Month: October 2022

On April 25, 2013, Ogamino, Takahisa; Yamazaki, Yukiyoshi; Tanikawa, Shin; Okuda, Ayumu; Fukuda, Tomoaki; Tokuda, Okihisa; Miyake, Yoshiharu; Itoh, Shinsuke; Ishiwata, Hiroyuki published a patent.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of spiroindoline compounds for activating glucokinase. And the patent contained the following:

Title compounds I [ring A = nitrogen-containing heterocyclyl; R1, R2 = independently H, halo, haloalkyl, etc.; R3 = H, (un)substituted alkyl, -COR7, etc.; R7 = H, (un)substituted alkyl, haloalkyl, etc.; R4 = H, halo, cyano, etc.; or salts or solvates thereof], useful for the treatment of diabetes, glucose intolerance, metabolic syndrome, etc., were prepared For example, reaction of 2-amino-5-chlorothiazole·HCl with 4-nitrophenyl chloroformate, treatment with tert-Bu 5-bromospiro[indoline-3,3′-pyrrolidine]-1′-carboxylate, deprotection using CF3CO2H, and acetylation afforded compound II. The invention compounds activated glucokinase activity in vitro assay, e.g., III showed 1192% activation at 1 μmol/L. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to spiroindoline preparation glucokinase activator, diabetes glucose intolerance metabolic syndrome treatment spiroindoline glucokinase activation, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On April 25, 2013, Ogamino, Takahisa; Yamazaki, Yukiyoshi; Tanikawa, Shin; Okuda, Ayumu; Fukuda, Tomoaki; Tokuda, Okihisa; Miyake, Yoshiharu; Itoh, Shinsuke; Ishiwata, Hiroyuki published a patent.Product Details of 64987-16-2 The title of the patent was Preparation of spiroindoline compounds for activating glucokinase. And the patent contained the following:

Title compounds I [ring A = nitrogen-containing heterocyclyl; R1, R2 = independently H, halo, haloalkyl, etc.; R3 = H, (un)substituted alkyl, -COR7, etc.; R7 = H, (un)substituted alkyl, haloalkyl, etc.; R4 = H, halo, cyano, etc.; or salts or solvates thereof], useful for the treatment of diabetes, glucose intolerance, metabolic syndrome, etc., were prepared For example, reaction of 2-amino-5-chlorothiazole·HCl with 4-nitrophenyl chloroformate, treatment with tert-Bu 5-bromospiro[indoline-3,3′-pyrrolidine]-1′-carboxylate, deprotection using CF3CO2H, and acetylation afforded compound II. The invention compounds activated glucokinase activity in vitro assay, e.g., III showed 1192% activation at 1 μmol/L. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Product Details of 64987-16-2

The Article related to spiroindoline preparation glucokinase activator, diabetes glucose intolerance metabolic syndrome treatment spiroindoline glucokinase activation, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Product Details of 64987-16-2

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

On October 15, 2006, Zhou, Yuefen; Sun, Zhongxiang; Froelich, Jamie M.; Hermann, Thomas; Wall, Daniel published an article.HPLC of Formula: 92-36-4 The title of the article was Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-Diamino-piperidinyl triazines. And the article contained the following:

Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking addnl. aromatic moieties at the triazine C-4 position. 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 antibacterial translation inhibition diaminopiperidinyl triazine derivative sar preparation, Air Pollution and Industrial Hygiene: Combustion Engine Exhaust Gas and Catalytic Converters and other aspects.HPLC of Formula: 92-36-4

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

On October 15, 2009, Hahn, Michael; Becker, Eva-Maria; Knorr, Andreas; Schneider, Dirk; Stasch, Johannes-Peter; Schlemmer, Karl-Heinz; Wunder, Frank; Stoll, Friederike; Heitmeier, Stefan; Muenter, Klaus; Griebenow, Nils published a patent.Category: thiazole The title of the patent was Preparation of phthalazinones as soluble guanylate cyclase inhibitors. And the patent contained the following:

Title compounds I [X = L1-M-L2CO2H; L1 = bond, methylene, etc.; M = phenylene, 5 or 6-membered heteroaryl with provisos; L2 = bond, methylene with provisos; A = 5-7 membered heterocycle ring with provisos; R1 = H, alkyl, cycloalkyl; R2 = H, halo, CN, etc.; R3 = alkyl, alkenyl, etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, NaOH/dioxane/H2O mediated saponification of ester II [Y = Me] afforded acid II [Y = H]. In soluble guanylate cyclase inhibition assays, 19 examples of compounds I exhibited MEC values ranging from 1-300 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Category: thiazole

