Day: February 22, 2023

The effect of heat on beef aroma: comparisons of chemical composition and sensory properties was written by MacLeod, Glesni;Ames, Jennifer M.. And the article was included in Flavour and Fragrance Journal in 1986.Safety of 2-Methyl-4,5-dihydrothiazole This article mentions the following:

Aroma volatiles of fresh cooked ground beef subjected to varying degrees of heating were adsorbed on to the adsorbent Tenax TA, and the desorbed aromas analyzed sensorially and chem. Several of the components identified by combined capillary gas chromatog.-mass spectrometry have not been reported previously from heated beef. Data is presented to support the generalization that the higher the degree of heating, the greater the concentrations of aliphatic aldehydes (especially Strecker aldehydes), benzenoids, aliphatic polysulfides, heterocyclic compounds and lipid-derived volatiles, whereas smaller contributions to the isolates arise from aliphatic ketones and alcs. (of non-lipid origin) and aliphatic mono-sulfur components. By sensory anal., eight of odor qualities were frequently used during gas chromatog. odor port assessment, namely buttery, caramel, burnt, green, fragrant, oily/fatty, nutty and meaty. Components associated with the former seven qualities are aroma modifiers whereas compounds contributing meaty quality are character impact compounds, e.g. 2-methyl-3-(methylthio)furan and 3-methylcyclopentanone. Addnl., several unsaturated alicyclic ketones were present which resemble the cyclohexenones previously known to be significant in meat aroma. In the experiment, the researchers used many compounds, for example, 2-Methyl-4,5-dihydrothiazole (cas: 2346-00-1Safety of 2-Methyl-4,5-dihydrothiazole).

2-Methyl-4,5-dihydrothiazole (cas: 2346-00-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Safety of 2-Methyl-4,5-dihydrothiazole

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

Incompatibility of cefotiam dihydrochloride in parenteral preparations by high-performance liquid chromatography was written by Tanno, Keiki;Ikarashi, Kuniichi;Sasahara, Kazuhisa;Kato, Masami. And the article was included in Japanese Journal of Antibiotics in 1982.Synthetic Route of C18H25Cl2N9O4S3 This article mentions the following:

Changes in external appearance, pH, and residual antimicrobial potency of cefotiam-HCl (I) [66309-69-1] were examined in combination with infusion solutions and other injections. The combination of I with bromhexine-HCl聽聽[611-75-6], dipyridamole聽聽[58-32-2], and gabexate聽mesilate聽聽[56974-61-9] was incompatible because of the turbidity produced. No change was observed in 34 other combinations. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1Synthetic Route of C18H25Cl2N9O4S3).

(6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Synthetic Route of C18H25Cl2N9O4S3

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

Organocatalyst-Mediated Dynamic Kinetic Enantioselective Acylation of 2-Chromanols was written by Glazier, Daniel A.;Schroeder, John M.;Liu, Jitian;Tang, Weiping. And the article was included in Advanced Synthesis & Catalysis in 2018.Synthetic Route of C15H12N2S This article mentions the following:

In this update, a catalytic method for the dynamic kinetic enantioselective acylation of 2-chromanols using benzotetramisole-derived catalysts is reported. High yields and enantiomeric excesses were obtained for a broad range of acylated 2-chromanols, which are important intermediates for the synthesis of various bioactive pharmaceuticals. The high stereoselectivity of the reaction originates from a novel cation-n interaction between the chromanol substrate and the acylated catalyst. In the experiment, the researchers used many compounds, for example, (S)-2-Phenyl-2,3-dihydrobenzo[d]imidazo[2,1-b]thiazole (cas: 950194-37-3Synthetic Route of C15H12N2S).

(S)-2-Phenyl-2,3-dihydrobenzo[d]imidazo[2,1-b]thiazole (cas: 950194-37-3) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Synthetic Route of C15H12N2S

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

Copper-Catalyzed Three-Component Synthesis of Benzothiazolethiones from o-Iodoanilines, Isocyanide, and Potassium Sulfide was written by Dang, Pan;Zeng, Weilan;Liang, Yun. And the article was included in Organic Letters in 2015.Computed Properties of C7H4FNS2 This article mentions the following:

An efficient copper catalyzed strategy for the synthesis of a variety of benzothiazolethione derivatives has been developed. In the presence of CuCl, the three-component reaction of o-iodoanilines and K₂S with p-toluenesulfonylmethyl isocyanide proceeded smoothly to obtain the corresponding benzothiazolethiones in good to excellent isolated yields. Notably, isocyanide functioned as a carbon source and K₂S functioned as a sulfur source in this reaction. In the experiment, the researchers used many compounds, for example, 6-Fluorobenzo[d]thiazole-2(3H)-thione (cas: 80087-71-4Computed Properties of C7H4FNS2).

