Tag: 100-200

On July 1, 2020, Amorim, Carina R.; Pavani, Thais F. A.; Lopes, Andrey F. S.; Duque, Marcelo D.; Mengarda, Ana C. A.; Silva, Marcos P.; de Moraes, Josue; Rando, Daniela G. G. published an article.Name: 4-Phenylthiazol-2-amine The title of the article was Schiff bases of 4-Phenyl-2-Aminothiazoles as hits to new antischistosomals: Synthesis, in-vitro, in-vivo and in-silico studies. And the article contained the following:

The synthesis of seventeen Schiff bases of 4-(4-Substituted phenyl)-N-(4-substituted benzylidene)thiazole-2-amines I [X = S, CH=CH; Z =H, O2N; R = H, 4-Me, 4-Et] which were tested in-vitro and in-vivo against Schistosoma mansoni adult worms. Moreover, in-silico studies to propose potential macromol. targets and to predict the oral bioavailability were also performed. The analog I [X = S; Z = O2N; R = H] exhibited the best in-vitro performance (IC50: 29.4μM, SI:6.1) associated with promising in-vivo activity, with a significant decrease in the adult life forms and oviposition. Oral bioavailability was impaired by the predicted low water solubility of I [X = S; Z = O2N; R = H] although it also exhibited good membrane permeability. The water solubility, however, was improved by decreasing the particles size. Serine/Threonine- and Tyrosine Kinases, Carbonic Anhydrase, Tyrosine Phosphatase and Arginase were predicted as potential macromol. targets through which the I [X = S; Z = O2N; R = H] was acting against the helminth. This class of compounds I exhibited an interesting initial therapeutic profile with the advantage of being chem. diverse from the PZQ and be easily synthesized from com. reagents which could lead to low-cost drugs. These aspects make this class of compounds I interesting hits to be explored against schistosomiasis. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine

The Article related to phenyl aminothiazole diastereoselective preparation antischistosomal agent mol modeling, 4-phenyl-2-aminothiazoles, antischistosomal, schiff bases, schistosoma mansoni, target fishing and other aspects.Name: 4-Phenylthiazol-2-amine

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

On June 30, 2019, Abo-Ashour, Mahmoud F.; Eldehna, Wagdy M.; Nocentini, Alessio; Ibrahim, Hany S.; Bua, Silvia; Abdel-Aziz, Hatem A.; Abou-Seri, Sahar M.; Supuran, Claudiu T. published an article.Synthetic Route of 2010-06-2 The title of the article was Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies. And the article contained the following:

In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogs (11a-d, 12a-d, 16a-c and 17a-d). A bioisosteric replacement approach was adopted to replace the 4-fluorophenyl tail of SLC-0111 with thiazole and thiadiazole ones, which were thereafter extended with lipophilic un/substituted Ph moieties. All the newly synthesized SLC-0111 analogs were evaluated in vitro for their inhibitory activity towards a panel of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms (hCA I, II, IX and XII), using a stopped-flow CO2 hydrase assay. All the examined isoforms were inhibited by the primary sulfonamide derivatives (11a-d and 12a-d) in variable degrees with the following KI ranges: 162.6-7136 nM for hCA I, 9.0-833.6 nM for hCA II, 7.9-153.0 nM for hCA IX, and 9.4-94.0 nM for hCA XII. In particular, compounds 12b and 12d displayed 5.5-fold more potent inhibitory activity (KIs = 8.3 and 7.9 nM, resp.) than SLC-0111 (KI = 45 nM) towards hCA IX. Mol. docking study was carried out for 12d within the hCA IX (PDB 3IAI) active site, to justify its inhibitory activity. 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 carbonic anhydrase inhibitors mol docking slc0111 analogs, carbonic anhydrase inhibitors, molecular docking, slc-0111 analogues, thiazoles and thiadiazoles, ureido-benzenesulfonamide and other aspects.Synthetic Route of 2010-06-2

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

On December 31, 2019, Kizimova, I. A.; Igidov, N. M.; Dmitriev, M. V.; Chashchina, S. V.; Makhmudov, R. R.; Siutkina, A. I. published an article.Application In Synthesis of 4-Phenylthiazol-2-amine The title of the article was Synthesis, Structure, and Biological Activity of 4-R-4-Oxo-2-[2-(phenylamino)benzoyl]hydrazinylidene-N-hetarylbutanamides. And the article contained the following:

Decyclization of N’-[5-R-2-oxofuran-3(2H)-ylidene]-2-(phenylamino)benzohydrazides I (R = Ph, t-Bu, 4-chlorophenyl, etc.) under the action of heterocyclic amines R1NH2 (R1 = thiazol-2-yl, 1,3,4-thiadiazol-2-yl, 4-phenylthiazol-2-yl, etc.) leads to the formation of N-hetaryl-4-R-4-oxo-2-[2-(phenylamino)benzoyl]hydrazinylidenebutanamides II and in some cases ring-chain tautomers. Antinociceptive and anti-inflammatory activities of the obtained compounds were studied. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application In Synthesis of 4-Phenylthiazol-2-amine

