High bioremediation potential of strain Chenggangzhangella methanolivorans CHL1 for soil polluted with metsulfuron-methyl or tribenuron-methyl in a pot experiment.

Soil contamination caused by long-term application of metsulfuron-methyl and tribenuron-methyl has become an issue of increasing concern. In our previous study, strain Chenggangzhangella methanolivorans CHL1, capable of efficiently degrading sulfonylurea herbicides, was isolated. Here, the bioremediation potential of strain CHL1 was assessed for soil polluted with metsulfuron-methyl or tribenuron-methyl in a pot experiment.

Intermediate derivatisation method in the discovery of new acaricide candidates: synthesis of N-substituted piperazine derivatives and their activity against phytophagous mites.

Background: To discover and exploit novel acaricidal compounds, a series of novel N-substituted piperazine derivatives were designed and synthesised using a tert-butyl piperazine-1-carboxylate as the starting material by intermediate derivatisation methods, and their acaricidal activities were evaluated.

Results: Compounds 11 and 12 exhibited significant acaricidal activity against adults of Tetranychus cinnabarinus in greenhouse tests. Compound 12, in particular, was found to be the best potential candidate acaricide and proved to be more active than the commercial positive controls spirodiclofen and pyridaben, with an LC of 0.

Measuring the bioactivity and molecular conformation of typically globular proteins with phenothiazine-derived methylene blue in solid and in solution: A comparative study using photochemistry and computational chemistry.

Methylene blue is a phenothiazine agent, that possesses a diversity of biomedical and biological therapeutic purpose, and it has also become the lead compound for the exploitation of other pharmaceuticals such as chlorpromazine and the tricyclic antidepressants. However, the U.S.

Biointeractions of C.I. Acid Red 2 and its structural analogues with transporter albumin: Fluorescence, circular dichroism, and ligand docking approaches.

In this contribution, the toxicological effects of C.I. Acid Red 2 and 1-(2-pyridylazo)-2-naphthol (PAN) have been elucidated by utilizing plasma albumin as a biological model.

Discovery of pyridine-based agrochemicals by using Intermediate Derivatization Methods.

Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error testing and new agrochemical discovery is not benefiting as much from the in silico new chemical compound identification/discovery techniques used in pharmaceutical research, it has become more important to find new methods to enhance the efficiency of discovering novel lead compounds in the agrochemical field to shorten the time of research phases in order to meet changing market requirements. In this review, we selected 18 representative known agrochemicals containing a pyridine moiety and extrapolate their discovery from the perspective of Intermediate Derivatization Methods in the hope that this approach will have greater appeal to researchers engaged in the discovery of agrochemicals and/or pharmaceuticals.

Design, synthesis and insecticidal evaluation of aryloxy dihalopropene derivatives.

Plutella xylostella (P. xylostella) is a highly migratory, cosmopolitan species and one of the most important pest of cruciferous crops worldwide. Pyridalyl as a novel class of insecticides has good efficacy against P.

Design, synthesis and structure-activity relationship of novel diphenylamine derivatives.

Diphenylamine derivatives have been reported with good fungicidal, insecticidal, acaricidal, rodenticidal and/or herbicidal activities. To find new lead compound of this kind, a series of novel diphenylamine derivatives were designed and synthesized by the approach of Intermediate Derivatization Methods. All compounds were identified by (1)H NMR and elemental analysis.

Synthesis and evaluation of substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives as potent herbicidal agents.

In an attempt to obtain novel candidate compound for weed control, a series of newly substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives 2 were designed and synthesized using compound II7 as a lead compound by Intermediate Derivatization Methods and their herbicidal activities were evaluated. The herbicidal activity assay in greenhouse tests showed several compounds (2g, 2i, 2j, 2k, 2l, 2m, 2n and 2o) exhibited significant herbicidal activity for controlling velvet leaf (Abutilon theophrasti medic.) and youth-and-old age (Zinnia elegans jacq.

Design, synthesis, and herbicidal activity of novel substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives.