6-Fluorobenzo[d]thiazole-2(3H)-thione (cas: 80087-71-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C7H4FNS2

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

A new class of chiral pyrrolidine-pyridine conjugate base catalysts for use in asymmetric Michael addition reactions was written by Ishii, Takaaki;Fujioka, Shingo;Sekiguchi, Yusuke;Kotsuki, Hiyoshizo. And the article was included in Journal of the American Chemical Society in 2004.Reference of 132635-95-1 This article mentions the following:

Direct catalytic asym. Michael addition reaction of ketones to nitroolefins, using chiral pyrrolidine-pyridine conjugate bases, e.g., I, as catalysts, is described. The desired 1,4-adducts were obtained in excellent yields with high enantio- and diastereoselectivities. In the experiment, the researchers used many compounds, for example, (S)-Tetrahydro-3H-pyrrolo[1,2-c][1,2,3]oxathiazole 1,1-dioxide (cas: 132635-95-1Reference of 132635-95-1).

(S)-Tetrahydro-3H-pyrrolo[1,2-c][1,2,3]oxathiazole 1,1-dioxide (cas: 132635-95-1) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Reference of 132635-95-1

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

Changes of antibiotic occurrence and hydrochemistry in groundwater under the influence of the South-to-North Water Diversion (the Hutuo River, China) was written by Wang, Jialin;Zhang, Chong;Xiong, Ling;Song, Guangdong;Liu, Fei. And the article was included in Science of the Total Environment in 2022.Quality Control of 4-Amino-N-(thiazol-2-yl)benzenesulfonamide This article mentions the following:

The occurrence of antibiotics in groundwater has significant spatial variability, owing to the complexity of pollutant properties, pollution sources and groundwater recharge and discharge conditions. This study aimed to identify the relationship between antibiotic occurrence and hydrochem. in groundwater. Thus, we undertook this study in a characteristic alluvial-diluvial aquifer where groundwater receives unidirectional recharge from surface water. In total, 47 samples were collected from the Hutuo River before and after an artificial replenishment project. We screened up to four classes of antibiotics and detected 28 types. The statistical anal. of antibiotic concentrations, indicated that there were two pollution areas. Next, we discussed the results pertaining to the occurrence and source of antibiotics by comparing them with hydrochem. data. In the study area, a pos. correlation has been found between inorganic compounds, as SO₄^2-and Cl^–, and the most mobile antibiotics given that both share the same source. This shows that a previous sound geochem. study may provide evidence of the extend of antibiotic occurrence, as in the Hutuo River aquifer. The relationship between antibiotics and hydrochem. in groundwater is determined by recharge sources (rainwater and surface water contaminated with antibiotics). Antibiotics from wastewater treatment plants enter groundwater indirectly through surface water with high SO₄^2- in lightly polluted areas, while in heavily polluted areas, there are high concentrations of inorganic components in garbage leachate and wastewater leakage that carry antibiotics directly into groundwater. In summarized, the relationship between antibiotics and hydrochem. observed in this study shows that a previous sound geochem. study may provide evidence of the extend of antibiotic occurrence. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(thiazol-2-yl)benzenesulfonamide (cas: 72-14-0Quality Control of 4-Amino-N-(thiazol-2-yl)benzenesulfonamide).

4-Amino-N-(thiazol-2-yl)benzenesulfonamide (cas: 72-14-0) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Quality Control of 4-Amino-N-(thiazol-2-yl)benzenesulfonamide

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

Genomewide comparison of the inducible transcriptomes of nuclear receptors CAR, PXR and PPAR伪 in primary human hepatocytes was written by Kandel, Benjamin A.;Thomas, Maria;Winter, Stefan;Damm, Georg;Seehofer, Daniel;Burk, Oliver;Schwab, Matthias;Zanger, Ulrich M.. And the article was included in Biochimica et Biophysica Acta, Gene Regulatory Mechanisms in 2016.Quality Control of 6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime This article mentions the following:

