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The increasing prevalence of drug-resistant bacterial infections is driving the discovery and development not only of new antibiotics, but also of inhibitors of virulence factors that are crucial for in vivo pathogenicity. One such virulence factor is the type III secretion system (T3SS), which plays a critical role in the establishment and dissemination of Pseudomonas aeruginosa infections. We have recently described the discovery and characterization of a series of inhibitors of P. aeruginosa T3SS based on a phenoxyacetamide scaffold. To better characterize the factors involved in potent T3SS inhibition, we have conducted a systematic exploration of this structure, revealing several highly responsive structure-activity relationships indicative of interaction with a specific target. Most of the structural features contributing to potency were additive, and combination of those features produced optimized inhibitors with IC50 values <1 muM. I am very proud of our efforts over the past few months and hope to 214894-89-0 help many people in the next few years. Related Products of 214894-89-0

Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C8 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; is linear C2-3 alkylene,; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR9 2, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR9 2 SO2NR9 2, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10) aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or f urther substituted by one or more F, Cl, Br, CN, NH2, NR3 2, NO2, CF3; and R9 is selected from H and a group R8 as hereinbefore defined; n7 and n8 and the sum thereof are independently selected from zero and the whole number integer 1 to 4; processes for the preparation thereof, compositions and uses.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The efficient Cu-catalyzed esterification of sulfonyl hydrazides with alcohols in air is described, providing sulfinic esters in good yields and broad scope. Mechanistic studies suggest that the reaction likely proceeds through free-radical formation including arylthio radical and arylsulfonyl radical, while arylsulfuric acid are the major esterification intermediate in this transformation.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Hydroboration of fluorinated styrenes with common hydroborating agents results in polymerization. However, regioselective hydroboration has been achieved by utilizing iodoborane-dimethyl sulfide. A series of fluorinated beta-phenethyl alcohols and amines were synthesized via this methodology.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A containing 1, 4 – benzodioxane of benzene and 1, 2, 4 – triazole class derivatives, has the following general formula: In the formula R is: The invention containing 1, 4 – benzodioxane of benzene and 1, 2, 4 – triazole class derivatives to the bacillus subtilis (B. subtilis), Staphylococcus aureus (S. aureus), Escherichia coli (E.coli), Pseudomonas aeruginosa (P. aeruginosa) is markedly inhibited, so this invention containing 1, 4 – benzodioxane of 1, 2, 4 – triazole class derivatives can be in preparing antibacterial drug application. The invention discloses the preparation method. (by machine translation)

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A photoredox and Br°nsted acid synergistically catalyzed cross-dehydrogenative C?O coupling reaction is developed in which isochroman peroxyacetals are formed through sp3 C?H bond peroxidation. The reported method is characterized by its extremely mild reaction conditions, excellent yields, and broad substrate scope. An oxocarbenium ion p-chlorobenzenesulfonate was speculated to be the reactive intermediate. The role of hemiacetals and oxygenated dimers on the effective stabilization of the oxocarbenium ion was investigated; the presence of acid appeared to establish equilibrium between hemiacetals and oxygenated dimers with the oxocarbenium ion pairs. The broad applicability of the method highlights the potential of the protocol for molecule synthesis.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The M5 muscarinic acetylcholine receptor is suggested to be a potential pharmacotherapeutic target for the treatment of drug abuse. We describe herein the discovery of a series of M5-preferring orthosteric antagonists based on the scaffold of 1,2,5,6-tetrahydropyridine-3- carboxylic acid. Compound 56, the most selective compound in this series, possesses an 11-fold selectivity for the M5 over M1 receptor and shows little activity at M2-M4. This compound, although exhibiting modest affinity (Ki = 2.24 muM) for the [3H]N-methylscopolamine binding site on the M5 receptor, is potent (IC50 = 0.45 nM) in inhibiting oxotremorine-evoked [3H]DA release from rat striatal slices. Further, a homology model of human M5 receptor based on the crystal structure of the rat M3 receptor was constructed, and docking studies of compounds 28 and 56 were performed in an attempt to understand the possible binding mode of these novel analogues to the receptor.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The disclosure generally relates to compounds of formula I, II, III and IV, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Benzyl esters and thiolesters of 4-aryl-3-butenoic acids, intermediates therefor, synthesis thereof, and the use of said esters and thiolesters for the control of pests.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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The promiscuity of the enzyme norcoclaurine synthase is described. This biocatalyst yielded a diverse array of substituted tetrahydroisoquinolines by cyclizing dopamine with various acetaldehydes in a Pictet-Spengler reaction. This enzymatic reaction may provide a biocatalytic route to a range of tetrahydroisoquinoline alkaloids.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem