Tag: 100-200

Burger, Alfred; Sawhney, S. N. published an article in 1968, the title of the article was Antimalarials. III. Benzothiazole amino alcohols.Computed Properties of 19989-66-3 And the article contains the following content:

Amino alcs. carrying a CHOH(CH2)1-3NR2 chain in position 6 of a benzothiazole nucleus, unsubstituted or substituted by Ph or CF3 in the 2 position, have been synthesized by standard methods and tested for activity against Plasmodium berghei in mice. Several of the amino alcs. showed weak antimalarial activity but only at toxic doses. 15 references. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Computed Properties of 19989-66-3

The Article related to amino alcohols: chemical synthesis, amino alcohols: therapeutic use, amino alcohols: toxicity, animals, antimalarials: chemical synthesis, antimalarials: therapeutic use, antimalarials: toxicity, mice, thiazoles: chemical synthesis, thiazoles: therapeutic use and other aspects.Computed Properties of 19989-66-3

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

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

On May 30, 2021, Wang, Xiao-Yuan; Ma, Yun-Jiao; Guo, Yu; Luo, Xiao-Lin; Du, Ming; Dong, Liang; Yu, Pei; Xu, Xian-Bing published an article.COA of Formula: C5H5NOS The title of the article was Reinvestigation of 2-acetylthiazole formation pathways in the Maillard reaction. And the article contained the following:

2-Acetylthiazole possesses a nutty, cereal-like and popcorn-like aroma and a low odor threshold, and this compound has been identified in some processed foods, while the formation pathway of 2-acetylthiazole has not been clearly elucidated. Here, a model reaction of D-glucose and L-cysteine was constructed to investigate the formation pathway of 2-acetylthiazole. L-Cysteine, D-glucose and the corresponding intermediates, namely, dicarbonyl compounds (DCs), were involved in the formation of 2-acetylthiazole and detected by high-performance liquid chromatog. with tandem mass spectrometry (HPLC-MS/MS), high-performance ion chromatog. (HPIC) and HPLC, resp. The carbon module labeling (CAMOLA) technique revealed that the C-4 and C-5 of 2-acetylthiazole were derived from the carbons of glucose. The potential of glyoxal, which is degraded by glucose, to form 2-acetylthiazole was revealed for the first time. A novel route to form 2-acetylthiazole by the reaction of glyoxal and methylglyoxal produced by D-glucose with H2S and NH3 produced by L-cysteine was proposed. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).COA of Formula: C5H5NOS

The Article related to methylglyoxal d glucose l cysteine 2 acetylthiazole maillard reaction, 2-acetylthiazole, formation pathway, glyoxal, d-glucose, l-cysteine, Food and Feed Chemistry: Analysis and other aspects.COA of Formula: C5H5NOS

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

On December 31, 2022, Wang, Haili; Yang, Ping; Liu, Chen; Song, Huanlu; Pan, Wenqing; Gong, Lin published an article.Application of 24295-03-2 The title of the article was Characterization of key odor-active compounds in thermal reaction beef flavoring by SGCxGC-O-MS, AEDA, DHDA, OAV and quantitative measurements. And the article contained the following:

Thermal reaction beef flavoring is a kind of food additive. In this study, three extraction methods of dynamic headspace sampling (DHS), solid phase micro-extraction (SPME) and liquid-liquid extraction (LLE) combined with switchable two-dimensional gas chromatog.-olfactometry-mass spectrometry (SGCxGC-O-MS) were employed to characterize volatile compounds in thermal reaction beef flavoring. The odor characteristics of thermal reaction beef flavors were identified by sensory evaluation, aroma extraction dilution anal. (AEDA), dynamic headspace dilution anal. (DHDA), odor activity value (OAV) and quant. measurements. A total of 231 volatile odor compounds were identified by the three extraction methods, which including 15 aldehydes, 41 ketones, 29 alcs., 27 esters, 13 furans, 20 pyrazines, 9 sulfur-containing compounds, 18 thiophenes and thiazoles, 19 acids and 40 other compounds Ninety-eight compounds had odor activity, and 22 odor-active compounds were quant. analyzed. 2-Methyl-3-furanthiol (meaty) and bis(2-methyl-3-furanyl) disulfide (onion) had the higher FD and OAV, 3-methylbutanal (chocolate) was first identified as the key odor-active compound in thermal reaction beef flavoring, Me furfuryl disulfide (meaty), 2-ethyl-3,5-dimethylpyrazine (roasted nuts), 2,3-butanedione (caramel), linalool (floral), furfural (baked bread), 2-furfurylthiol (sulfury) and other compounds were also identified as the key aroma components in thermal reaction beef flavoring. The results showed that SPME and DHS were more suitable than LLE for the separation and extraction of volatile odor compounds in thermal reaction beef flavoring, and there were some masking and synergistic effects between odor-active compounds The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Application of 24295-03-2

The Article related to furanthiol methylbutanal beef flavoring extraction mass spectrometry gas chromatog, Food and Feed Chemistry: Analysis and other aspects.Application of 24295-03-2

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

On November 30, 2020, Kaneko, Shu; Kumazawa, Kenji published an article.COA of Formula: C5H5NOS The title of the article was Comparative aroma extract dilution analysis of changes in aroma components of seasoned soy sauce prepared from soy sauce and mirin during heating. And the article contained the following:

An investigation using Aroma Extract Dilution Anal. (AEDA) applied to the aroma concentrate of a model heated seasoned soy sauce, prepared from soy sauce and mirin, revealed 36 aroma peaks, and 32 compounds were identified or tentatively identified from the detected peaks. Among them, 3-(methylthio) propanal was the most dominant compound, showing the highest Flavor Dilution (FD) factor, followed by 4-hydroxy-2,5-dimethyl-3(2)-furanone, 5(or 2)-ethyl-4-hydroxy-2(or 5)-methyl-3(2)-furanone, and 3-hydroxy-4,5-dimethyl-2(5)-furanone. While most of the identified compounds have already been reported, 2,3-dihydro-5-hydroxy-6-methyl-4(4)-pyranone was identified in the seasoned soy sauce for the first time. A comparative AEDA study of the unheated and heated seasoned soy sauces revealed that approx. half of the aroma peaks were detected at FD factors that were 16-fold higher in the heated seasoned soy sauce, while the remainder showed equal or highly similar FD factors. This indicated that the heating history of the seasoned soy sauce as well as the materials employed are important in the aroma of heated seasoned soy sauce, and a limited number of aroma components are related to changes in the seasoned soy sauce aroma by heating. Finally, relative quant. anal. of aroma active compounds, i.e., Strecker aldehydes, furanone/pyranones, and phenols, in the seasoned soy sauce heated for different times revealed that only a few components greatly increased during heating and these might be important for the changes in the seasoned soy sauce aromas with different heating times. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).COA of Formula: C5H5NOS

The Article related to extract aroma component seasoned soy sauce mirin heating, real quant analysis, Food and Feed Chemistry: Analysis and other aspects.COA of Formula: C5H5NOS

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

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

On March 20, 2003, Deghati, Paymaneh Y. F.; Borghini, Alice; Van Den Nieuwendijk, Adrianus M. C. H.; Dissen-de Groote, Miriam; IJzerman, Adriaan P. published an article.Recommanded Product: 19989-66-3 The title of the article was Inhibition of nucleoside transport By new analogues of nitrobenzylthioinosine. And the article contained the following:

Nitrobenzylthioinosine (NBTI, 1) was systematically modified by attachment of substituents at positions C6 and N9, and also by substitution of N1 with C. These modifications were chosen to reduce the polarity of the new compounds Incorporation of the nitro functionality into a benzoxadiazole ring system was considered first. These new nucleosides showed high affinity (1.5-10 nM) towards the nucleoside transport protein as present on human erythrocyte ghosts. Next, modification of this benzoxadiazole ring system with C, S and O in different positions produced a number of less polar nucleosides with affinity in the higher nanomolar range. Modification of N9 was achieved with different alkyl and alc. substituents. An Bu substituent proved best, although all variations yielded substantial decreases in affinity. Replacement of N1 by a carbon atom in combination with a 2-Cl substituent also resulted in a relatively potent NBTI derivative (47 nM). 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 nitrobenzylthioinosine analog preparation structure activity nucleoside transport protein, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 19989-66-3

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

Hawas, Samia S.; El-Gohary, Nadia S.; Gabr, Moustafa T.; Shaaban, Mona I.; El-Ashmawy, Mahmoud B. published an article in 2019, the title of the article was Synthesis, molecular docking, antimicrobial, antiquorum-sensing and antiproliferative activities of new series of pyrazolo[3,4-b]pyridine analogs.Name: 4-Phenylthiazol-2-amine And the article contains the following content:

New series of pyrazolo[3,4-b]pyridines were prepared and evaluated for antimicrobial activity toward six selected microorganisms. Compounds and exhibited good activity toward Bacillus cereus. On the other hand, and evinced interesting activity over Candida albicans, whereas and displayed promising activity over Aspergillus fumigatus. Antiquorum-sensing effectiveness of the new members over Chromobacterium violaceum was also assessed, where compounds and exhibited higher activity than that of the reference compound, indole. In vitro antiproliferative assessment toward HepG2, HCT-116 and MCF-7 cancer cells evidenced that has notable effectiveness on all examined cell lines, whereas were active but to a lower extent. In vivo antitumor activity of and against EAC cells was also esteemed, where and showed considerable activity comparable to that of doxorubicin. Cytotoxicity screening over WI38 and WISH normal cells evinced that and are less cytotoxic than doxorubicin. Compounds and were evaluated for DNA-binding affinity and topoisomerase IIβ inhibitory activity. Analogs and illustrated strong DNA-binding affinity, whereas and exhibited interesting topoisomerase IIβ inhibitory activity. Compounds and were docked into topoisomerase IIβ, where showed preferential binding to topoisomerase IIβ. Computational studies articulated that the new members are in compliance with Veber’s standards and Lipinski’s rule. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine

The Article related to pyrazolo pyridine analog preparation antimicrobial antiquorum cancer topoisomerase, Pharmacology: Structure-Activity and other aspects.Name: 4-Phenylthiazol-2-amine

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

On May 25, 2019, Jalal, Mahir A.; TAlmalki, Ziyad; Radhi, Wisam A. published an article.SDS of cas: 2010-06-2 The title of the article was Quantitative structure-activity relationship studies of amino acids conjugated 2-amnio-arylthiazole as antifungal. And the article contained the following:

Thiazole derivatives as fungi-inhibitors belonging to 16 amino acids conjugated 2- amnio-arylthiazole was subjected computationally to quant. structure-activity relationship (QSAR) anal. by optimization of chem. structures at min. energy using mol. mechanics (MM+) theory and the semi-empirical MO (AM1) method. Correlation of their exptl. inhibitory zones against three types of fungi, namely, Fusarium monoliforme, Aspergillus Flavus, and Aspergillus niger with obtained physiochem. parameters was carried out using multiple linear regression (MLR) anal. As a result, there excellent out of 12 models were correlated with numerous descriptors having correlation coefficient rang (0.967-0.843). discriminant models were selected depending on their correlation coefficients (R2), Fisher ratios (F), and standard errors (S). These QSAR results and the probable pharmacophore features identified in this study offer important structural insight into designing novel amino acids conjugated 2-amnio-arylthiazole. Other 15 thiazole derivatives was proposed and it found that they are in good inhibitory zones. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).SDS of cas: 2010-06-2

The Article related to amino acid arylthiazole antifungal quant structure activity relationship analysis, Pharmacology: Structure-Activity and other aspects.SDS of cas: 2010-06-2

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

On October 14, 2021, Lee, Kun-Hung; Yen, Wan-Ching; Lin, Wen-Hsing; Wang, Pei-Chen; Lai, You-Liang; Su, Yu-Chieh; Chang, Chun-Yu; Wu, Cai-Syuan; Huang, Yu-Chen; Yang, Chen-Ming; Chou, Ling-Hui; Yeh, Teng-Kuang; Chen, Chiung-Tong; Shih, Chuan; Hsieh, Hsing-Pang published an article.Category: thiazole The title of the article was Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model. And the article contained the following:

Colony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven optimization of BPR1K871 (9), our clin. multitargeting kinase inhibitor. Mol. docking revealed an addnl. nonclassical hydrogen-bonding (NCHB) interaction between the unique 7-aminoquinazoline scaffold and the CSF1R hinge region, contributing to CSF1R potency enhancement. Structural studies of CSF1R and Aurora kinase B (AURB) demonstrated the differences in their back pockets, which inspired the use of a chain extension strategy to diminish the AURA/B activities. A lead compound BPR1R024 (12) exhibited potent CSF1R activity (IC50 = 0.53 nM) and specifically inhibited protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. In vivo, oral administration of 12 mesylate delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Category: thiazole

The Article related to quinazoline derivative preparation oral csf1r inhibitor antitumor immunomodulator, Pharmacology: Structure-Activity and other aspects.Category: thiazole

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