in () remained limited.

Methods: To explore the expression and function of differentially expressed genes in after treatment with compound C1, we analyzed the expression profile of mRNAs using a microarray analysis and GO, KEGG and WGCNA analysis, followed by qRT-PCR and Western blots to validate our findings.

Design, synthesis and antifungal activity of novel furancarboxamide derivatives.

Twenty-seven novel furancarboxamide derivatives with a diphenyl ether moiety were synthesized and evaluated for their antifungal activity against Rhizoctonia solani, Botrytis cirerea, Valsa mali and Sphaceloma ampelimum. Antifungal bioassay results indicated that most compounds had good or excellent fungicidal activities for R. solani and S.

Isopropanol biodegradation by immobilized Paracoccus denitrificans in a three-phase fluidized bed reactor.

A three-phase bed bioreactor including a mix of immobilized microbes was used to degrade isopropanol (IPA). The immobilization method was studied and cells immobilized with calcium alginate, polyvinyl alcohol, activated carbon, and SiO were demonstrated to be the best immobilization method for the degradation of 90% of 2 g/L IPA in just 4 days, 1 day earlier than with free cells. Acetone was monitored as an indicator of microbial IPA utilization as the major intermediate of aerobic IPA biodegradation.

Antimicrobial activity of secondary metabolites from Streptomyces sp. K15, an endophyte in Houttuynia cordata Thunb.

We isolated Streptomyces sp. K15 from the root tissue of Houttuynia cordata Thunb and found that some of its secondary metabolites exhibited significant antimicrobial activity against Botrytis cinerea. Moreover, we separated, purified and identified the major active ingredient to be 2-pyrrol formic acid by using silica gel column chromatography, high-performance liquid chromatography and NMR analysis of the spectral data.

Biodegradation of isopropanol by a solvent-tolerant Paracoccus denitrificans strain.

The biodegradation of high concentration isopropanol (2-propanol, IPA) at 16 g/L was investigated by a solvent-tolerant strain of bacteria identified as Paracoccus denitrificans for the first time by 16S rDNA gene sequencing. The strain P. denitrificans GH3 was able to utilize the high concentration of IPA as the sole carbon source within a minimal salts medium with a cell density of 1.

Biodegradation of cypermethrin by a novel Catellibacterium sp. strain CC-5 isolated from contaminated soil.

The bacterial strain CC-5, isolated from contaminated soil and identified as Catellibacterium sp. based on morphology and partial 16S rDNA gene sequence analysis, utilized cypermethrin as its sole carbon source and degraded 97% of 100 mg·L(-1) cypermethrin within 7 days. The optimal degradation conditions were determined to be 30 °C and pH 7.

Isolation, identification and characterization of a glyphosate-degrading bacterium, Bacillus cereus CB4, from soil.

A bacterial strain named CB4, with highly effective glyphosate degradation capability, was isolated from soil after enrichment. On the basis of the Biolog omniLog identification system (Biolog) and 16S ribosomal RNA (rRNA) gene sequencing methods, strain CB4 was identified as Bacillus cereus. Further experiments were carried out to optimize the growth of strain CB4 and the glyphosate degradation activity by high performance liquid chromatography (HPLC).