Tag: 200-300

On May 16, 2006, Masuda, Masami; Suzuki, Nobuyuki; Taniguchi, Sayuri; Oikawa, Takayuki; Nonaka, Takashi; Iwatsubo, Takeshi; Hisanaga, Shin-ichi; Goedert, Michel; Hasegawa, Masato published an article.COA of Formula: C14H12N2S The title of the article was Small Molecule Inhibitors of α-Synuclein Filament Assembly. And the article contained the following:

α-Synuclein is the major component of the filamentous inclusions that constitute defining characteristics of Parkinson’s disease and other α-synucleinopathies. Here we have tested 79 compounds belonging to 12 different chem. classes for their ability to inhibit the assembly of α-synuclein into filaments in vitro. Several polyphenols, phenothiazines, porphyrins, polyene macrolides, and Congo red and its derivatives, BSB and FSB, inhibited α-synuclein filament assembly with IC50 values in the low micromolar range. Many compounds that inhibited α-synuclein assembly were also found to inhibit the formation of Aβ and tau filaments. Biochem. anal. revealed the formation of soluble oligomeric α-synuclein in the presence of inhibitory compounds, suggesting that this may be the mechanism by which filament formation is inhibited. Unlike α-synuclein filaments and protofibrils, these soluble oligomeric species did not reduce the viability of SH-SY5Y cells. These findings suggest that the soluble oligomers formed in the presence of inhibitory compounds may not be toxic to nerve cells and that these compounds may therefore have therapeutic potential for α-synucleinopathies and other brain amyloidoses. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).COA of Formula: C14H12N2S

The Article related to alpha synuclein filament inhibitor polyphenol phenothiazine amyloid beta tau, parkinson disease protofibril alpha synuclein nerve cytotoxicity, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.COA of Formula: C14H12N2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 29, 2013, Megill, Andrea; Lee, Taehee; DiBattista, Amanda Marie; Song, Jung Min; Spitzer, Matthew H.; Rubinshtein, Mark; Habib, Lila K.; Capule, Christina C.; Mayer, Michael; Turner, R. Scott; Kirkwood, Alfredo; Yang, Jerry; Pak, Daniel T. S.; Lee, Hey-Kyoung; Hoe, Hyang-Sook published an article.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was A tetra(ethylene glycol) derivative of benzothiazole aniline enhances Ras-mediated spinogenesis. And the article contained the following:

The tetra(ethylene glycol) derivative of benzothiazole aniline, BTA-EG4, is a novel amyloid-binding small mol. that can penetrate the blood-brain barrier and protect cells from Aβ-induced toxicity. However, the effects of Aβ-targeting mols. on other cellular processes, including those that modulate synaptic plasticity, remain unknown. We report here that BTA-EG4 decreases Aβ levels, alters cell surface expression of amyloid precursor protein (APP), and improves memory in wild-type mice. Interestingly, the BTA-EG4-mediated behavioral improvement is not correlated with LTP, but with increased spinogenesis. The higher dendritic spine d. reflects an increase in the number of functional synapses as determined by increased miniature EPSC (mEPSC) frequency without changes in presynaptic parameters or postsynaptic mEPSC amplitude. Addnl., BTA-EG4 requires APP to regulate dendritic spine d. through a Ras signaling-dependent mechanism. Thus, BTA-EG4 may provide broad therapeutic benefits for improving neuronal and cognitive function, and may have implications in neurodegenerative disease therapy. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to benzothiazole aniline tetraethylene glycol derivative ras protein spinogenesis neuroprotectant, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On March 4, 2005, Taniguchi, Sayuri; Suzuki, Nobuyuki; Masuda, Masami; Hisanaga, Shin-ichi; Iwatsubo, Takeshi; Goedert, Michel; Hasegawa, Masato published an article.Category: thiazole The title of the article was Inhibition of Heparin-induced Tau Filament Formation by Phenothiazines, Polyphenols, and Porphyrins. And the article contained the following:

Tau protein is the major component of the intraneuronal filamentous inclusions that constitute defining neuropathol. characteristics of Alzheimer’s disease and other tauopathies. The discovery of tau gene mutations in familial forms of frontotemporal dementia has established that dysfunction of the tau protein is sufficient to cause neurodegeneration and dementia. Here we have tested 42 compounds belonging to nine different chem. classes for their ability to inhibit heparin-induced assembly of tau into filaments in vitro. Several phenothiazines (methylene blue, azure A, azure B, and quinacrine mustard), polyphenols (myricetin, epicatechin 5-gallate, gossypetin, and 2,3,4,2′,4′-pentahydroxybenzophenone), and the porphyrin ferric deuteroporphyrin IX inhibited tau filament formation with IC50 values in the low micromolar range as assessed by thioflavin S fluorescence, electron microscopy, and Sarkosyl insolubility Disassembly of tau filaments was observed in the presence of the porphyrin phthalocyanine. Compounds that inhibited tau filament assembly were also found to inhibit the formation of Aβ fibrils. Biochem. anal. revealed the formation of soluble oligomeric tau in the presence of the inhibitory compounds, suggesting that this may be the mechanism by which tau filament formation is inhibited. The compounds investigated did not affect the ability of tau to interact with microtubules. Identification of small mol. inhibitors of heparin-induced assembly of tau will form a starting point for the development of mechanism-based therapies for the tauopathies. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Category: thiazole

The Article related to tau filament inhibition phenothiazine polyphenol porphyrin amyloid fibril, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 18, 2008, Gaufreteau, Delphine; Nettekoven, Matthias; Plancher, Jean-Marc; Roche, Olivier; Schmitt, Sebastien; Takahashi, Tadakatsu published a patent.Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide The title of the patent was Preparation of cyclohexyl piperazinyl methanones as modulators of histamine H3 receptors.. And the patent contained the following:

Title compounds [I; R1 = alkyl, cycloalkyl; R2 = (substituted) heteroarylphenyl, heterocyclylphenyl, heteroaryl], were prepared Thus, cis-4-hydroxycyclohexanecarboxylic acid, 1-cyclobutylpiperazine dihydrochloride, TBTU, and diisopropylethylamine were stirred together for 8 h at room temperature in DMF to give 76% amide, which was stirred with 4-(1,2,4-triazol-1-yl)phenol, Ph3P, and di-tert-Bu azodicarboxylate in THF for 72 h to give 11% trans-(4-cyclobutylpiperazin-1-yl)-[4-[4-[1,2,4]triazol-1-ylphenoxy]cyclohexyl]methanone. The latter showed a Ki value of 6.5 nM in an H3 binding assay. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide

The Article related to cyclohexyl piperazinyl methanone preparation histamine h3 receptor modulator, obesity diabetes treatment cyclohexylcarbonylpiperazine preparation antihistamine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of 2-Bromo-N-methylthiazole-4-carboxamide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On August 31, 2008, Ukrainets, I. V.; Tkach, A. A.; Grinevich, L. A. published an article.HPLC of Formula: 92-36-4 The title of the article was 4-Hydroxy-2-quinolones 148. Synthesis and antitubercular activity of 1-hydroxy-3-oxo-6,7-dihydro-3H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid N-R-amides. And the article contained the following:

A method for the synthesis of the title compound [i.e., 1-hydroxy-3-oxo-6,7-dihydro-3H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid N-amides] is reported here. A reaction of 1,2,3,4-tetrahydroquinoline with methanetricarboxylic acid 1,1,1-tri-Et ester provided an ester compound [i.e., 2,3-dihydro-7-hydroxy-5-oxo-1H,5H-benzo[ij]quinolizine-6-carboxylic acid Et ester]. The above-mentioned amides were prepared from this intermediate by a reaction with primary amines. A comparative anal. has been carried out of the antitubercular activity of the compounds thus prepared with active structural analogs. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to tuberculostatic hydroxy oxo benzoquinolizinecarboxamide preparation, antibacterial antimycobacterial agent hydroxy oxo benzoquinolizinecarboxamide preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 15, 2005, Zhuravel’, Irina O.; Kovalenko, Sergiy M.; Ivachtchenko, Alexandre V.; Balakin, Konstantin V.; Kazmirchuk, Victor V. published an article.HPLC of Formula: 92-36-4 The title of the article was Synthesis and antimicrobial activity of 5-hydroxymethyl- 8-methyl-2-(N-arylimino)-pyrano[2,3-c]pyridine-3-(N-aryl)-carboxamides. And the article contained the following:

Several 2-imino-5-hydroxymethyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-(N-aryl)carboxamides, e.g., I, were prepared by reaction of pyridoxal hydrochloride with various N-aryl cyanoacetamides. Reaction of these compounds with aromatic amines furnished a wide series of 2-(N-R-phenyl) imino-5-hydroxymethyl-8-methyl-2H-pyrano[2,3-c]pyridine-3-carboxamides. Antibacterial and antifungal activities of the synthesized compounds were studied. Most of the obtained compounds demonstrated significant activity against bacterial or fungal strains (MIC in the range of 12.5-25 μg/mL), displaying comparable or even better efficacy than the standard drugs. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to pyridoxal cyanoacetamide cyclization, iminopyranopyridinecarboxamide preparation arylamine arylation, arylimino pyranopyridinecarboxamide preparation antimicrobial, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.HPLC of Formula: 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zhuravel’, I. O.; Kovalenko, S. M.; Ivashchenko, A. V.; Chernykh, V. P. published an article in 2005, the title of the article was Construction of the combinatorial libraries of 5-hydroxymethyl-2-imino-8-methyl-2H-pyrano[2,3-c]pyridin-3-N-arylcarboxamides.SDS of cas: 92-36-4 And the article contains the following content:

Using the parallel solution-phase synthesis combinatorial libraries of 5-hydroxymethyl-2-imino-8-methyl-2H-pyrano[2,3-c]pyridin-3-N-arylcarboxamides, 5-hydroxymethyl-2-N-arylimino-methyl-2H-pyrano[2,3-c]pyridin-3-N-arylcarboxamides and their acyclic derivatives were obtained. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).SDS of cas: 92-36-4

The Article related to pyranopyridine preparation biol activity prediction, pyridoxal hydrochloride cyanoacetarylamide cyclization, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.SDS of cas: 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On February 4, 2021, Anderson, David Randolph; Jacobsen, Eric Jon; Blinn, James Robert; Hockerman, Susan Landis; Mukherjee, Paramita; Changelian, Paul published a patent.Synthetic Route of 1092942-42-1 The title of the patent was Substituted sulfonamide pyrrolopyridines as JAK inhibitors and their preparation. And the patent contained the following:

The invention relates to sulfonamide pyrrolopyridine compounds of formula I and compositions useful in the treatment of JAK-mediated conditions. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided. Exemplary indications treated by inhibition of JAK kinase activity include, but are not limited to, inflammatory bowel disease, Crohn’s disease, ulcerative colitis, irritable bowel syndrome, and Celiac disease. Compounds of formula I wherein R1 is CN, CO2C1-6 alkyl and (un)substituted 5- to 10-membered heteroaromatic ring; R2 and R3 are independently H, (un)substituted C1-4 alkyl and (un)substituted C0-2 alkyl-C3-6 cycloalkyl; R4 is (un)substituted C1-6 alkyl, (un)substituted C0-4 alkyl-C3-6 cycloalkyl, (un)substituted C2-5 alkyl-COC0-4 alkyl-C3-6 cycloalkyl, etc.; are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for the JAK inhibitory activity (data given). The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Synthetic Route of 1092942-42-1

The Article related to pyrrolopyridine sulfonamide preparation jak inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Synthetic Route of 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 5, 2020, Jacobsen, Eric Jon; Anderson, David Randolph; Blinn, James Robert; Mukherjee, Paramita; Changelian, Paul; Xu, Canxin published a patent.Recommanded Product: 1092942-42-1 The title of the patent was Substituted pyrrolopyridines as JAK inhibitors and their preparation and their preparation. And the patent contained the following:

The invention relates to pyrrolopyridine compounds having the structures of formula I, and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis. Compounds of formula I wherein R1 is CN and (un)substituted heteroaryl; R2 is H, (un)substituted C1-4 alkyl, (un)substituted C3-6 cycloalkyl and (un)substituted C1-2 alkyl-C3-6 cycloalkyl; Q is absent, CH2 and CH2CH2; R3 is H, halo, (un)substituted C1-4 alkyl, (un)substituted C3-6 cycloalkyl, etc.; two R3 groups may be taken together to form a spirocyclic or bicyclic ring system; R4 is COR6, CH2R5, COC1-5 alkyl and COC3-6 cycloalkyl; R6 is C1-5 alkyl, C3-6 cycloalkyl, aryl, aryloxy, etc.; and derivatives thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their JAK inhibitory activity (data given). The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Recommanded Product: 1092942-42-1

The Article related to pyrrolopyridine preparation jak inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Recommanded Product: 1092942-42-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nazarov, V. N.; Marchenko, Ya. S.; Taran, S. V.; Ignatenko, O. N. published an article in 2006, the title of the article was Acylation of amines by diphenic anhydride.Synthetic Route of 92-36-4 And the article contains the following content:

The acylation reaction of various aliphatic, aromatic and heterocyclic amines, hydrazines and hydrazides with diphenic anhydride has been investigated. The corresponding monoamides have been exclusively obtained. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Synthetic Route of 92-36-4

The Article related to amine hydrazine hydrazine primary acylation diphenic anhydride, amide carboxybiphenyl preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Synthetic Route of 92-36-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica