Category: 64987-16-2

Tomasic, Tihomir’s team published research in Bioorganic & Medicinal Chemistry in 25 | CAS: 64987-16-2

Bioorganic & Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C13H15NO6S, Application of Methyl 2-(2-aminothiazol-4-yl)acetate.

Tomasic, Tihomir published the artcileDesign, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors, Application of Methyl 2-(2-aminothiazol-4-yl)acetate, the publication is Bioorganic & Medicinal Chemistry (2017), 25(1), 338-349, database is CAplus and MEDLINE.

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.

Bioorganic & Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C13H15NO6S, Application of Methyl 2-(2-aminothiazol-4-yl)acetate.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Muri, E. M. F.’s team published research in Letters in Drug Design & Discovery in 1 | CAS: 64987-16-2

Letters in Drug Design & Discovery published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Computed Properties of 64987-16-2.

Muri, E. M. F. published the artcileMolecular modeling, synthesis and biological evaluation of heterocyclic hydroxamic acids designed as Helicobacter pylori urease inhibitors, Computed Properties of 64987-16-2, the publication is Letters in Drug Design & Discovery (2004), 1(1), 30-34, database is CAplus.

A computer-generated homol. model of the antimicrobial target Helicobacter pylori urease was derived, using the x-ray crystal structure of Klebsiella aerogenes as a template, in order to design novel urease inhibitors. Based on these computational studies, several heterocyclic hydroxamic acid derivatives have been designed, synthesized, and examined for their ability to inhibit urease activity.

Letters in Drug Design & Discovery published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Computed Properties of 64987-16-2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Muri, Estela Maris F.’s team published research in Synthetic Communications in 33 | CAS: 64987-16-2

Synthetic Communications published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate.

Muri, Estela Maris F. published the artcileDesign and synthesis of heterocyclic hydroxamic acid derivatives as inhibitors of Helicobacter pylori urease, Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate, the publication is Synthetic Communications (2003), 33(12), 1977-1995, database is CAplus.

Helicobacter pylori produces ammonia to help counter the acidic environment in the human stomach. The production of ammonia, essential for the microorganism’s survival and virulence, is the product of enzymic conversion of urea by the H. pylori’s urease. Inhibition of urease activity by dipeptide hydroxamic acids has previously been demonstrated using a variety of fluorides, thiols and hydroxamic acids. Studies employing computer-aided drug design techniques have been utilized to suggest a novel series of heterocyclic hydroxamic acid derivatives as potential urease inhibitors. Heterocyclic compounds such as I, II, III, and IV have been designed, synthesized, and preliminarily tested as dipeptide mimics which offer a structure that is more biol. stable than that of the reported dipeptide inhibitors.

Synthetic Communications published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Margathe, Jean-Francois’s team published research in Journal of Medicinal Chemistry in 57 | CAS: 64987-16-2

Journal of Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Quality Control of 64987-16-2.

Margathe, Jean-Francois published the artcileStructure-Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists, Quality Control of 64987-16-2, the publication is Journal of Medicinal Chemistry (2014), 57(7), 2908-2919, database is CAplus and MEDLINE.

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).

Journal of Medicinal Chemistry published new progress about 64987-16-2. 64987-16-2 belongs to thiazole, auxiliary class Thiazole,Amine,Ester, name is Methyl 2-(2-aminothiazol-4-yl)acetate, and the molecular formula is C6H8N2O2S, Quality Control of 64987-16-2.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Mugherli, Laurent et al. published their research in Angewandte Chemie, International Edition in 2009 |CAS: 64987-16-2

The Article related to drug screening ns3 4a protease inhibitor preparation microarray, Pharmacology: Methods and other aspects.Synthetic Route of 64987-16-2

Mugherli, Laurent; Burchak, Olga N.; Balakireva, Larissa A.; Thomas, Aline; Chatelain, Francois; Balakirev, Maxim Y. published an article in 2009, the title of the article was In Situ Assembly and Screening of Enzyme Inhibitors with Surface-Tension Microarrays.Synthetic Route of 64987-16-2 And the article contains the following content:

Hundreds of reactions were conducted in parallel in droplets maintained on a glass slide through differential surface tension in a new approach to submicroliter-scale synthesis. This surface-tension microarray was applied to the in situ assembly of thousands of derivatives of phenylboronic acid and their profiling against the NS3/4A protease of the hepatitis C virus. Several potent inhibitors of the enzyme were identified. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Synthetic Route of 64987-16-2

The Article related to drug screening ns3 4a protease inhibitor preparation microarray, Pharmacology: Methods and other aspects.Synthetic Route of 64987-16-2

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

Bolchi, Cristiano et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2011 |CAS: 64987-16-2

The Article related to preparation thiazole imidazole peptidomimetic inhibitor farnesyltransferase, Pharmacology: Structure-Activity and other aspects.SDS of cas: 64987-16-2

Bolchi, Cristiano; Pallavicini, Marco; Bernini, Sergio K.; Chiodini, Giuseppe; Corsini, Alberto; Ferri, Nicola; Fumagalli, Laura; Straniero, Valentina; Valoti, Ermanno published an article in 2011, the title of the article was Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.SDS of cas: 64987-16-2 And the article contains the following content:

Mimetics of the C-terminal CAAX tetrapeptide of Ras protein were designed replacing internal dipeptide AA with 4-amino-2-phenylbenzoic acid and cysteine (C) with 2-amino-4-thiazolyl-, 2-mercapto-4-thiazolyl-, 2-mercapto-4-imidazolyl- and 2-methylmercapto-4-thiazolyl-acetic or propionic acid. The compound in which C is replaced by 2-amino-4-thiazolylacetic acid inhibited FTase activity in the low nanomolar range and showed antiproliferative effect on rat aortic smooth muscle cells interfering with Ras farnesylation. On the basis of these results, 2-aminothiazole can be considered as an alternative to heterocycles, such as pyridine and imidazole, normally used in FTase inhibitors designed as non-thiol CAAX mimetics. 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 preparation thiazole imidazole peptidomimetic inhibitor farnesyltransferase, Pharmacology: Structure-Activity and other aspects.SDS of cas: 64987-16-2

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

Muri, E. M. F. et al. published their research in Letters in Drug Design & Discovery in 2004 |CAS: 64987-16-2

The Article related to helicobacter urease inhibitor heterocyclic hydroxamate derivative preparation, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 64987-16-2

On January 31, 2004, Muri, E. M. F.; Mishra, H.; Stein, S. M.; Williamson, J. S. published an article.Recommanded Product: 64987-16-2 The title of the article was Molecular modeling, synthesis and biological evaluation of heterocyclic hydroxamic acids designed as Helicobacter pylori urease inhibitors. And the article contained the following:

A computer-generated homol. model of the antimicrobial target Helicobacter pylori urease was derived, using the x-ray crystal structure of Klebsiella aerogenes as a template, in order to design novel urease inhibitors. Based on these computational studies, several heterocyclic hydroxamic acid derivatives have been designed, synthesized, and examined for their ability to inhibit urease activity. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Recommanded Product: 64987-16-2

The Article related to helicobacter urease inhibitor heterocyclic hydroxamate derivative preparation, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 64987-16-2

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

Sheth, Hasmukh B. et al. published their research in Journal of Agricultural and Food Chemistry in 1991 |CAS: 64987-16-2

The Article related to sulfonamide determination food, immunoassay sulfonamide, elisa sulfonamide, Food and Feed Chemistry: Analysis and other aspects.Synthetic Route of 64987-16-2

On September 30, 1991, Sheth, Hasmukh B.; Sporns, Peter published an article.Synthetic Route of 64987-16-2 The title of the article was Development of a single ELISA for detection of sulfonamides. And the article contained the following:

A sulfathiazole derivative was chem. linked to proteins in such a way that the aromatic amino group, common to all sulfonamides, was distal to the protein. A subset of the antibodies developed against this immunization conjugate could be used competitively with different sulfonamide haptens, linking methods and proteins to develop ELISA methods that had a broad spectrum of sulfonamide recognition. By use of the best ELISA protocol, 9 different sulfonamides decreased absorbance values 50% at concentrations <2 nM per assay. The sulfonamides recognized by the competitive ELISA had similar steric characteristics but considerable variation in electronic configuration. The method may be developed for screening of foods and related materials. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Synthetic Route of 64987-16-2

