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ANTIBIOTIC COMPOUNDS

The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.

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Isoxazole – Wikipedia,
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6-SULFONYLAMINO QUINOLINE COMPOUNDS AS PLANT GROWTH REGULATORS

The present invention relates to novel sulfonamide derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants, improving plant tolerance to abiotic stress (including environmental and chemical stresses) and/or inhibiting the germination of seeds.

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2,1-benzothiazine 2,2-dioxides. 3*. 4-hydroxy-1-methyl-2,2-dioxo-n- (1,3-thiazol-2-yl)-1H-2lambda6,1-benzothiazine-3-carboxamides – A new group of potential analgetics

We have developed an effective synthetic method and prepared several 4-hydroxy-1-methyl-2,2-dioxo-N-(1,3-thiazol-2-yl)-1H-2lambda6,1- benzothiazine-3-carboxamides and a few structurally related heterocyclic arylamides. The structural features of one of the substituted thiazolyl-2-amides obtained have been investigated. Compounds with a high analgesic activity have been identified within this group by pharmacological screening.

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Synthesis and antimicrobial evaluation of isoxazole-substituted 1,3,4-oxadiazoles

Synthesis of N-(5-methylisoxazol-3-yl)-2-(5-aryl-1,3,4-oxadiazol-2-yl)acetamides 5a-k was achieved from readily available materials. The compounds were screened for their in vitro antimicrobial activity against representative bacterial and fungal strains. Compounds 5b, 5d and 5f exhibit good activity.

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Isoxazole – Wikipedia,
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Directed lithiation of N-(tert-butoxycarbonyl)aminoisoxazole: Synthesis of 4-substituted aminoisoxazoles

Directed lithiation of 3-(Boc-amino)isoxazole 4 and 5-(Boc-amino)isoxazole 9 is described. Dilithioisoxazoles reacted with a variety of electrophiles to give the corresponding 4-substituted isoxazoles.

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Aerobic degradation of sulfadiazine by arthrobacter spp.: Kinetics, pathways, and genomic characterization

Two aerobic sulfadiazine (SDZ) degrading bacterial strains, D2 and D4, affiliated with the genus Arthrobacter, were isolated from SDZ-enriched activated sludge. The degradation of SDZ by the two isolates followed first-order decay kinetics. The half-life time of complete SDZ degradation was 11.3 h for strain D2 and 46.4 h for strain D4. Degradation kinetic changed from nongrowth to growth-linked when glucose was introduced as the cosubstrate, and accelerated biodegradation rate was observed after the adaption period. Both isolates could degrade SDZ into 12 biodegradation products via 3 parallel pathways, of which 2-amino-4-hydroxypyrimidine was detected as the principal intermediate product toward the pyrimidine ring cleavage. Compared with five Arthrobacter strains reported previously, D2 and D4 were the only Arthrobacter strains which could degrade SDZ as the sole carbon source. The draft genomes of D2 and D4, with the same completeness of 99.7%, were compared to other genomes of related species. Overall, these two isolates shared high genomic similarities with the s-triazine-degrading Arthrobacter sp. AK-YN10 and the sulfonamide-degrading bacteria Microbacterium sp. C448. In addition, the two genomes contained a few significant regions of difference which may carry the functional genes involved in sulfonamide degradation.

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BETA-LACTAM ANTIBACTERIAL AGENTS

Compounds of the formula wherein A is one of the following: in which R1, is acyl, R2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R3 is hydrogen or lower alkyl and R4 and R4′ are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.

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Synthesis of spiro heterocyclic systems from 2-(3-oxoisobenzofuran-1(3H)-ylidene)malononitrile and binucleophiles

The reaction of 2-(3-oxoisobenzofuran-1(3H)-ylidene)malononitrile, generated from phthalic anhydride and malononitrile, with different binucleophiles led to the formation of spiro heterocycles possessing a phthalide ring system in good yields.

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A new synthesis method of N-substituted spiro terpene aza-diperoxides

[Figure not available: see fulltext.] An efficient method has been developed for the synthesis of new spiro terpene aza-diperoxides by heterocyclization of bishydroperoxides with N-aryl-N,N-bis(methoxymethyl)amines in the presence of EuCl3/gamma-Al2O3 as a catalyst. The assignment of signals in the NMR spectra of the synthesized compounds was performed taking into account the dynamics of the conformation of the tetraoxazocane ring with two rigid peroxide bonds. Structures of some aza-diperoxides were determined by X-ray structural analysis.

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An efficient and novel protocol for the synthesis of spiro[1,3]oxazino[5,6-c]quinoline derivatives by one-pot, three-component reaction

Abstract: One-pot, three-component reaction of various aryl glyoxal monohydrates, 5-methylisoxazol-3-amine and 4-hydroxyquinolin-2(1H)-one in the presence of a catalytic amount of DBU in H2O/EtOH (1:1) at 50?C produced the 4-aroyl-5?-methyl-3,4-dihydro-2?H-spiro[[1,3]oxazino[5,6-c]quinoline-2,3?-isoxazol]-5(6H)-one derivatives containing spiro[1,3]oxazino[5,6-c]quinoline moiety in 82?89% yield. The high yields of products, easy work-up, and availability of starting materials are the main advantages of this synthetic strategy. Graphic abstract: [Figure not available: see fulltext.]

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Isoxazole – Wikipedia,
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