The Article related to phthalazinone preparation soluble guanylate cyclase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: thiazole

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

On October 22, 2009, Hahn, Michael G.; Becker, Eva-Maria; Knorr, Andreas; Schneider, Dirk; Stasch, Johannes-Peter; Schlemmer, Karl-Heinz; Wunder, Frank; Stoll, Frederike; Heitmeier, Stefan; Muenter, Klaus; Griebenow, Nils; Lampe, Thomas; El Sheikh, Sherif; Li, Volkhart Min-Jian published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of phthalazinones as soluble guanylate cyclase inhibitors. And the patent contained the following:

Title compounds I [X = L1-M-L2CO2H; L1 = bond, methylene, etc.; M = phenylene, 5 or 6-membered heteroaryl with provisos; L2 = bond, methylene with provisos; A = 5-7 membered heterocycle ring with provisos; R1 = H, alkyl, cycloalkyl; R2 = H, halo, CN, etc.; R3 = alkyl, alkenyl, etc.] and their pharmaceutically acceptable salts and formulations were prepared For example, NaOH/dioxane/H2O mediated saponification of ester II [Y = Me] afforded acid II [Y = H]. In soluble guanylate cyclase inhibition assays, 48-examples of compounds I exhibited MEC values ranging from 0.1-300 nM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to phthalazinone preparation soluble guanylate cyclase inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.HPLC of Formula: 64987-16-2

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

On April 9, 2020, Qiu, Yunguang; Huang, Lu; Fu, Jie; Han, Chenxia; Fang, Jing; Liao, Ping; Chen, Zhuo; Mo, Yiqing; Sun, Peihua; Liao, Daqing; Yang, Linghui; Wang, Jing; Zhang, Qiansen; Liu, Jin; Liu, Feng; Liu, Tingting; Huang, Wei; Yang, Huaiyu; Jiang, Ruotian published an article.Product Details of 92-36-4 The title of the article was TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation. And the article contained the following:

TWIK-related K+ (TREK) channels are potential analgesic targets. However, selective activators for TREK with both defined action mechanism and analgesic ability for chronic pain have been lacking. Here, we report (1S,3R)-3-((4-(6-methylbenzo[d]thiazol-2-yl)phenyl)carbamoyl)cyclopentane-1-carboxylic acid (C3001a), a selective activator for TREK, against other two-pore domain K+ (K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1, as suggested by computational modeling and exptl. anal. Furthermore, we identify the carboxyl group of C3001a as a structural determinant for binding to TREK-1/2 and the key residue that defines the subtype selectivity of C3001a. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mech. allodynia and inflammation. Together, C3001a represents a lead compound which could advance the rational design of peripherally acting analgesics targeting K2P channels without opioid-like adverse effects. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Product Details of 92-36-4

The Article related to trek channel activator preparation pain neuroinflammation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Product Details of 92-36-4

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 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 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 March 31, 2021, Masih, Anup; Agnihotri, Amol K.; Srivastava, Jitendra K.; Pandey, Nidhi; Bhat, Hans R.; Singh, Udaya P. published an article.Recommanded Product: 4-Phenylthiazol-2-amine The title of the article was Discovery of novel 1,3,5-triazine as adenosine A2A receptor antagonist for benefit in Parkinson’s disease. And the article contained the following:

Parkinson’s disease (PD) is a chronic neuro-degenerative ailment characterized by impairment in various motor and nonmotor functions of the body. In the past few years, adenosine A2A receptor (A2AR) antagonists have attracted much attention due to significant relief in PD. Therefore, in the current study, we intend to disclose the development of novel 1,3,5-triazines as A2AR antagonist. The radioligand binding and selectivity of analogs were tested in HEK293 (human embryonic kidney) and the cells were transfected with pcDNA 3.1(+) containing full-length human A2AR cDNA and pcDNA 3.1(+) containing full-length human A1R cDNA, where they exhibit selective affinity for A2AR. Mol. docking anal. was also conducted to rationalize the probable mode of action, binding affinity, and orientation of the most potent mol. (7c) at the active site of A2AR. It has been shown that compound 7c form numerous nonbonded interactions in the active site of A2AR by interacting with Ala59, Ala63, Ile80, Val84 Glu169, Phe168, Met270, and Ile274. The study revealed 1,3,5-triazines as a novel class of A2AR antagonists. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Recommanded Product: 4-Phenylthiazol-2-amine

The Article related to parkinson disease 123 triazine adenosine a2a receptor antagonist, 1,3,5-triazine, parkinson’s disease, adenosine a2a receptor, antagonist, docking, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Recommanded Product: 4-Phenylthiazol-2-amine

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