Category: 16982-21-1

In 2019,European Journal of Medicinal Chemistry included an article by Li, Zheng; Chen, Yueming; Zhou, Zongtao; Deng, Liming; Xu, Yawen; Hu, Lijun; Liu, Bing; Zhang, Luyong. HPLC of Formula: 16982-21-1. The article was titled 《Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agents》. The information in the text is summarized as follows:

The free fatty acid receptor 1 (FFA1 or GPR40) and peroxisome proliferator-activated receptor δ (PPARδ) have attracted a lot of attention due to their role in promoting insulin secretion and sensibility, resp., which are two major features of diabetes. Therefore, the dual FFA1/PPARδ agonists would increase insulin secretion and sensibility by FFA1 and PPARδ activation. In this study, we hybrid FFA1 agonist AM-4668 with PPARδ agonist GW501516, leading to the identification of orally bioavailable dual agonist 32(I), which revealed high selectivity over other PPARs. Moreover, compound 32 exhibited good pharmacokinetic profiles with high plasma concentration, sustained half-life and low clearance in vivo. During the hypoglycemic test, a dual agonist 32 enhanced the tolerance of ob/ob mice for glucose loading in a dose-dependent manner. Our results suggest that dual FFA1/PPARδ agonist could be a valuable therapy for type 2 diabetes. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1HPLC of Formula: 16982-21-1)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.HPLC of Formula: 16982-21-1

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In 2010,Morinaka, Brandon I.; Pawlik, Joseph R.; Molinski, Tadeusz F. published 《Amaranzoles B-F, Imidazole-2-carboxy Steroids from the Marine Sponge Phorbas amaranthus. C24-N- and C24-O-Analogues from a Divergent Oxidative Biosynthesis》.Journal of Organic Chemistry published the findings.Electric Literature of C4H7NO2S The information in the text is summarized as follows:

Five new steroidal imidazoles, amaranzoles B-F (I-V), were isolated from extracts of the marine sponge Phorbas amaranthus along with the known amaranzole A. The C24-N-(4-p-hydroxyphenyl)imidazol-5-yl constitution found in amaranzoles A, C, and D is replaced by a C24-O-(4-p-hydroxyphenyl)imidazole-2-carboxylate motif in amaranzoles B, E, and F. The structures were elucidated by interpretation of spectroscopic data. The C24 side chain configuration was assigned by synthesis of a model ester followed by chiroptical comparisons of its CD spectrum with that of an amaranzole B derivative In the experiment, the researchers used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Electric Literature of C4H7NO2S)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Electric Literature of C4H7NO2S

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In 2015,Chudinov, M. V.; Matveev, A. V.; Zhurilo, N. I.; Prutkov, A. N.; Shvets, V. I. published 《An Efficient Route to Ethyl 5-Alkyl- (Aryl)-1H-1,2,4-triazole-3-carboxylates》.Journal of Heterocyclic Chemistry published the findings.Computed Properties of C4H7NO2S The information in the text is summarized as follows:

An efficient general route to the synthesis of 5-substituted 1H-1,2,4-triazole-3-carboxylates was developed. N-acylamidrazones were obtained from carboxylic acid hydrazides and Et thiooxamate or Et 2-ethoxy-2-iminoacetate hydrochloride and then were reacted with chloroanhydride of the same carboxylic acid. As the next step, diacylamidrazones were cyclized to 5-substituted 1H-1,2,4-triazole-3-carboxylates in one pot in mild conditions. In the experiment, the researchers used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Computed Properties of C4H7NO2S)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Computed Properties of C4H7NO2S

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《Synthesis and biological evaluation of panaxatriol derivatives against myocardial ischemia/reperfusion injury in the rat》 was written by Wu, Qiong; Wang, Ruiying; Shi, Yang; Li, Wenchao; Li, Meng; Chen, Peng; Pan, Bowen; Wang, Qing; Li, Caifeng; Wang, Jianbing; Sun, Guibo; Sun, Xiaobo; Fu, Hongzheng. Safety of Ethyl 2-amino-2-thioxoacetate And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

