Tag: 100-200

On April 10, 2014, Margathe, Jean-Francois; Iturrioz, Xavier; Alvear-Perez, Rodrigo; Marsol, Claire; Riche, Stephanie; Chabane, Hadjila; Tounsi, Nassera; Kuhry, Maxime; Heissler, Denis; Hibert, Marcel; Llorens-Cortes, Catherine; Bonnet, Dominique published an article.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the article was Structure-Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists. And the article contained the following:

Apelin is the endogenous ligand for the previously orphaned G protein-coupled receptor APJ. Apelin and its receptor are widely distributed in the brain, heart, and vasculature, and are emerging as an important regulator of body fluid homeostasis and cardiovascular functions. To further progress in the pharmacol. and the physiol. role of the apelin receptor, the development of small, bioavailable agonists and antagonists of the apelin receptor, is crucial. In this context, E339-3D6 was described as the first nonpeptidic apelin receptor agonist. The authors show here that 1 is actually a mixture of polymethylated species, and they describe an alternative and versatile solid-phase approach that allows access to highly pure 27, the major component of 1. This approach was also applied to prepare a series of derivatives in order to identify the crucial structural determinants required for the ligand to maintain its affinity for the apelin receptor as well as its capacity to promote apelin receptor signaling and internalization. The study of the structure-activity relationships led to the identification of ligands 19, 21, and 38, which display an increased affinity compared to that of 27. The latter and 19 behave as full agonists with regard to cAMP production and apelin receptor internalization, whereas 21 is a biased agonist toward cAMP production Interestingly, the three ligands display a much higher stability in mouse plasma (T1/2 > 10 h) than the endogenous apelin-17 peptide 2 (T1/2 < 4 min). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to apelin receptor ligand fluorescent peptide solid phase preparation sar, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On December 5, 2022, Odey, Joseph O.; Ubana, Emmanuel I.; Eko, Ishegbe J.; Jones, Okama O. published an article.Electric Literature of 2010-06-2 The title of the article was Synthesis, characterization and theoretical studies of the photovoltaic properties of novel bifunctional reactive disperse dyes based on aminothiazole derivatives. And the article contained the following:

This article comprises synthesis and characterization of two polyfunctional diazo reactive-disperse dyes with aminothiazole moiety for application in dye-sensitized solar cells (DSSC). The characterization techniques employed were Gas chromatog.-mass spectrometry (GC-MS), Fourier-transform IR spectroscopy (FT-IR), UV-visible spectroscopy (UV-vis), and NMR to determine the different functional groups, mol. connectivities and mol. weight of the various fragments of the synthesized dyes. Theor. D. Functional Theory (DFT) and Time-Dependent TD-DFT calculations were performed using B3LYP/6-311+g(d,p). It can be observed that the HOMO energy levels of the resp. dyes have lower values than I-/I3- redox couple level (around -4.80 eV) in the four different phases studied, which is crucial for the regeneration of the oxidized dye mol. and efficient charge separation Furthermore, the HOMO-LUMO energy gaps of DYES F and S are within the range 2.38-5.40 eV, where all LUMO-CB of TiO2 energy gap values are sufficient for generating enough driving force for effective electron injection. The promising results of Light-harvesting efficiency (LHE) (values ranging from 0.81 to 0.89 except for DYE S in chloroform phase where it has an unusual value of 0.21) and Open-circuit voltage (VOC) values gotten compared with other organic, and natural sensitizers were due to the better interaction between the carboxyl and carbonyl groups of aryl azo mol. joined to the thiazolyl nucleus and the surface of TiO2 permeable film. DYE S exhibits the lowest band gap (2.374eV), which designates the highest chem. activity of the two dyes. Results from the quantum theory of atoms-in-mols. indicate that DYES F and S exhibit addnl. stability due to their relatively high H-bond interactions as well as certain addnl. intra-at. bonds among the atoms of the investigated compounds The outcome of the Natural bond orbital (NBO) anal. suggests that the strongest charge transfer occurs in DYE S as compared to DYE F. The types and modes of excitations for the first five excited states of the synthesized dyes were observed from the results of the hole-electron excitation anal. First hyperpolarizability values of the dye F and dye S were determined to be 47.24 and 46.90 times the hyperpolarizability value of urea, demonstrating its excellent non-linear optical (NLO) response. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Electric Literature of 2010-06-2

The Article related to bifunctional aminothiazole dye preparation dssc electron transfer nlo, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Electric Literature of 2010-06-2

