Tag: 100-200

On October 3, 2013, Saito, Noriko; Egi, Jun; Nagai, Hiroshi; Ueno, Megumi; Shintani, Yusuke; Inaba, Yusuke; Adachi, Michiaki; Hirai, Yuichi; Kawazu, Takeshi; Yasutake, Koichi; Takahashi, Daiki published a patent.Recommanded Product: 19989-66-3 The title of the patent was Preparation of triazinone compounds as T-type calcium channel inhibitors. And the patent contained the following:

The title compounds [I; R1 = H, halo, each (un)substituted C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, mono- or di(C1-6 alkyl)amino, or C3-11 cycloalkyl; L1, L2 = a single bond, (un)substituted NH or C1-6 alkylene, O, S(O), SO2; B = each (un)substituted C3-11 cycloalkylene, C3-11 cycloalkenylene, 3-11 membered heterocyclylene, C6-14 arylene, 5-10 membered heteroarylene, C1-6 alkylene, C2-6 alkenylene, or C2-6 alkynylene; A = each (un)substituted C1-6 alkyl, C2-6 alkenyl, C3-11 cycloalkyl, C3-11 cycloalkenyl, 3-11 membered heterocyclyl, C6-14 aryl, or 5-10 membered heteroaryl; L3 = (un)substituted C1-6 alkylene optionally having one of the methylene groups replaced by C(O) or C(S); D = each (un)substituted C3-11 cycloalkyl, C3-11 cycloalkenyl, 3-11 membered heterocyclyl, C6-14 aryl, or 5-10 membered heteroaryl], tautomers or pharmaceutically acceptable salts of the compounds, or solvates of the compounds, the tautomers or the pharmaceutically acceptable salts are prepared These compounds have an inhibitory activity on a T-type voltage-dependent calcium channel and are useful for the prevention, treatment, and/or improvement of diseases for which the T-type calcium channel-inhibitory activity are effective, in particular pain, more specifically neuropathic pain. Thus, amination of 1,3,5-trichlorotriazine with 1-(4-fluorophenyl)piperazine dihydrochloride in the presence of Na2CO3 in THF at room temperature for 3 days quant. gave 2,4-dichloro-6-[4-(4-fluorophenyl)piperazin-1-yl]-1,3,5-triazine which underwent hydrolysis with aqueous NaOH solution at room temperature for 2 days and 2 h to give 79% 6-chloro-4-[4-(4-fluorophenyl)piperazin-1-yl]-1,3,5-triazin-2(1H)-one (II; X = Cl). Hydrogenation of II (X = Cl) in the presence of Pd(OH)2/activated charcoal in aqueous acetic acid solution under hydrogen atm. at room temperature for 3 days gave 99% 4-[4-(4-fluorophenyl)piperazin-1-yl]-1,3,5-triazin-2(1H)-one II (X = H) which underwent benzylation by 4-chlorobenzyl bromide in the presence of K2CO3 in N,N-dimethylformamide at 70° for 5 h to give 53% 1-(4-Chlorobenzyl)-4-[4-(4-fluorophenyl)piperazin-1-yl]-1,3,5-triazin-2(1H)-one (III). III and (R)-4-[4-(4-fluorophenyl)-5-hydroxy-5,6-dihydropyridin-1(2H)-yl]-1-[[5-(trifluoromethyl)thiophen-2-yl]methyl]-1,3,5-triazin-2(1H)-one (IV) showed IC50 of 0.17 and 0.00046 μM, resp., for inhibiting the cellular calcium influx in KSE293 cells expressing human type T calcium channel (Cav3.2). The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Recommanded Product: 19989-66-3

The Article related to triazinone preparation t type calcium channel inhibitor, benzylphenylpiperazinyltriazinone phenylpyridinylthiophenylmethyltriazinone preparation t type calcium channel inhibitor, pain neuropathic pain treatment prevention improvement triazinone preparation and other aspects.Recommanded Product: 19989-66-3

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

On March 1, 2022, Zhan, Huan; Cui, Heping; Yu, Junhe; Hayat, Khizar; Wu, Xian; Zhang, Xiaoming; Ho, Chi-Tang published an article.Formula: C5H5NOS The title of the article was Characteristic flavor formation of thermally processed N-(1-deoxy-α-D-ribulos-1-yl)-glycine: Decisive role of additional amino acids and promotional effect of glyoxal. And the article contained the following:

