Heterocyclic Building Blocks-Isothiazole

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HETEROARYL-SUBSTITUTED SULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to pyridine- and thiophene-sulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/ or epileptic seizure disorders.

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

 

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3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds

There are disclosed compounds of the formula, STR1 where n is 0, 1 or 2; A is STR2 where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, STR3 or aryl except that when R1 is STR4 or aryl, R2 is hydrogen, or alternatively R1 +R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3 +R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: isothiazole, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 288-16-4, Name is Isothiazole, molecular formula is C3H3NS

Synthesis and application of stable nitroxide free radicals fused with carbocycles and heterocycles

Stable nitroxide free radicals have traditionally been associated with 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) or its 4-substituted derivatives as relatively inexpensive and readily accessible compounds with limited possibilities for further chemical modification. Over the past two decades, there has been a resurgence of interest in stable free radicals with proper functionalization tuned for various applications. The objective of this review is to present recent results with synthetic methodologies to achieve stable nitroxide free radicals fused with aromatic carbocycles and heterocycles. There are two main approaches for accessing stable nitroxide free radicals fused with arenes, e.g., isoin-doline-like nitroxides: further functionalization and oxidation of phthalimide or inventive functionalization of pyrroline nitroxide key compounds. The latter also offers the con-structions of versatile heterocyclic scaffolds (furan, pyrrole, thiophene, 1,2-thiazole, selenophene, pyrazole, pyrimidine, pyridine, pyridazine, 1,5-benzothiazepine) that are fused with pyrroline or tetrahydropyridine nitroxide rings. The possible applications of these new stable nitroxide free radicals, such as covalent spin labels and noncovalent spin probes of proteins and nucleic acids, profluorescent probes, building blocks for construction of dual active drugs and electroactive materials, and substances for controlled free radical polymerization, are discussed.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

288-16-4, Name is Isothiazole, belongs to isothiazole compound, is a common compound. Formula: C3H3NSIn an article, once mentioned the new application about 288-16-4.

PDE7-selective and dual inhibitors: Advances in chemical and biological research

Phosphodiesterase 7 (PDE7) is an intracellular enzyme that specifically hydrolyzes the second messenger, cyclic-3?,5?-adenosine monophosphate (cAMP), into inactive noncyclic nucleotide, 5?-AMP. To date, many structurally diverse compounds with PDE7 inhibitory properties have been described, including selective PDE7 inhibitors, dual PDE4/PDE7, PDE7/PDE8, and PDE7/GSK-3 inhibitors, and non-selective PDE inhibitors with high affinity for PDE7. Inhibitors of PDE7 have provided beneficial effects in animal models of inflammatory and neurological disorders, including Alzheimer?s disease, Parkinson?s disease, multiple sclerosis, and many others. This review is a comprehensive summary of the current state-of-the-art in the field of design and synthesis of PDE7 inhibitors, their physicochemical properties, biological evaluation, and structure-activity relationships as well as it highlights the updated evidence for a potential therapeutic utility of these compounds. Moreover, new approaches to obtain more effective and safer PDE7 inhibitors than those available now are presented.

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

 

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Process for the preparation of substituted pyrrolidine derivatives and intermediates

Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

27148-03-4, Name is Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide, belongs to isothiazole compound, is a common compound. Formula: C7H5NO2S2In an article, once mentioned the new application about 27148-03-4.

A comparative study of the coordination of saccharinate (sac), thiosaccharinate (tsac) and benzisothiazolinate (bit) ligands to trans-[PdCl2(H2NBz)2]: molecular structure of cis-[Pd(bit)2(H2NBz)2]

A comparative study of reactions of saccharinate (sac), thiosaccharinate (tsac) and benzisothiozolinate (bit) with trans-[PdCl2(H2NBz)2] is reported. While in all cases substitution of both chlorides occurs, product types differ for the three closely related ligands. With sodium saccharinate, trans-[Pd(N-sac)2(H2NBz)2] results in which the sac ligands are N-bound. A similar N-bound coordination is observed with sodium benzisothiazolinate, but a crystal structure shows that they adopt a mutual cis arrangement in cis-[Pd(N-bit)2(H2NBz)2]. In contrast, with sodium thiosaccharinate it is proposed that the new ligands adopt an S-bound coordination mode in trans-[Pd(S-tsac)2(H2NBz)2].

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Quality Control of Benzo[d]isothiazole, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 272-16-2, name is Benzo[d]isothiazole. In an article£¬Which mentioned a new discovery about 272-16-2

A survey of core replacements in indole-based HIV-1 attachment inhibitors

Indole- and azaindole-based glyoxylyl amide derivatives have been described as HIV-1 attachment inhibitors (AIs) that act by blocking the interaction between the viral gp120 coat protein and the human host cell CD4 receptor. As part of an effort to more deeply understand the role of the indole/azaindole heterocycle in the expression of antiviral activity, a survey of potential replacements was conducted using parallel synthesis methodology. The design and optimization was guided by a simple 2-dimensional overlay based on an overall planar topography between the indole/azaindole and C-7 substituents that had been deduced from structure-activity studies leading to the discovery of temsavir (3). 2-Substituted naphthalene- and quinoline-derived chemotypes emerged as the most interesting prototypes, with C-5 and C-6 substituents enhancing antiviral potency. Despite the fact that neither of these chemotypes incorporated a H-bond donor that has been shown to engage the side chain carboxylate of Asp113 in gp120, the antiviral potency of several analogues met or exceeded that of 3, demonstrating that engaging Asp113 is not a prerequisite for potent antiviral activity.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

Application of 288-16-4, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 288-16-4, Name is Isothiazole, molecular formula is C3H3NS. In a Article£¬once mentioned of 288-16-4

Spin-Spin Couplings Between 13C Nuclei in Five-Membered Heteroaromatic Ring Systems

A set of 1J(CC) spin-spin coupling constants are reported for 11 five-membered heteroaromatic molecules, including all relevant diazole, triazole, oxazole, oxadiazole, thiazole and thiadiazole systems.The coupling show a clear distinction between carbon-carbon bonds which are formally double or single, respectively.There seems to be no correlation of the couplings with the bond lengths concerned, in spite of some apparent trends.Potential applications of the couplings are discussed in assessing the aromaticity of five-membered heterocycles. – Keywords: 13C NMR Carbon-carbon coupling constants Heteroaromatic five-membered rings Diazoles Triazoles Oxazoles Oxadiazoles Thiazoles Thiadiazoles

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Medicinal chemistry perspective of fused isoxazole derivatives

Nitrogen containing heterocyclic rings with an oxygen atom is considered as one of the best combination in medicinal chemistry due to their diversified biological activities. Isoxazole, a five membered heterocyclic azole ring is found in naturally occuring ibetonic acid along with some of the marketed drugs such as valdecoxib, flucloxacillin, cloxacillin, dicloxacillin, and danazol. It is also significant for showing antipsychotic activity in risperidone and anticonvulsant activity in zonisamide, the marketed drugs. This review article covers research articles reported till date covering biological activity along with SAR of fused isoxazole derivatives.

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