Panaxatriol (PT) is a natural product derived from ginseng that possesses cardioprotective effects in isolated rat hearts. To develop more potent therapeutic agents against myocardial ischemia/reperfusion (MI/R) injury from natural products, a novel series of heterocycle ring-fused panaxatriol derivatives were designed and synthesized. In vitro results showed that approx. half of them exhibited increased cytoprotective activity compared with PT in a cardiomyocyte model of oxygen-glucose deprivation and reperfusion (OGD/R) injury. Furthermore, the in vitro activity of the representative derivative, isoxazole derivative I, was also confirmed in a rat model of MI/R injury. In vivo results showed that I can markedly reduce myocardial infarction size, decrease circulating cardiac troponin I (cTnI) leakage, and alleviate cardiac tissue damage in the rats. Therefore, these findings provide the basis for further development of novel anti-MI/R injury agents. In addition to this study using Ethyl 2-amino-2-thioxoacetate, there are many other studies that have used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Safety of Ethyl 2-amino-2-thioxoacetate) was used in this study.

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Safety of Ethyl 2-amino-2-thioxoacetate

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Recommanded Product: 16982-21-1In 2016 ,《Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes》 was published in European Journal of Medicinal Chemistry. The article was written by Li, Zheng; Qiu, Qianqian; Xu, Xue; Wang, Xuekun; Jiao, Lei; Su, Xin; Pan, Miaobo; Huang, Wenlong; Qian, Hai. The article contains the following contents:

The free fatty acid receptor 1 (FFA1/GPR40) has attracted interest as a novel target for the treatment of type 2 diabetes. Several series of FFA1 agonists including TAK-875, the most advanced compound terminated in phase III studies due to concerns about liver toxicity, have been hampered by relatively high mol. weight and lipophilicity. Aiming to develop potent FFA1 agonists with low risk of liver toxicity by decreasing the lipophilicity, the middle benzene ring of TAK-875 was replaced by 11 polar five-membered heteroaromatics Subsequently, systematic exploration of SAR and application of mol. modeling, leads to the identification of compound I, which was an excellent FFA1 agonist with robustly hypoglycemic effect both in normal and type 2 diabetic mice, low risks of hypoglycemia and liver toxicity even at the twice molar dose of TAK-875. Meanwhile, two important findings were noted. First, the Me group in our thiazole series occupied a small hydrophobic subpocket which had no interactions with TAK-875. Furthermore, the agonistic activity revealed a good correlation with the dihedral angle between thiazole core and the terminal benzene ring. These results promote the understanding of ligand-binding pocket and might help to design more promising FFA1 agonists. In the experiment, the researchers used many compounds, for example, Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Recommanded Product: 16982-21-1)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Recommanded Product: 16982-21-1

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Safety of Ethyl 2-amino-2-thioxoacetateIn 2002 ,《Anilinoquinazoline Inhibitors of Fructose 1,6-Bisphosphatase Bind at a Novel Allosteric Site: Synthesis, In Vitro Characterization, and X-ray Crystallography》 was published in Journal of Medicinal Chemistry. The article was written by Wright, Stephen W.; Carlo, Anthony A.; Carty, Maynard D.; Danley, Dennis E.; Hageman, David L.; Karam, George A.; Levy, Carolyn B.; Mansour, Mahmoud N.; Mathiowetz, Alan M.; McClure, Lester D.; Nestor, Nestor B.; McPherson, R. Kirk; Pandit, Jayvardhan; Pustilnik, Leslie R.; Schulte, Gayle K.; Soeller, Walter C.; Treadway, Judith L.; Wang, Ing-Kae; Bauer, Paul H.. The article contains the following contents:

Thiazolylphenylaminoquinazolines I (R = H, Me, c-C3H5, EtCH2, Ph, PhCH2, HOCH2, MeOCH2, H2N, MeNH, Me2N, H2NNH, MeO, EtO, HO2C, H2NCO; R1 = H, F; R2 = H, Cl, F; R3 = H, F3C; R4 = H, Br, Cl, F, Me, MeO, Et, EtO; R5 = H, Me, Et, EtCH2, Me2CH, PhCH2, Cl, ClCH2, ClCH2CH2, ClCH2CH2CH2, F3C, MeSO2CH2, MeOCH2, H2NCH2, Me2NCH2, EtNHCH2, 1-pyrrolidinylmethyl, HO2CCH2, 1-imidazolyl, H2NCH2CH2) and other heterocyclyl- and arylphenylaminoquinazolines were prepared and found to act as allosteric inhibitors of fructose-1,6-bisphosphatase (F16BPase); the structure-activity relationship of I to binding at F16BPase and selectivity for F16BPase over the epidermal growth factor receptor tyrosine kinase (EGFR), the original target for I, were evaluated. I have a different SAR as inhibitors of F16Bpase than anilinoquinazolines previously reported. Selective inhibition of F16BPase was attained through the addition of appropriate polar functional groups at the quinazoline 2-position, thus separating the F16BPase inhibitory activity from the epidermal growth factor receptor tyrosine kinase inhibitory activity previously observed with similar structures. Substitution of other heterocycles for the thiazolyl moiety in I gave compounds with variable activities at both F16BPase and at EGFR; the effective inhibitors were selective for EGFR. Alteration of the 6,7-diethoxyquinazoline segment abolished F16BPase inhibition. A symmetry-repeated novel allosteric site present in the homotetrameric form of F16BPase at the interface of its subunits was found to bind I and related anilinoquinazolines. I inhibit F16BPase by binding to a loop comprised of residues 52-72 in the monomer, preventing the necessary participation of these residues in the assembly of the catalytic site. Mutagenesis of glutamine 50 and of glutamine 55 of F16BPase abolish the binding of I and are the key amino acid residues required for inhibitor recognition and binding. The crystal structure of I (R = HOCH2; R1 = R2 = R3 = R4 = R5 = H) bound to porcine kidney F16BPase was determined In the experimental materials used by the author, we found Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Safety of Ethyl 2-amino-2-thioxoacetate)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Safety of Ethyl 2-amino-2-thioxoacetate

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Computed Properties of C4H7NO2SIn 2020 ,《Design, Synthesis, and Evaluation of the Antifungal Activity of Novel Pyrazole-Thiazole Carboxamides as Succinate Dehydrogenase Inhibitors》 appeared in Journal of Agricultural and Food Chemistry. The author of the article were Yu, Bin; Zhou, Shuang; Cao, Lixin; Hao, Zesheng; Yang, Dongyan; Guo, Xiaofeng; Zhang, Nailou; Bakulev, Vasiliy A.; Fan, Zhijin. The article conveys some information:

Succinate dehydrogenase (SDH) is regarded as a promising target for fungicide discovery. To continue our ongoing studies on the discovery of novel SDH inhibitors as fungicides, novel pyrazole-thiazole carboxamides were designed, synthesized, and evaluated for their antifungal activity. The results indicated that compounds 9ac, 9bf, and 9cb showed excellent in vitro activities against Rhizoctonia cerealis with EC50 values from 1.1 to 4.9 mg/L, superior to that of the com. fungicide thifluzamide (EC50 = 23.1 mg/L). Compound 9cd (EC50 = 0.8 mg/L) was far more active than thifluzamide (EC50 = 4.9 mg/L) against Sclerotinia sclerotiorum. Compound 9ac exhibited promising in vivo activity against Rhizoctonia solani (90% at 10 mg/L), which was better than that of thifluzamide (80% at 10 mg/L). The field experiment showed that compound 9ac had 74.4% efficacy against Rhizoctonia solani on the 15th day after two consecutive sprayings at an application rate of 4.80 g a.i./667 m2, which was close to that of thifluzamide (83.3%). Furthermore, mol. docking explained the possible binding mode of compound 9ac in the RcSDH active site. Our studies indicated that the pyrazole-thiazole carboxamide hybrid is a new scaffold of SDH inhibitors. The experimental process involved the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Computed Properties of C4H7NO2S)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Computed Properties of C4H7NO2S