The role of amino acids and α-dicarbonyls in the flavor formation of Amadori rearrangement product (ARP) during thermal processing was investigated. Comparisons of the volatile compounds and their concentrations when N-(1-deoxy-α-D-ribulos-1-yl)-glycine reacted with different amino acids or glyoxal (GO) at 100°C were executed. Addnl. amino acids, such as glycine (Gly), in ARP models contributed to the diversity of furanoids by the chain elongation of the derived formaldehyde. Whereas the monoanion of addnl. glutamic acid acted as nucleophile, favored 2-ethyl-3,5-dimethylpyrazine and 2,5-dimethylpyrazine formation; the nonionized amino group of addnl. lysine were involved in α-dicarbonyls formation, causing pyrazine and methylpyrazine accumulation in the ARP model. Moreover, the high dosage and pH stabilization of addnl. GO probably promoted the ARP degradation and deoxyosones retro-aldol cleavage, resulting in methylpyrazine rather than furanoids formation. The present work provided the guidance for the controlled flavor formation of ARP in industrial application. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Formula: C5H5NOS

The Article related to amadori rearrangement product thermal processing flavor formation, amadori rearrangement product, flavor, furanoids, pyrazines, strecker degradation, d-ribose, l-cysteine, l-glutamic acid, l-glycine, l-histidine, l-lysine, l-methionine, α-dicarbonyls and other aspects.Formula: C5H5NOS

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

Kasetti, Ashok Babu; Singhvi, Indrajeet; Nagasuri, Ravindra; Bhandare, Richie R.; Shaik, Afzal B. published an article in 2021, the title of the article was Thiazole-chalcone hybrids as prospective antitubercular and antiproliferative agents: design, synthesis, biological, molecular docking studies and in silico ADME evaluation.Computed Properties of 24295-03-2 And the article contains the following content:

In this paper design, a novel series of thiazole-chalcone hybrids I (R = 2-ClC6H4, 2-pyridyl, 2-thiazolyl, etc.) was synthesized and characterized and further evaluated for their antitubercular and antiproliferative activities by employing standard protocols. Among the twenty compounds, chalcones I (R = 2,4-(F)2C6H3, 2,4-(Cl)2C6H3), containing 2,4-difluorophenyl and 2,4-dichlorophenyl groups, showed potential antitubercular activity higher than the standard pyrazinamide (MIC = 25.34μM) with MICs of 2.43 and 4.41μM, resp. Chalcone I (R = 2-thiazolyl) containing heteroaryl 2-thiazolyl moiety exhibited promising antiproliferative activity against the prostate cancer cell line (DU-145), higher than the standard methotrexate (IC50 = 11 ± 1μM) with an IC50 value of 6.86 ± 1μM. Furthermore, cytotoxicity studies of these compounds against normal human liver cell lines (L02) revealed that the target mols. were comparatively less selective against L02. Addnl. computational studies using AutoDock predicted the key binding interactions responsible for the activity and the SwissADME tool computed the in silico drug likeliness properties. The lead compounds generated through this study, create a way for the optimization and development of novel drugs against tuberculosis infections and prostate cancer. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Computed Properties of 24295-03-2

The Article related to thiazole chalcone preparation diastereoselective antitubercular antitumor cytotoxic activity, pharmacodynamic study sar mol docking, autodock, swissadme, antiproliferative activity, antitubercular activity, chalcone, cytotoxic activity, thiazole and other aspects.Computed Properties of 24295-03-2

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

On April 15, 2020, Malecka, Magdalena; Machura, Barbara; Switlicka, Anna; Kotowicz, Sonia; Szafraniec-Gorol, Grazyna; Siwy, Mariola; Szalkowski, Marcin; Mackowski, Sebastian; Schab-Balcerzak, Ewa published an article.Recommanded Product: 2-Acetylthiazole The title of the article was Towards better understanding of photophysical properties of rhenium(I) tricarbonyl complexes with terpy-like ligands. And the article contained the following:

Series of Re(I) carbonyls complexes were designed and synthesized to explore the impact of the triimine skeleton and number of methoxy groups attached to aryl substituents on their optoelectronic and thermal properties. The chem. structures of the prepared complexes were confirmed by 1H and 13C NMR spectroscopy, HR-MS, elemental anal., and x-ray measurements. DSC measurements showed that they melted in the range of 198-325°. Some of them form stable mol. glasses with high glass transition temperatures (158-173°). Exptl. obtained optical properties were supported by DFT calculations The UV-Vis spectra display a series of overlapping absorption bands in the range 200-350 nm, and much weaker broad band in the visible spectral region, due to intraligand and charge transfer transitions, resp. All synthesized complexes were emissive in solution and in solid state as powder. Moreover, when applied in diodes, some of them exhibited ability for emission of light under external voltage with maximum of electroluminescence band located at 591-630 nm. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Recommanded Product: 2-Acetylthiazole

The Article related to crystal structure mol rhenium tricarbonyl terpyridine complex optimized dft, rhenium tricarbonyl terpyridine complex preparation photophys thermal optical electrochem, electroluminescence, photoluminescence, re(i) carbonyl, terpy-like ligands and other aspects.Recommanded Product: 2-Acetylthiazole

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

Kadam, Shuddhodan N.; Ambhore, Ajay N.; Kamble, Rahul D.; Wakhradkar, Mahesh G.; Gavhane, Priya D.; Gaikwad, Milind V.; Gunturu, Krishna Chaitanya; Dawane, Bhaskar S. published an article in 2021, the title of the article was Metal-free efficient thiolation of C(sp2) functionalization via in situ-generated NHTS for the synthesis of novel sulfenylated 2-aminothiazole and imidazothiazole.Synthetic Route of 2010-06-2 And the article contains the following content:

A direct metal-free approach for the synthesis of novel sulfenylated 2-aminothiazole and imidazothiazole derivatives at room temperature was reported via an in situ-generated electrophilic thiolating agent. The present protocol provided mild and selective access for the insertion of C-S bond functionalization with good yield. The mechanistic path was justified via d. functional theory (DFT) calculations, which explored the role of the solvent in the reaction mechanism. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Synthetic Route of 2010-06-2

The Article related to phenyl aminothiazole heterocyclic thiol chemoselective thiolation dft, thio phenyl thiazolamine preparation, heterocyclic thiol phenyl imidazolthiazole chemoselective thiolation dft, hydroxyethyl thio phenyl methylimidazothiazole preparation and other aspects.Synthetic Route of 2010-06-2

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

Spunde, Karina; Vigante, Brigita; Dubova, Unda Nelda; Sipola, Anda; Timofejeva, Irena; Zajakina, Anna; Jansons, Juris; Plotniece, Aiva; Pajuste, Karlis; Sobolev, Arkadij; Muhamadejev, Ruslan; Jaudzems, Kristaps; Duburs, Gunars; Kozlovska, Tatjana published an article in 2022, the title of the article was Design and Synthesis of Hepatitis B Virus (HBV) Capsid Assembly Modulators and Evaluation of Their Activity in Mammalian Cell Model.COA of Formula: C5H5NOS And the article contains the following content:

Capsid assembly modulators (CAMs) have emerged as a promising class of antiviral agents. Herein, the effects of twenty-one newly designed and synthesized CAMs including (heteroaryl)dihydropyrimidines (HAPs), their analogs and standard compounds on hepatitis B virus (HBV) capsid assembly have been studied. Cytoplasmic expression of the HBV core (HBc) gene driven by the exogenously delivered recombinant alphavirus RNA replicon was used for high level production of the full-length HBc protein in mammalian cells. HBV capsid assembly was assessed by native agarose gel immunoblot anal., electron microscopy and inhibition of virion secretion in HepG2.2.15 HBV producing cell line. Induced fit docking simulation was applied for modeling the structural relationships of the synthesized compounds and HBc. The most efficient were the HAP class compounds, dihydropyrimidine-5-carboxylic acid n-alkoxyalkyl esters, which induced the formation of incorrectly assembled capsid products and their accumulation within the cells. HBc product accumulation in the cells was not detected with the reference HAP compound Bay 41-4109, suggesting different modes of action. A significant antiviral effect and substantially reduced toxicity were revealed for two of the synthesized compounds Two new HAP compounds revealed a significant antiviral effect and a favorable toxicity profile that allows these compounds to be considered promising leads and drug candidates for the treatment of HBV infection. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).COA of Formula: C5H5NOS

The Article related to dihydropyrimidine heteroaryl preparation hepatitis virus capsid assembly modulator antitumor, bay 41-4109, antivirals, capsid assembly, capsid assembly modulator, full-length hbv core, hepatitis b virus, heteroaryldihydropyrimidines and other aspects.COA of Formula: C5H5NOS

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

On January 1, 2017, Tomasic, Tihomir; Mirt, Matic; Barancokova, Michaela; Ilas, Janez; Zidar, Nace; Tammela, Paivi; Kikelj, Danijel published an article.SDS of cas: 64987-16-2 The title of the article was Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors. And the article contained the following:

Two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety was designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC50 values between 0.891 and 10.4 μM). Their “ring-opened” analogs, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC50 values between 15.9 and 169 μM. Mol. docking experiments were conducted to study the binding modes of inhibitors. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).SDS of cas: 64987-16-2

The Article related to amido tetrahydrobenzothiazolyl pyrrolylcarboxamide preparation sar dna gyrase mol docking, phenyl acetamidothiazolyl pyrrolylcarboxamide preparation sar dna gyrase mol docking, antibacterial, dna gyrase, docking, inhibitor, thiazole and other aspects.SDS of cas: 64987-16-2