The ligand-activated nuclear receptor pregnane X receptor (PXR, NR1I2) and the constitutive androstane receptor (CAR, NR1I3) are two master transcriptional regulators of many important drug metabolizing enzymes and transporter genes (DMET) in response to xenobiotics including many drugs. The peroxisome proliferator-activated receptor alpha (PPAR伪, NR1C1), the target of lipid lowering fibrate drugs, primarily regulates fatty acid catabolism and energy-homeostasis. Recent research has shown that there are substantial overlaps in the regulated genes of these receptors. For example, both CAR and PXR also modulate the transcription of key enzymes involved in lipid and glucose metabolism and PPAR伪 also functions as a direct transcriptional regulator of important DMET genes including cytochrome P450s CYP3A4 and CYP2C8. Despite their important and widespread influence on liver metabolism, comparative data are scarce, particularly at a global level and in humans. The major objective of this study was to directly compare the genome-wide transcriptional changes elucidated by the activation of these three nuclear receptors in primary human hepatocytes. Cultures from six individual donors were treated with the prototypical ligands for CAR (CITCO), PXR (rifampicin) and PPAR伪 (WY14,643) or DMSO as vehicle control. Genomewide mRNA profiles determined with Affymetrix microarrays were analyzed for differentially expressed genes and metabolic functions. The results confirmed known prototype target genes and revealed strongly overlapping sets of coregulated but also distinctly regulated and novel responsive genes and pathways. The results further specify the role of PPAR伪 as a regulator of drug metabolism and the role of the xenosensors PXR and CAR in lipid metabolism and energy homeostasis. This article is part of a Special Issue entitled: Xenobiotic nuclear receptors: New Tricks for An Old Dog, edited by Dr. Wen Xie. In the experiment, the researchers used many compounds, for example, 6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime (cas: 338404-52-7Quality Control of 6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime).

6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime (cas: 338404-52-7) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Quality Control of 6-(4-Chlorophenyl)imidazo[2,1-b]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl) oxime

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

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13 was written by Liu, Yao;Hao, Mingfeng;Leggett, Alan L.;Gao, Yang;Ficarro, Scott B.;Che, Jianwei;He, Zhixiang;Olson, Calla M.;Marto, Jarrod A.;Kwiatkowski, Nicholas P.;Zhang, Tinghu;Gray, Nathanael S.. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 3034-57-9 This article mentions the following:

Genetic depletion of cyclin-dependent kinase 12 (CDK12) or selective inhibition of an analog-sensitive CDK12 reduces DNA damage repair gene expression, but selective inhibition of endogenous CDK12 is difficult. Here, we report the development of MFH290(I), a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib. In the experiment, the researchers used many compounds, for example, 2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9Product Details of 3034-57-9).

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Product Details of 3034-57-9

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

Tryptophan Pathway-Targeted Metabolomics Study on the Mechanism and Intervention of Cisplatin-Induced Acute Kidney Injury in Rats was written by Tan, Bei;Chen, Jie;Qin, Siyuan;Liao, Chuyao;Zhang, Ying;Wang, Di;Li, Siqi;Zhang, Zunjian;Zhang, Pei;Xu, Fengguo. And the article was included in Chemical Research in Toxicology in 2021.Application of 533-45-9 This article mentions the following:

Cisplatin is a chemotherapeutic agent widely employed in the treatment of various solid tumors. However, its use is often restricted by acute kidney injury (AKI) which is the dose-limiting adverse effect of cisplatin. While numerous studies aiming to alleviate the AKI have been conducted, there are no effective remedies in clin. practice. In this paper, a targeted metabolomics study was performed to reveal the potential relationship between tryptophan metabolism and cisplatin-induced AKI. A chem. derivatization integrated liquid chromatog. coupled tandem mass spectrometry (LC-MS/MS) approach was utilized to quantify 29 metabolites in the tryptophan pathway in rat kidney medulla and cortex after cisplatin administration. Results showed that tryptophan metabolism was remarkably disturbed both in the medulla and cortex after cisplatin administration. We also found that the tryptophan pathway in the medulla was more sensitive to cisplatin exposure compared with the cortex. Among these metabolites, indoxyl sulfate was focused for further study because it accumulated most significantly in the kidney cortex and medulla in a dose-dependent manner. A function verification study proved that chlormethiazole, a widely used CYP2E1 inhibitor, could reduce the production of indoxyl sulfate in the liver and attenuate cisplatin-induced AKI in rats. In conclusion, our study depicted the tryptophan pathway in cisplatin-induced AKI for the first time and demonstrated tryptophan metabolism is closely associated with the renal toxicity caused by cisplatin, which can be of great use for the discovery of renal toxicity attenuating remedies. In the experiment, the researchers used many compounds, for example, 5-(2-Chloroethyl)-4-methylthiazole (cas: 533-45-9Application of 533-45-9).

5-(2-Chloroethyl)-4-methylthiazole (cas: 533-45-9) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Application of 533-45-9

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

Reconstitution time and microbial contamination during reconstitution of antibiotic kit product was written by Ishii, Masahide. And the article was included in Igaku to Yakugaku in 1995.Reference of 66309-69-1 This article mentions the following:

Reconstitution time determination indicated that antibiotic (pansporin) kit preparation is superior to antibiotic half kit preparation or conventional injection. Microbial contamination tests showed similar results (neg.) for all the 3 products (methods) tested. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1Reference of 66309-69-1).

(6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 66309-69-1

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