A series of novel substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives were designed and synthesized using 2-phenylpridines as the lead compound by intermediate derivatization methods in an attempt to obtain novel compound candidates for weed control. The herbicidal activity assay in glasshouse tests showed several compounds (II6, II7, II8, II9, II10, II11, III2, III3, III4, and III5) could efficiently control velvet leaf, youth-and-old age, barnyard grass, and foxtail at the 37.5 g/ha active substance.

Probing the active conformation of FGLamide allatostatin analogs with N-terminal modifications using NMR spectroscopy and molecular modeling.

The FGLamide allatostatins (ASTs) can inhibit the production of juvenile hormone in vitro, and they therefore are regarded as possible insect growth regulator candidates for pest control. To understand the structural features of the ASTs that cause the differences in their activity the pentapeptide and four N-terminal modifications of AST analogs (H17, K9, K10 and K23) were selected to investigate their conformations. From NMR spectroscopy and molecular modeling, it is clear that K23 and K9 have a type IV β-turn and a γ turn in DMSO, respectively.

Solution-phase parallel syntheses of herbicidal 1-phenyl-2,4,5- imidazolidinetriones and 2-thioxo-4,5-imidazolidinediones.

In order to find new herbicidally active compounds, a fifteen-member library, focusing on the variation of 3- position substituents of 2,4,5-imidazolidine-trione or 2-thioxo-4,5-imidazolidinedione, was designed and prepared in parallel by the reaction of various ureas or thioureas with oxalyl chloride using solution-phase technology. An interesting and, to the best of our knowledge, unprecedented finding is that a by-product of 1-phenyl-3-propylcarbodiimide was formed during the addition of oxalyl chloride into the solution of 1-phenyl-3-propylthiourea in the presence of triethylamine in dichloromethane. It has been shown that the herbicidal activity of 2,4,5-imidazolidinetriones is about the same as that of their analogous 2-thioxo-4,5-imidazolidinediones.

Design, synthesis and structure-activity relationship of novel insecticidal dichloro-allyloxy-phenol derivatives containing substituted pyrazol-3-ols.

Background: Pyridalyl, consisting of dicholoro-allyoxy-phenol moiety, is a novel class of insecticide showing extraordinary activities against various lepidopterous and thysanopterous pests on cotton and vegetables. To discover further novel insecticides, a series of new dichloro-allyloxy-phenol derivatives containing substituted pyrazol-3-ol moieties were designed and synthesised via the intermediate derivatisation method.

Results: The target compounds were characterised by (1) H NMR, IR, MS and elemental analysis.

Synthesis and bioactivity of novel coumarin derivatives.

A series of coumarin derivatives (6-8) containing (E)-methyl 2-(methoxyimino)-2-phenylacetate, (E)-2-(methoxyimino)-N-methyl-2-phenylacetamide and methyl methoxy(phenyl)carbamate were synthesized from substituted resorcinols (1) and substituted beta-keto esters (2) as starting material via cyclization and condensation reactions. The test results indicated that (E)-methyl 2-{2-[(3-hexyl-4-methyl-coumarin-7-yloxy)methyl]phenyl}-2-(methoxyimino)acetate (6f) was the optimal structure with good fungicidal activity against cucumber grey mold (CGM) giving 100% control at 100 mg L(-1) concentration, much higher than that of coumoxystrobin. Methyl 2-[(3,4-dimethyl-coumarin -7-yloxy)methyl]phenyl(methoxy)carbamate (8a) was another optimal structure with good fungicidal activity against wheat powdery mildew (WPM) showing 100% control at 50 mg L(-1) concentration, at the same level as that of the commercial kresoxim-methyl, and very significantly higher than that of coumoxystrobin (no control against WPM at 400 mg L(-1)).

Synthesis and herbicidal activity of diphenyl ether derivatives containing unsaturated carboxylates.

A series of novel diphenyl ether derivatives containing unsaturated carboxylates were designed and synthesized. Their structures were identified by (1)H nuclear magnetic resonance and elemental analyses. The bioassays indicated that the compounds 5b and 5c exhibited good herbicidal activities against velvetleaf at a concentration of 30-40 g/hm(2).