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

On July 1, 2019, Olawode, Emmanuel O.; Tandlich, Roman; Prinsloo, Earl; Isaacs, Michelle; Hoppe, Heinrich; Seldon, Ronnett; Warner, Digby F.; Steenkamp, Vanessa; Kaye, Perry T. published an article.Computed Properties of 2010-06-2 The title of the article was Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones. And the article contained the following:

A series of novel, substituted 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones have been prepared and shown to exhibit promising concentration-dependent activity against human SH-SY5Y cells, Plasmodium falciparum, Mycobacterium tuberculosis and P. aeruginosa. Substituent effects on observed bioactivity have been explored; the para-fluorophenyl derivative I exhibited activity across the range of the bioassays employed, indicating the potential of the 2-chloro-3-[(4-arylthiazol-2-yl)amino]-1,4-naphthoquinone scaffold in the development of novel, broad spectrum therapeutics. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Computed Properties of 2010-06-2

The Article related to chlorothiazolylaminonaphthoquinone preparation antimalaria antibacterial antituberculosis anticancer, 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones, anti-bacterial, anti-malarial, anti-tuberculosis, cytotoxicity, hela cells and other aspects.Computed Properties of 2010-06-2

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

On October 20, 2021, Marcinkowska, Monika; Frank, Stephanie; Steinhaus, Martin; Jelen, Henryk H. published an article.HPLC of Formula: 24295-03-2 The title of the article was Key Odorants of Raw and Cooked Green Kohlrabi (Brassica oleracea var. gongylodes L.). And the article contained the following:

Volatile compounds of raw and cooked green kohlrabi were investigated using a sensomics approach. A total of 55 odor-active compounds were detected and identified in raw and cooked green kohlrabi using GC-O. Twenty-eight odor-active compounds with high flavor dilution (FD) factors ranging from 64 to 1024 were quantitated, and odor activity values (OAVs) were determined Eight compounds showed high OAVs in raw and cooked kohlrabi: five sulfur compounds (di-Me trisulfide, Me 2-methyl-3-furyl disulfide, and three isothiocyanates (1-isothiocyanato-3-(methylsulfanyl)propane, benzyl isothiocyanate, and 1-isothiocyanato-4-(methylsulfanyl)butane)), two lipid oxidation products (1-octen-3-one and trans-4,5-epoxy-(2E)-dec-2-enal), and 2-isopropyl-3-methoxypyrazine. Among these, the sulfur compounds contributed most to the overall smell of the raw and cooked vegetables. The quantitation anal. indicates that the eight odorants are the backbone compounds for raw and cooked kohlrabi. The OAVs for the backbone compounds and also for minor odorants are clearly higher in raw kohlrabi than in the cooked one. Differences can be explained by the influence of the cooking process. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).HPLC of Formula: 24295-03-2

The Article related to odorant raw cooked brassica kohlrabi, gc-o, aroma extract dilution analysis (aeda), isothiocyanate (itc), kohlrabi (brassica oleracea var. gongylodes l.), nitrile, odor activity value (oav), stable isotope dilution assay (sida) and other aspects.HPLC of Formula: 24295-03-2

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

Cernosek, Terezie; Eckert, Kevin E.; Carter, David O.; Perrault, Katelynn A. published an article in 2020, the title of the article was Volatile Organic Compound Profiling from Postmortem Microbes using Gas Chromatography-Mass Spectrometry.Recommanded Product: 24295-03-2 And the article contains the following content:

Volatile organic compounds (VOCs) are byproducts of cadaveric decomposition and are responsible for the odor associated with decomposing remains. The direct link between VOC production and individual postmortem microbes has not been well characterized exptl. The purpose of this study was to profile VOCs released from three postmortem bacterial isolates (Bacillus subtilis, Ignatzschineria indica, I. ureiclastica) using solid-phase microextraction arrow (SPME Arrow) and gas chromatog.-mass spectrometry (GC-MS). Species were inoculated in headspace vials on Standard Nutrient Agar and monitored over 5 days at 24°C. Each species exhibited a different VOC profile that included common decomposition VOCs. VOCs exhibited upward or downward temporal trends over time. Ignatzschineria indica produced a large amount of dimethyldisulfide. Other compounds of interest included alcs., aldehydes, aromatics, and ketones. This provides foundational data to link decomposition odor with specific postmortem microbes to improve understanding of underlying mechanisms for decomposition VOC production The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Recommanded Product: 24295-03-2

The Article related to forensic volatile organic compound gas chromatog mass spectrometry, cadaver decomposition, decomposition odor, forensic chemistry, forensic science, forensic taphonomy, postmortem microbiology, solid-phase microextraction arrow and other aspects.Recommanded Product: 24295-03-2

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