The Article related to sulfonamide determination food, immunoassay sulfonamide, elisa sulfonamide, Food and Feed Chemistry: Analysis and other aspects.Synthetic Route of 64987-16-2

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

Haasnoot, Willem et al. published their research in Food and Agricultural Immunology in 2000 |CAS: 64987-16-2

The Article related to elisa sulfonamide immunodetection, Biochemical Methods: Immunological and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

On June 30, 2000, Haasnoot, Willem; Du Pre, Jolanda; Cazemier, Geert; Kemmers-Voncken, Anniek; Verheijen, Ron; Jansen, Ben J. M. published an article.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the article was Monoclonal antibodies against a sulfathiazole derivative for the immunochemical detection of sulfonamides. And the article contained the following:

To prepare monoclonal antibodies (mAbs) against the generic part of sulfonamides, a sulfathiazole derivative was chem. linked to carrier proteins in such a way that the aromatic amino group, common to all sulfonamides, was distal to the proteins. Four mice were immunized with the sulfathiazole-protein derivatives The spleen cells of one of the mice were fused with myeloma cells to produce hybridomas of which the supernatants were screened in an indirect ELISA (iELISA) for the presence of sulfathiazole antibodies. After cloning, pos. supernatants were tested in a competitive iELISA (ciELISA) for inhibition with 18 sulfonamides. This resulted in four different mAbs (all IgG1 kappa light chain) which recognized several sulfonamides. By use of the best monoclonal (27G3) and an optimized ciELISA protocol, eight structurally different sulfonamides showed 50% inhibition at concentrations less than 100 ng ml-1 or 5 ng/well. However, other relevant sulfonamides (such as sulfadimidine, sulfatroxazole and sulfachloropyrazine) were detected at a high level only with this mAb. This means that the ciELISA (with the best Mab) showed a broad specificity for sulfonamides but the sensitivity towards the different sulfonamides varied too much to call it a generic sulfonamide ELISA. 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 elisa sulfonamide immunodetection, Biochemical Methods: Immunological and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

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

Hua, Jin et al. published their patent in 2017 |CAS: 64987-16-2

The Article related to immunoaffinity chromatog animal derived food sulfonamide feed additives spectrometry, Biochemical Methods: Chromatographic and other aspects.Recommanded Product: 64987-16-2

On June 30, 2017, Hua, Jin published a patent.Recommanded Product: 64987-16-2 The title of the patent was Preparation method of immunoaffinity column (IAC) for detecting sulfonamide residue in animal-derived food. And the patent contained the following:

The title preparation method includes (1) preparing sulfonamide artificial antigens TS-BSA and SM2-BSA by sep. coupling tetramethylthiuram monosulfide (TS) antigen and sulfadimidine SM2 antigen with bovine serum albumin (BSA) and ovalbumin; (2) immunizing mouse, collecting B lymphocytes, fusing with myeloma cells to obtain hybridoma cells, and preparing Batroxobin toxin monoclonal antibody 5H4, NR3C2 monoclonal antibody 2B5 and PPBP monoclonal antibody 5C7 by in vivo induced ascites generation method; and (3) sep. coupling the monoclonal antibodies with cyanogen bromide-activated sepharose 4B, mixing at ratio of 1:1:1, and packing into a column to obtain composite immunoaffinity column (IAC). The composite IAC has good specific adsorption effect on at least 12 kinds of sulfonamides as follows: ulfaquinoxaline, sulfadiazine, sulfapyridine, sulfameter, sulfadimidine, sulfamethoxazole, sulfisoxazole, sulfadimethoxypyrimidine, sulfathiazole, slfamerazine free acid, sodium N-(6-chloropyridazin-3-yl)sulphanilamidate and sulfamonomethoxine. The inventive IAC has high coupling rate, strong specific adsorption and high column capacity and yield, and can be used for detecting the above sulfonamide residues in animal-derived food sensitively, rapidly and simply. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Recommanded Product: 64987-16-2

The Article related to immunoaffinity chromatog animal derived food sulfonamide feed additives spectrometry, Biochemical Methods: Chromatographic and other aspects.Recommanded Product: 64987-16-2

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