Month: November 2022

On January 8, 2009, Wang, Xueqing; Sarris, Katerina; Kage, Karen; Zhang, Di; Brown, Scott P.; Kolasa, Teodozyi; Surowy, Carol; El Kouhen, Odile F.; Muchmore, Steven W.; Brioni, Jorge D.; Stewart, Andrew O. published an article.Formula: C14H12N2S The title of the article was Synthesis and Evaluation of Benzothiazole-Based Analogues as Novel, Potent, and Selective Fatty Acid Amide Hydrolase Inhibitors. And the article contained the following:

High-throughput screening (HTS) identified benzothiazole analog (I) as a potent fatty acid amide hydrolase (FAAH) inhibitor. Structure-activity relationship (SAR) studies indicated that the sulfonyl group, the piperidine ring and benzothiazole were the key components to their activity, with II being the most potent analog in this series. Time-dependent preincubation study of compound I was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation of I in rat tissues revealed that it had exceptional selectivity and no off-target activity with respect to other serine hydrolases. Mol. shape overlay of I with a known FAAH inhibitor indicated that these compounds might act as transition-state analogs, forming putative hydrogen bonds with catalytic residues and mimicking the charge distribution of the tetrahedral transition state. The modeling study also indicated that hydrophobic interactions of the benzothiazole ring with the enzyme contributed to its extraordinary potency. These compounds may provide useful tools for the study of FAAH and the endocannabinoid system. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Formula: C14H12N2S

The Article related to carboxylic acid amine acylation, azacycle preparation fatty acid amide hydrolase inhibition, structure activity antinociception human, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C14H12N2S

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

On April 30, 2007, Karade, Hitendra; Sathe, Manisha; Kaushik, M. P. published an article.Name: 2-Amino-4-(4-iodophenyl)thiazole The title of the article was An efficient method for the synthesis of 2-aminothiazoles using silica chloride as a heterogeneous catalyst. And the article contained the following:

Preparation of 2-aminothiazoles under mild reaction conditions with quant. yields using silica chloride as an effective heterogeneous catalyst is reported. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Name: 2-Amino-4-(4-iodophenyl)thiazole

The Article related to aminothiazole preparation ketone thiourea silica chloride catalyst, thiazole amino preparation ketone thiourea silica chloride catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: 2-Amino-4-(4-iodophenyl)thiazole

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

On January 20, 2018, Liessi, Nara; Cichero, Elena; Pesce, Emanuela; Arkel, Maria; Salis, Annalisa; Tomati, Valeria; Paccagnella, Matteo; Damonte, Gianluca; Tasso, Bruno; Galietta, Luis J. V.; Pedemonte, Nicoletta; Fossa, Paola; Millo, Enrico published an article.Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole The title of the article was Synthesis and biological evaluation of novel thiazole- VX-809 hybrid derivatives as F508del correctors by QSAR-based filtering tools. And the article contained the following:

The most common CF mutation, F508del, impairs the processing and gating of CFTR protein. This deletion results in the improper folding of the protein and its degradation before it reaches the plasma membrane of epithelial cells. Present correctors, like VX809 only induce a partial rescue of the mutant protein. Our previous studies reported a class of compounds, called aminoarylthiazoles (AATs), featuring an interesting activity as correctors. Some of them show additive effect with VX-809 (I) indicating a different mechanism of action. In an attempt to construct more interesting mols., it was thought to generate chem. hybrid compounds, blending a portion of VX-809 merged to the thiazole scaffold. This approach was guided by the development of QSAR analyses, which were performed based on the F508del correctors so far disclosed in the literature. This strategy was aimed at exploring the key requirements turning in the corrector ability of the collected derivatives and allowed us to derive a predictive model guiding for the synthesis of novel hybrids as promising correctors. The new mols. were tested in functional and biochem. assays on bronchial CFBE41o-cells expressing F508del-CFTR showing a promising corrector activity. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole

The Article related to thiazole vx809 hybrid cystic fibrosis deletion mutation corrector qsar, aminoarylthiazole, cftr, corrector, cystic fibrosis, qsar, vx809, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application In Synthesis of 2-Amino-4-(4-iodophenyl)thiazole

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

On January 27, 1998, Iwasaki, Fumiaki; Miharu, Michiko published a patent.Related Products of 64987-16-2 The title of the patent was Preparation of 2-aminothiazoleacetic acids as intermediates for cephem antibiotics. And the patent contained the following:

Title compounds I (R1 = CO2H-protecting group; R2 = alkyl) are prepared by reaction of thiazoles II (R1 = same as I) with dialkyl carbonates in the presence of aminopyridines. II (R1 = Et) was treated with (t-BuO)2CO in PhMe in the presence of 4-N,N-dimethylaminopyridine at 50° for 7 h to give 77.0% I (R1 = Et, R2 = t-Bu). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Related Products of 64987-16-2

The Article related to aminothiazoleacetic acid preparation cephem antibiotic intermediate, aminothiazole alkoxycarbonylation alkyl carbonate aminopyridine catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 64987-16-2

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

On February 13, 2003, Wells, Geoffrey; Berry, Jane M.; Bradshaw, Tracey D.; Burger, Angelika M.; Seaton, Angela; Wang, Bo; Westwell, Andrew D.; Stevens, Malcolm F. G. published an article.Application of 92-36-4 The title of the article was 4-Substituted 4-Hydroxycyclohexa-2,5-dien-1-ones with Selective Activities against Colon and Renal Cancer Cell Lines. And the article contained the following:

The synthesis and antitumor evaluation of a series of new heteroaromatic- and aromatic-substituted hydroxycyclohexadienones (quinols), and their imine counterparts, are described. The quinols were synthesized via the addition of a lithiated aromatic moiety to a quinone ketal followed by deprotection. When the aromatic portion of the mol. is a fused heterobicyclic structure (e.g., benzothiazole derivative I), potent in vitro antitumor activity was observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM) human colon as well in as MCF-7 and MDA 468 human breast cancer cell lines. When examined on the NCI Developmental Therapeutics Screening Program in vitro screen (60 human cancer cell lines), active compounds in this series consistently displayed a highly unusual pattern of selectivity; cytotoxicity (LC50) was concentrated in certain colon and renal cell lines only. I also showed in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice and is the focus of further study. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Application of 92-36-4

The Article related to hydroxycyclohexadienone aryl heteroaryl preparation antitumor colon rectal cancer, quinol aryl heteroaryl preparation antitumor colon renal cancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application of 92-36-4

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

On February 28, 2022, Cai, Mingzhong; Ye, Qian; Huang, Wencheng; Hao, Wenyan published an article.SDS of cas: 92-36-4 The title of the article was Recyclable copper-catalyzed cyclization of o-haloanilides and metal sulfides: An efficient and practical access to substituted benzothiazoles. And the article contained the following:

An efficient heterogeneous copper-catalyzed cyclization of o-haloanilides and metal sulfides has been achieved via the C-S coupling in DMF at 80 or 140° in the existence of an MCM-41-bound NHC-Cu(I) catalyst and then intramol. condensation, delivering a wide range of substituted benzothiazoles in mostly good to high yields. This new MCM-41-NHC-CuI complex can facilely be obtained by a two-step procedure starting from easily accessible and inexpensive reagents and reused more than seven times without any significant loss of its catalytic efficiency. The present protocol has been successfully applied to the gram-scale synthesis of two antitumor agents 5F203 and PMX 610. 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 benzothiazole preparation green chem, haloanilide metal sulfide cross coupling intramol condensation, mesoporous silica mcm 41 anchored nhc copper complex, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.SDS of cas: 92-36-4