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

On October 15, 2003, Puetz, Claudia; Sundermann, Bernd; Sundermann, Corinna; Ijzermann, Adriaan Pieter; Tromp, Reynier; Von Frijtag, Drabbe Kuenzel Jacobien published a patent.Electric Literature of 19989-66-3 The title of the patent was Preparation of analogs of nitrobenzylthioinosine for the treatment of pain, epilepsy, and other CNS-related disorders. And the patent contained the following:

This invention relates to new nucleoside analogs I, wherein or derivatives of nitrobenzylthioinosine, use of these new analogs of nitrobenzylthioinosine for the treatment of pain and various other diseases as well as pharmaceuticals comprising at least on new analog of nitrobenzylthioinosine. The derivatives of nitrobenzylthioinosine according to the invention are surprisingly effective in the treatment of pain and in other indications. Therefore a further embodiment of the invention comprises the use of a derivatives of nitrobenzylthioinosine according to the invention for the treatment of pain, especially acute, chronic and/or neuropathic pain. Treatment using derivatives of nitrobenzylthioinosine according to the invention especially for the treatment of pain, especially acute, chronic and/or neuropathic pain; the treatment of epilepsy and other CNS-related disorders as well as for neuro-protection or cardio-protection. A further embodiment of the invention comprises the use of a derivatives of nitrobenzylthioinosine according to the invention for the treatment of epilepsy and other CNS-related disorders as well as for neuroprotection or cardio-protection. Thus, 2-[6-(benzo[c]iso-thiazol-5-ylmethylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol was prepared and tested for the treatment of pain, epilepsy, transport protein on human erythrocyte membranes (Ki > 1.5 nM), and other CNS-related disorders. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Electric Literature of 19989-66-3

The Article related to human nitrobenzylthioinosine nucleoside preparation treatment pain epilepsy cns, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.Electric Literature of 19989-66-3

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

On February 26, 1986, Onoue, Hiroshi; Takahashi, Hiromi published a patent.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Thiazolylpentenedioic acids. And the patent contained the following:

Esters I (R1 = NH2, protected amino; R2 = standard alc. residue; R3 = H, cyano, esterified CO2H; R4 = H, cyano, esterified CO2H) were prepared Thiazoleacetate ester II was treated with MeOCH:C(CO2Me)2; the product underwent elimination reaction to yield I (R1 = NHCO2CH2Ph, R2 = Me, R3 = R4 = CO2H), and the latter was subjected to hydrolysis-decarboxylation to give I (R1 = NHCO2CH2Ph, R2 = R3 = H, R4 = CO2H). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazolylpentenedioic acid, glutaconic acid thiazolyl, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On January 31, 2014, Praveen, Aletti S.; Yathirajan, Hemmige S.; Narayana, Badiadka; Sarojini, Balladka K. published an article.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the article was Synthesis, characterization and antimicrobial studies of a few novel thiazole derivatives. And the article contained the following:

A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted)acetamides and Me 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetates were synthesized. All compounds were screened for their in vitro antibacterial activity against S. aureus, E. coli, P. aeruginosa, and K. pneumonia by disk diffusion and for antifungal activity against P. marneffei, T. mentagrophytes, A. flavus, and A. fumigatus by serial plate dilution Some of the compounds exhibited growth inhibition against all the tested bacterial strains, with MIC of 12.5-6.25 μg/mL. Among the compounds tested for antifungal activity, several of them showed a wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds showed selective sensitivity against some of the bacterial strains, whereas they were unable to sustain the growth of other strains. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazole amide preparation antibacterial antifungal, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

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

On May 21, 2008, Zhao, Hongfu; Liu, Gang; Zheng, Gengxiu; Sun, Bin; Guo, Fangshui; Wang, Guangzheng published a patent.Electric Literature of 64987-16-2 The title of the patent was Method for preparing 2-(2-butoxycarbonylaminothiazol-4-yl)-2-pentenoate. And the patent contained the following:

The title method comprises: (1) carrying out reaction of alkyl 2-(2-aminothiazol-4-yl)acetate 1.0 mol and di-tert-Bu dicarbonate 1.0-1.5 mol in the presence of 4-N,N-dimethylaminopyridine as catalyst at 0-80°C to obtain alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate, and (2) cooling alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate to -60-0°C, adding alkali, adding propionaldehyde, heating to room temperature, and carrying out reaction to obtain the final product. The method has the advantages of shortening reaction time, reducing usage of di-tert-Bu dicarbonate, and enhancing yield. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to aminothiazolylpentenoate butoxycarbonyl preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Electric Literature of 64987-16-2

