3547-07-7Relevant articles and documents
Identification of small molecules blocking the pseudomonas aeruginosa type iii secretion system protein pcrv
Sundin, Charlotta,Saleeb, Michael,Spjut, Sara,Qin, Liena,Elofsson, Mikael
, p. 1 - 17 (2021/01/13)
Pseudomonas aeruginosa is an opportunistic bacterial pathogen that employs its type III secretion system (T3SS) during the acute phase of infection to translocate cytotoxins into the host cell cytoplasm to evade the immune system. The PcrV protein is located at the tip of the T3SS, facilitates the integration of pore-forming proteins into the eukaryotic cell membrane, and is required for translocation of cytotoxins into the host cell. In this study, we used surface plasmon resonance screening to identify small molecule binders of PcrV. A follow-up structure-activity relationship analysis resulted in PcrV binders that protect macrophages in a P. aeruginosa cell-based infection assay. Treatment of P. aeruginosa infections is challenging due to acquired, intrinsic, and adaptive resistance in addition to a broad arsenal of virulence systems such as the T3SS. Virulence blocking molecules targeting PcrV constitute valuable starting points for development of next generation antibacterials to treat infections caused by P. aeruginosa.
Synthesis and Herbicidal Activity of α-(Substituted Phenoxybutyryloxy or Valeryloxy)alkylphosphonates and 2-(Substituted Phenoxybutyryloxy)alkyl-5,5-dimethyl-1,3,2-dioxaphosphinan-2-one
Wang, Wei,Zhang, Sha-Sha,Zhou, Yuan,Peng, Hao,He, Hong-Wu,Lu, Xing-Tao
, p. 6911 - 6915 (2016/10/03)
On the basis of our work on the modification of alkylphosphonates 1, a series of α-(substituted phenoxybutyryloxy or valeryloxy)alkylphosphonates (4-5) and 2-(substituted phenoxybutyryloxy)alkyl-5,5-dimethyl-1,3,2-dioxaphosphinan-2-one (6) were designed and synthesized. The bioassay results indicated that 14 of title compounds 4 exhibited significant postemergence herbicidal activity against velvetleaf, common amaranth, and false daisy at 150 g ai/ha. Compounds 5 were inactive against all tested weeds. Compounds 6 exhibited moderate to good inhibitory effect against the tested dicotyledonous weeds. Structure-activity relationship (SAR) analyses showed that the length of the carbon chain as linking bridge had a great effect on the herbicidal activity. Broad-spectrum tests of compounds 4-1, 4-2, 4-9, 4-30, and 4-36 were carried out at 75 g ai/ha. Especially, 4-1 exhibited 100% inhibition activity against the tested dicotyledonous weeds, which was higher than that of glyphosate.
Active substances for increasing the stress defense in plants to abiotic stress, and methods of finding them
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, (2008/06/13)
The invention relates to a method of finding compounds which increase the tolerance of plants to abiotic stress factors acting on this plant, such as, for example, temperature (such as chill, frost or heat), water (such as dryness, drought or anoxia), or the chemical load (such as lack of or excess of mineral salts, heavy metals, gaseous noxious substances) by increasing the expression of plant-endogenous proteins, and to the use of these compounds for increasing the tolerance in plants to abiotic stress factors.
Herbicides comprising benzoylcyclohexanediones and safeners
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, (2008/06/13)
Herbicidal compositions are described that comprise active substances from the group of the benzoylcyclohexanediones and also safeners. These herbicidal compositions are especially suitable for use against weed plants in crop plant cultures.
Combination of herbicides and safeners
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, (2008/06/13)
A herbicidally active composition comprises a mixture of A. a herbicidally effective amount of one or more compounds of the formula (I), ?and B. an antidote-effective amount of one or more compounds of the formulae (II) to (IV),
COMBINATIONS OF HERBICIDES AND SAFENERS
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, (2008/06/13)
There are described herbicidal compositions which comprise at least one herbicidally active compound of the formula (I) and at least one crop-plant-protecting compound as safener. In this formula (I), V is an optionally substituted radical selected from the group consisting of isoxazol-4-yl, pyrazol-4-yl, cyclohexane-1,3-dion-2-yl and 3-oxopropionitril-2-yl and R9 is nitro, amino, halogen or a carbon-containing radical. The group of the safeners contains, for example, 2,4-D, cyometrinil, dicamba, dymron, fenclorim, flurazole, fluxofenim, lactidichlor, MCPA, mecoprop, MG-191, oxabetrinil, methyl diphenylmethoxyacetate, 1-[4-(N-2-methoxybenzoylsulfamoyl)phenyl]-3-methylurea, 1,8-naphthalaic anhydride, 1-[4-(N-2-methoxybenzoylsulfamoyl)phenyl]-3,3-dimethylurea, 1-[4-(N-4,5-dimethylbenzoylsulfamoyl)phenyl]-3-methylurea, 1-[4-(N-naphthoylsulfamoyl)phenyl]-3,3-dimethylurea, (4-chlorophenoxy)acetic acid, 4-(2,4-dichlorophenoxy)butyric acid, 4-(4-chloro-o-tolyloxy)butyric acid, 4-(4-chlorophenoxy)butyric acid, in each case their acids and esters, N-acylsulfonamides, N-acylsulfamoyl-benzamides, in each case, if appropriate, also in salt form and in each case optionally substituted 1-phenylpyrazoline, 1-phenylpyrazole, 1-phenyl-triazole, 5-phenylisoxazoline and 5-phenylmethylisoxazoline-3-carboxylic esters and 2-(8-quinolinyloxy)acetic acid derivatives.
A New Class of Antiarrhythmic Agents: Mannich Bases of 3,4-Dihydro-1-benzoxepin-5(2H)-ones and Related Compounds
Khanna, J. M.,Tandon, V. K.,Kar, K.,Sur, R. N.
, p. 71 - 77 (2007/10/02)
Mannich bases derived from 3,4-dihydro-1-benzoxepin-5(2H)-ones, chromanones and 6,7,8,9-tetrahydrobenzocyclohepten-5(H)-one have been synthesised and shown to possess marked antiarrhythmic activity; 3,4-dihydro-7-methyl-4-(1-piperidinomethyl)- and 3,4-dih