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Formula: C4H7NO2SIn 2021 ,《Structure-activity relationship studies in substituted sulfamoyl benzamidothiazoles that prolong NF-κB activation》 was published in Bioorganic & Medicinal Chemistry. The article was written by Shukla, Nikunj M.; Chan, Michael; Lao, Fitzgerald S.; Chu, Paul J.; Belsuzarri, Masiel; Yao, Shiyin; Nan, Jason; Sato-Kaneko, Fumi; Saito, Tetsuya; Hayashi, Tomoko; Corr, Maripat; Carson, Dennis A.; Cottam, Howard B.. The article contains the following contents:

In the face of emerging infectious diseases, there remains an unmet need for vaccine development where adjuvants that enhance immune responses to pathogenic antigens are highly desired. Using high-throughput screens with a cell-based nuclear factor κB (NF-κB) reporter assay, we identified a sulfamoyl benzamidothiazole bearing compound 1 that demonstrated a sustained activation of NF-κB after a primary stimulus with a Toll-like receptor (TLR)-4 agonist, lipopolysaccharide (LPS). Here, we explore systematic structure-activity relationship (SAR) studies on compound 1 that indicated the sites on the scaffold that tolerated modification and yielded more potent compounds compared to 1. The selected analogs enhanced release of immunostimulatory cytokines in the human monocytic cell line THP-1 cells and murine primary dendritic cells. In murine vaccination studies, select compounds were used as co-adjuvants in combination with the Food and Drug Administration approved TLR-4 agonistic adjuvant, monophosphoryl lipid A (MPLA) that showed significant enhancement in antigen-specific antibody titers compared to MPLA alone. Addnl., our SAR studies led to identification of a photoaffinity probe which will aid the target identification and mechanism of action studies in the future. In the experiment, the researchers used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Formula: C4H7NO2S)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Formula: C4H7NO2S

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《Design, Synthesis, and Anticancer Activity of 1,2,3-Triazole Linked Thiazole-1,2-isoxazole Derivatives》 was written by Yakantham, T.; Sreenivasulu, R.; Alluraiah, G.; Tej, M. B.; Ramesh Raju, R.. Name: Ethyl 2-amino-2-thioxoacetateThis research focused ontriazole thiazole isoxazole derivative preparation cancer. The article conveys some information:

Abstract: A series of novel 1,2,3-triazole linked thiazole-1,2-isoxazole derivatives has been designed, synthesized and characterized by 1H and 13C NMR, and mass spectral anal. The compounds have been tested for their anticancer activity towards MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer), and A2780 (ovarian cancer) by using the MTT method using etoposide as the reference Most of the tested compounds demonstrate good to moderate activity against all cell lines. The compounds 14b, 14e, 14g, and 14h are characterized by inhibitory activity stronger than that of etoposide. After reading the article, we found that the author used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Name: Ethyl 2-amino-2-thioxoacetate)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Name: Ethyl 2-amino-2-thioxoacetate

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In 2012,Nitta, Aiko; Fujii, Hideaki; Sakami, Satoshi; Satoh, Mikiya; Nakaki, Junko; Satoh, Shiho; Kumagai, Hiroki; Kawai, Hideki published 《Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 16982-21-1 The information in the text is summarized as follows:

A series of novel 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides were investigated as dipeptidyl peptidase IV (DPP-4) inhibitors. Introduction of a 4-phenylthiazol-2-yl group showed highly potent DPP-4 inhibitory activity. Among various derivatives, (3R)-3-amino-N-(4-(4-phenylthiazol-2-yl)-tetrahydro-2H-thiopyran-4-yl)-4-(2,4,5-trifluorophenyl)butanamide 1,1-dioxide reduced blood glucose excursion in an oral glucose tolerance test by oral administration. In the experiment, the researchers used Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Application of 16982-21-1)

Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Application of 16982-21-1

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