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Synthesis and biological evaluation of novel 1beta-methylcarbapenems with isothiazoloethenyl side chains

The synthesis of novel 1beta-methylcarbapenems 1a,b bearing isothiazoloethenyl moieties at C-5 position of pyrrolidine ring and their biological evaluation are described. Both compounds showed potent and well-balanced antibacterial activity as well as high stability to DHP-I. Especially, 5-isothiazole derivative 1a exhibited excellent DHP-I stability and advanced pharmacokinetics profiles, compared to 5-isoxazole derivative 2, imipenem, and meropenem.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Volatile compounds of past?rma under different curing processes

The effects of different curing processes (curing temperature 4C or 10C and curing agent 150?mg/kg nitrite or 300?mg/kg nitrate) on the volatile compound profile of the past?rma (Turkish dry-cured meat product) have been investigated. A total of 45 volatile compounds, including alcohols, aldehydes, ketones, aliphatic and aromatic hydrocarbons, terpenes, sulphur compounds, esters, furans and nitrogenous compounds have been identified in past?rma samples. The curing temperature did not have a significant effect on any compound. The curing agent had statistically a significant or very significant influence on 12 compounds. In general, the use of nitrate increased the amount of volatile compound. However, lower mean hexanal value was determined in past?rma samples cured with nitrite than those cured with nitrate. Practical applications: Past?rma is a traditional dry-cured meat product. It is produced from whole muscle and/or mucsles of certain parts of beef or water buffalo carcasses. In curing stage, nitrate was used generally. However, nitrite can be used alone or with nitrate in this stage. In this study, the effects of different curing conditions (150?mg/kg nitrite or 300?mg/kg nitrate and 4C or 10C) on volatile compounds of past?rma were investigated. According to the results, past?rma produced with nitrate generally showed higher amounts of volatile compounds. On the other hand, curing temperature was not significant factor in terms of volatile compounds.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Arsoles, stiboles, and bismoles

The developments in the synthesis of the five-membered heterocycles with one pnictogen (As, Sb, Bi) heteroatom have in the last 15 years or so been practically focused only on three types of compounds: saturated or unsaturated pnictogenoles, monofused pnictogenoles, and diffused pnictogenoles, where the fused ring is benzene, thiophene, isothiazole, benzothiophene, or benzofuran. Trendy is preparation and tuning of the optoelectronic properties of the target compounds, their complexes or polymers, respectively. Almost all syntheses of nearly all systems are based on transmetallation of lithium (for 1,3-diene known as Ashe’s method), potassium, Grignard, copper, titanium, or zirconium species (Fagan?Nugent zirconium metallacycle-transfer method), regardless of whether the system is saturated (as is the case for the majority of compounds) or unsaturated.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Five-Membered Ring Systems: With N and S Atoms

This review chapter describes the syntheses and reactions of five-membered heterocyclic ring systems containing nitrogen and sulfur published in 2017.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Isoxazolyl and isothiazolyl aromatase inhibitors

This invention provides certain isoxazole and isothiazole derivatives, their pharmaceutical formulations, and their use in inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Heterocyclic Analogues of Chlorcyclizine with Potent Hypolipidemic Activity

A series of piperazines was synthesized and their effect of reducing serum cholesterol and triglyceride levels in the rat was evaluated.A systematic exploration of the structure-activity relationships led to the synthesis of (R,S)-(3,5-dimethylisoxazol-4-yl)<4-(1-methylethyl)phenyl>(4-methylpiperazin-1-yl)methane dihydrochloride (M and B 31426), which had potent activity in lowering serum lipid levels at a daily oral dose of 2 mg/kg and was 100 times more potent than clofibrate.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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The proton affinities of saturated and unsaturated heterocyclic molecules

The proton affinities derived from G3-calculations of 23 five-membered ring heteroaromatic molecules agree well with the experimentally determined values available in the literature. The calculated local proton affinities show that the principal site of protonation of the heteroaromatic compounds examined is an atom of the ring, carbon when there is only one heteroatom in the ring, and nitrogen where there are two or more heteroatoms. The experimental proton affinities of non-aromatic cyclic ethers, amines and thioethers are also in excellent agreement with the calculated values, with two exceptions (oxetane, N-methylazetidine). The literature proton affinities of the four simple cyclic ethers, oxetane, tetrahydrofuran, tetrahydropyran and oxepane were confirmed by Fourier Transform Ion Cyclotron Resonance (FT-ICR) mass spectrometry, in order to examine the disagreement between the values predicted by extrapolation or additivity for tetrahydrofuran and tetrahydropyran and those determined by experiment and by calculation. The proton affinity differences between the pairs tetrahydropyran/1,4-dioxane, piperidine/morpholine and related compounds show that introduction of an additional oxygen atom in the ring considerably lowers the basicity.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Time-Resolved Photoelectron Studies of Thiophene and 2,5-Dimethylthiophene

The photoinduced dynamics of thiophene and 2,5-dimethylthiophene (2,5-DMT) were investigated upon excitation at 200 and 255 nm (2,5-DMT only) using time-resolved photoelectron spectroscopy and compared with results from ab initio coupled cluster calculations. For thiophene, depopulation of the initially excited B2(pi3pi4?) state to the lower-lying A1(pi2pi4?) state occurs within 25 ¡À 20 fs, with a subsequent bifurcation into a ring-puckering channel and a ring-opening channel with lifetimes of 80 ¡À 20 and 450 ¡À 50 fs, respectively. For 2,5-DMT, the dynamics following excitation at 200 nm is described by a monoexponential decay with a time constant of 120 ¡À 20 fs, while that following excitation at 255 nm is best fit by a biexponential decay with time constants of 115 ¡À 20 fs and 15 ¡À 3 ps, respectively. The fast signal observed after excitation of 2,5-DMT is assigned to the ring-opening channel, which is favored with respect to thiophene due to a lower excited-state barrier along the ring-opening coordinate and an increased inertia toward the ring-puckering channel. Coupled cluster calculations have been undertaken to compare the relaxation dynamics of thiophene to thiazole and isothiazole. For the latter two molecules, we find a strong gradient along the ring-opening coordinate in the Franck-Condon region of the initially populated pipi? state and predict that ring-opening is the dominating relaxation channel after photoexcitation. We use the extracted information for a comparison of the thiophene dynamics with the light-induced processes observed in other five-membered heterocyclic molecules.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Benzo-fused cyclic compounds

Herbicidal benzo-fused cyclic compounds of the formula STR1 wherein Q is STR2 Y is O or S, W is STR3 T is O, S, –NH– or STR4 and R4 may represent, together with T, chlorine, Z is O or S, X is hydrogen or halogen, n is 0 or 1 and R is C3-6 cycloalkyl, an optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms, and salts thereof.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Application of 288-16-4, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Chapter, and a compound is mentioned, 288-16-4, Isothiazole, introducing its new discovery.

Metal-catalyzed direct arylation of 1,2-azoles

Over the last 20 years, there has been significant progress in the direct CH (het)arylation chemistry of a wide variety of (het)arenes. Herein, the application of direct CH arylation on the 1,2-azoles: pyrazoles, isothiazoles, and isoxazoles and their annulated analogues is reviewed starting from the first arylation methods on 1,2-azoles until 2018.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com