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

On January 24, 1985, there was a patent about blood platelet.Application of 64987-16-2 The title of the patent was Alkyl 2-substituted amino-4-thiazolylacetates. And the patent contained the following:

The title esters I [R, R1 = 5-(1-imidazolyl)pentyl, Me; cyclohexylamino, Me; EtNH, Et] were prepared by reaction of II with the corresponding carboxylic acids or isocyanates. I had platelet aggregation inhibitory activity at 5-25 mg/kg-day. Thus, a mixture of 6-(1-imidazolyl)hexanoic acid 0.9, 1-hydroxybenzotriazole 0.7, and DCC 1 g in DMF was stirred 30 min at 40-50°, 0.9 g II (R1 = Me) in DMF added, and the whole stirred 1 h at 40-50% to give I [R = 5-(1-imidazolyl)pentyl, R1 = Me]. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application of 64987-16-2

The Article related to aminothiazolylacetate blood platelet aggregation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application of 64987-16-2

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

On January 9, 2020, Glick, Gary; Roush, William; Venkatraman, Shankar; Shen, Dong-Ming; Ghosh, Shomir; Seidel, Hans Martin; Franchi, Luigi; Winkler, David Guenther; Opipari, Anthony William, Jr.; Katz, Jason published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Aryl and heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl, SONR11R12 and CR11R12NR11R12; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; R11 and R12 are independently H and (un)substituted C1-6 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by chlorination of 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetic acid; the resulting 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetyl chloride underwent amidation with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide to give compound II. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.04μM to < 0.2μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On January 9, 2020, Franch, Luigi; Ghosh, Shomir; Glick, Gary; Katz, Jason; Opipari, Anthony William, Jr.; Roush, William R.; Seidel, Hans Martin; Shen, Dong-Ming; Venkatraman, Shankar; Winkler, David Guenther published a patent.Related Products of 64987-16-2 The title of the patent was Heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl and SONH2 and derivatives; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2,2,2-trichloroethyl N-[2-azatricyclo[7.3.0.0[3,7]]dodeca-1,3(7),8-trien-8-yl]carbamate with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.2μM to < 1μM. 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 heteroaryl preparation nlrp3 modulator, 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 28, 2022, Kalhor, Mehdi; Zarnegar, Zohre published an article.Quality Control of 4-Phenylthiazol-2-amine The title of the article was 1-Methylimidazolium ionic liquid supported on Ni@zeolite-Y: fabrication and performance as a novel multi-functional nanocatalyst for one-pot synthesis of 2-aminothiazoles and 2-aryl benzimidazoles. And the article contained the following:

In the present study, 1-methyl-3-(3-trimethoxysilylpropyl)-1H-imidazol-3-ium chloride-supported Ni@zeolite-Y-based nanoporous materials (Ni@zeolite-Im-IL) were synthesized and their structures were confirmed using different characterization techniques such as FT-IR, FE-SEM, EDX, XRD, BET and TGA-DTG analyses. In order to synthesize this multi-functional nano-system, zeolite-NaY was modified first, with exchanged Ni2+ ions and 3-chloropropyltriethoxysilane (CPTES) as a coupling reagent and then functionalized to imidazolium chloride ionic liquid by N-methylimidazole. New multi-functional nano-material of Ni@zeolite-Im-IL demonstrated high activity in the catalytic synthesis of 2-aminothiazoles 3a-l by one-pot reaction of methylcarbonyls, thiourea and iodine at 80°C in DMSO with good to excellent yields (85-98%). Also, the catalytic synthesis of 2-aryl benzimidazoles, 6a-m was performed by the condensational reaction of o-arylendiamine and aromatic aldehydes in EtOH at room temperature with excellent yields (90-98%). Advantages of this efficient synthetic strategy include higher purity and shorter reaction time, excellent yield, easy isolation of products, the good stability, activity and feasible reusability of the metallic ionic liquid nanocatalyst. These benefits have made this method more compatible with the principles of green chem. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Quality Control of 4-Phenylthiazol-2-amine

The Article related to methylimidazolium ionic liquid supported nickel zeolitey nanocatalyst synthesis fabrication, Catalysis, Reaction Kinetics, and Inorganic Reaction Mechanisms: Catalysts and other aspects.Quality Control of 4-Phenylthiazol-2-amine

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