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

On September 2, 2013, Bort, Guillaume; Sylla-Iyarreta Veitia, Maite; Ferroud, Clotilde published an article.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Straightforward synthesis of PET tracer precursors used for the early diagnosis of Alzheimers disease through Suzuki-Miyaura cross-coupling reactions. And the article contained the following:

In positron emission tomog. [11C]PIB, Pittsburgh Compound-B, is currently the most widely used radiopharmaceutical for the early diagnosis of Alzheimer’s disease. Synthetic routes for the preparation of the precursor of [11C]PIB are reported in the literature. These strategies require multiple steps and the use of protecting groups. This paper describes a simple 1-step synthesis of the precursor of [11C]PIB through a Suzuki-Miyaura coupling reaction using thermal conditions or microwave activation. These methods were successfully applied to the synthesis of various 2-arylbenzothiazole and 2-pyridinylbenzothiazole compounds including [18F] precursor derivatives of PIB containing a nitro function. 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 pittsburgh compound b pet tracer precursor alzheimer diagnosis preparation, benzothiazole pittsburgh b pet tracer precursor alzheimer diagnosis preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On July 5, 1988, Kinast, Guenther published a patent.Related Products of 64987-16-2 The title of the patent was Preparation of aminothiazole derivatives as cephalosporin antibiotic intermediates. And the patent contained the following:

The title compounds [I; R1 = (substituted) alkyl, cycloalkyl, (hetero)aryl; R2 = CO2R3; R3, R4 = alkyl, alkenyl, cycloalkyl, cycloalkenyl, (hetero)aryl], useful as intermediates for cephalosporin antibiotics, were prepared from iminothiazolineacetates II. A mixture of Et 2-[(tert-butoxycarbonyl)imino]-3-(tert-butoxycarbonyl)-4-thiazoline-4-acetate, BuLi, and AcH in THF was stirred 2 h at -50 to -60° to give Et 2-[2-[(tert-butoxycarbonyl)amino]thiazol-4-yl]-3-[(tert-butoxycarbonyl)oxybutyrate. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Related Products of 64987-16-2

The Article related to thiazole amino preparation antibiotic intermediate, cephalosporin intermediate aminothiazole preparation, antibiotic intermediate aminothiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 64987-16-2

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

On April 3, 2012, Jeppesen, Lone; Kristiansen, Marit published a patent.Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Heteroaromatic glucokinase activators. And the patent contained the following:

The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, of Formula (I) wherein the substitution at the 3-position is an optionally substituted Ph ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment of type II diabetes. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to heteroaromatic propionamide preparation glucokinase activator diabetes treatment, metabolic disorder treatment heteroaromatic propionamide glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On June 8, 2006, Jeppesen, Lone; Kristiansen, Marit published a patent.Formula: C7H10N2O2S2 The title of the patent was Preparation of N-heteroaromatic propionamides as glucokinase activators for treating diabetes and other diseases. And the patent contained the following:

The present invention describes 2,3-di-substituted N-heteroaromatic propionamides of Formula I ( wherein the * indicates an asym. atom; R1,R2 = H, halo, NH2, NHOH, C1-6 alkyl, perfluoro-C1-6 alkyl, etc.; R3 = C3-7 cycloalkyl and C2-4 alkyl; ring A = a monosubstituted or a disubstituted 5-6 membered heteroaromatic ring consisting of, in addition to the C=N shown, carbon atoms and 0-2 heteroatoms selected from S(O)p, 0, and N; p= 0-2) pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators for the treatment II diabetes and other disorders(no data given). The preparation of I is exemplified. For example, II was prepared in 2 steps by reacting intermediate 2-amino-5-(4-methylpiperazin-1-yl)thiazole (preparation given) with 3-cyclopentyl-2-(4-methanesulfonylphenyl)propionic acid. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Formula: C7H10N2O2S2

The Article related to heteroaromatic propionamide preparation glucokinase activator diabetes treatment, metabolic disorder treatment heteroaromatic propionamide glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C7H10N2O2S2

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