- Structure of cytochrome P450 PimD suggests epoxidation of the polyene macrolide pimaricin occurs via a hydroperoxoferric intermediate
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We present the X-ray structure of PimD, both substrate-free and in complex with 4,5-desepoxypimaricin. PimD is a cytochrome P450 monooxygenase with native epoxidase activity that is critical in the biosynthesis of the polyene macrolide antibiotic pimaricin. Intervention in this secondary metabolic pathway could advance the development of drugs with improved pharmacologic properties. Epoxidation by P450 typically includes formation of a charge-transfer complex between an oxoferryl π-cation radical species (Compound I) and the olefin π-bond as the initial intermediate. Catalytic and structural evidence presented here suggest that epoxidation of 4,5-desepoxypimaricin proceeds via a hydroperoxoferric intermediate (Compound 0). The oxygen atom of Compound 0 distal to the heme iron may insert into the double bond of the substrate to make an epoxide ring. Stereoelectronic features of the putative transition state suggest substrate-assisted proton delivery.
- Kells, Petrea M.,Ouellet, Hugues,Santos-Aberturas, Javier,Aparicio, Jesus F.,Podust, Larissa M.
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- SEED TREATMENT COMPOSITION
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The present invention relates to novel compositions for treating seeds. Moreover, the present invention is directed to the production of these compositions and the uses of these compositions.
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- POLYENE ANTIBIOTICS, COMPOSITIONS CONTAINING SAID ANTIBIOTICS, METHOD AND MICRO-ORGANISMS USED TO OBTAIN SAME AND APPLICATIONS THEREOF
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Abstract: The invention relates to novel polyenes having formula (I), wherein: R1 represents alkyl C1-C3; and R2 represents a functional group selected from CH3- or CONH2- (methyl- or primary amide-). The aforementioned polyenes have a biocide action on organisms comprising cell membranes that contain ergosterol, e.g., fungi or parasites. Said compounds can be obtained using a method that consists in cultivating a producing micro-organism under conditions that enable the production thereof. In addition, the invention also relates to a mechanism for the in vitro production of amidated polyenes, consisting in incubating carboxylated polyenes with cell-free extracts (or proteinaceous fractions) of the producers of same in the presence of ATP/Mg++ and an amide-group donor compound (preferably glutamine).
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(2008/06/13)
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- Substituted imide derivatives
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The present invention relates to novel substituted imide derivatives of the general formula (I) in which R1 represents optionally substituted cycloalkyl, R2 represents optionally substituted alkyl or optionally substituted cycloalkyl, R3 represents alkyl, alkoxy, alkylthio, amino, alkylamino or dialkylamino and R4 represents cyano or nitro, and to processes for their preparation and to their use for controlling animal pests and as herbicides.
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- Pyrazolyl benzyl ether derivatives containing a fluoromethoxyimino group and use thereof as pesticides
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The invention relates to novel pyrazolyl benzyl ethers, to a plurality of processes for their preparation and to their use for controlling harmful organisms.
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- Iminoacetic acid amides and their use as pest control agents
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PCT No. PCT/EP96/04345 Sec. 371 Date Apr. 15, 1998 Sec. 102(e) Date Apr. 15, 1998 PCT Filed Oct. 7, 1996 PCT Pub. No. WO97/14673 PCT Pub. Date Apr. 24, 1997Iminoacetamides of the formula (I) in which A represents a single bond or optionally substituted alkylene, Q represents oxygen or sulphur, R1 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl, R2 represents respectively optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl, R3 represents hydrogen or respectively optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R4 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclcyl a process for their preparation, pesticidal compositions containing them, and their use for controlling pests.
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- 2-and 2,5-substituted phenylketoenols
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PCT No. PCT/EP97/03973 Sec. 371 Date Jan. 28, 1999 Sec. 102(e) Date Jan. 28, 1999 PCT Filed Jul. 23, 1997 PCT Pub. No. WO98/05638 PCT Pub. Date Feb. 12, 1998The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.
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- Microbicidal benzotriazoles
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Novel benzotriazoles of the formula STR1 in which R, X1, X2, X3, X4 and Y have the meanings given in the description, and their acid addition salts and metal salt complexes, a process for the preparation of these substances and their use as microbicides in crop protection and in material protection.
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- Halogen alkenyl azolyl microbicides
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Novel halogenoalkenyl-azolyl derivatives of the formula STR1 in which R1 represents optionally substituted alkyl, optionally substituted alkenyl, optionally substituted cycloalkyl, optionally substituted aryl or represents optionally substituted heteroaryl, R2 represents alkyl, halogenoalkyl, 1-hydroxyalkyl, 2-hydroxyalkyl, 1-hydroxyhalogenalkyl, 1-alkenyl or 2-alkenyl, X1 represents fluorine, chlorine, bromine or iodine, X2 represents fluorine, chlorine, bromine or iodine, and Y represents nitrogen or a CH group, and addition products thereof with acids or metal salts are very active as microbicides in plant protection and in the protection of materials.
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- Substituted biphenyl oxazolines
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The invention relates to new substituted biphenyloxazolines of the formula (I) STR1 in which R1 represents C1 -C6 -halogenoalkylthio and R2 represents hydrogen, or R1 and R2 together with the carbon atoms to which they are bonded form a halogen-substituted 5- or 6-membered heterocyclic ring, X represents hydrogen, halogen, C1 -C6 -alkyl or C1 -C6 -alkoxy, and m represents 0, 1 or 2, to processes for their preparation, to new intermediates, and to the use of the substituted biphenyloxazolines for combating animal pests, with the exception of the compound of the formula STR2
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- Acylated 5-aminopyrazoles and the use thereof to combat animal parasites
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The present invention relates to new acylated 5-aminopyrazoles of the formula (I) STR1 in which R1, R2, R3, R4 and R5 have the meaning given in the description, to processes for their preparation and to their use as pesticides.
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- Substituted tetrahydro-5-nitro-pyrimidines
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The present invention relates to novel substituted in that one tetrahydro-5-nitro-pyrimidine of the formula (I), according to claim 1, STR1 in which n, R1, R2 have the meaning given in the description, to a process for its preparation and to its use for combating animal pests, especially insects, arachnids and nematodes, which are encountered in agricultural, in forestry, in the protection of stored products and of materials and, in the hygiene sector.
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