The Article related to hetaryl oxo phenylamino benzoyl hydrazinylidene butanamide preparation antinociceptive antiinflammatory, oxofuranylidene phenylamino benzohydrazide heterocyclic amine decyclization and other aspects.Application In Synthesis of 4-Phenylthiazol-2-amine

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

On June 18, 2009, Ellman, Jonathan A.; Brak, Katrien published a patent.Related Products of 19989-66-3 The title of the patent was Triazole derivatives and aminocoumarin derivatives as nonpeptidic inhibitors of cruzain and their preparation and use in the treatment of Chagas disease. And the patent contained the following:

Cruzain is the major cysteine protease of T. cruzi, which is the causative agent of Chagas’ disease and is a promising target for the development of chemotherapy. With the goal of developing potent nonpeptidic inhibitors of cruzain, of formula I, the substrate activity screening method was used to screen a library of protease substrates initially designed to target the homologous human protease cathepsin S. Structure-based design was next used to further improve substrate cleavage efficiency by introducing addnl. binding interactions in the S3 pocket of cruzain. Substrates of formula I wherein R1 is H, OH and derivatives, NH2 and derivatives, SH and derivatives, SOH and derivatives, SO2H and derivatives, SO2NH2 and derivatives, NO2, halo, CN, (un)substituted (hetero)alkyl, etc.; are claimed. The optimized substrates were then converted to inhibitors by the introduction of cysteine protease mechanism-based pharmacophores. Inhibitors II and III were prepared by multistep procedures (procedures given). Inhibitor II was determined to be reversible even though it incorporated the vinyl sulfone pharmacophore that is well documented to give irreversible cruzain inhibition for peptidic inhibitors. The previously unexplored β-chloro vinyl sulfone pharmacophore provided mechanistic insight that led to the development of potent irreversible acyl- and aryl- oxymethyl ketone cruzain inhibitors. For these inhibitors, potency did not solely depend on leaving group pTa, with 2,3,5,6-tetrafluorophenoxy Me ketone III identified as one of the most potent inhibitors with a second order inactivation constant of 147,000 s-1M-1. This inhibitor completely eradicated the T. cruzi parasite from mammalian cell cultures and consequently has the potential to lead to new chemo therapeutics for Chagas’ disease. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Related Products of 19989-66-3

The Article related to triazole derivative preparation nonpeptidic cruzain inhibitor treatment chagas disease, aminocoumarin derivative preparation nonpeptidic cruzain inhibitor treatment chagas disease and other aspects.Related Products of 19989-66-3

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

Gaddam, Lakshmi Teja; Thata, Sreenivasulu; Adivireddy, Padmaja; Venkatapuram, Padmavathi published an article in 2019, the title of the article was Synthesis of carboxamide and sulfonyl carboxamide linked heterocycles under green conditions.HPLC of Formula: 2010-06-2 And the article contains the following content:

Direct coupling of heteroaldehydes RCHO (R = furan-2-yl, pyridin-4-yl, 2,4-dichloro-1,3-oxazol-5-yl, etc.) with heteroaryl amines R1NH2 (R1 = 4-phenyl-1H-imidazol-2-yl, 4-phenyl-1,3-thiazol-2-yl)/sulfonylamine N-(5-(aminosulfonyl)-4-phenyl-1H-imidazol-2-yl)benzamide is performed under green conditions using PEG-400 in the presence of oxidant CCl3CN/H2O2. The presence of electron withdrawing substituents on heteroaldehydes increased the yield. Further heteroaryl amines favor the reaction when compared with heteroaryl sulfonylamines. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).HPLC of Formula: 2010-06-2

The Article related to carboxamide preparation green chem, heteroaldehyde heteroaryl amine coupling reaction, sulfonyl carboxamide preparation green chem, sulfonylamine heteroaldehyde coupling reaction and other aspects.HPLC of Formula: 2010-06-2

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

On February 23, 2006, Blake, James F.; Fell, Jay Bradford; Fischer, John P.; Hendricks, Robert Than; Robinson, John E.; Spencer, Stacey Renee; Stengel, Peter J. published a patent.Recommanded Product: Benzo[d]thiazol-6-ylmethanol The title of the patent was Preparation of benzothiazine dioxides as antivirals.. And the patent contained the following:

Title compounds [I; R1 = OH, halo, NO2, cyano, alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, (substituted) Ph, phenylalkyl, PhO, etc.; R6 = H, alkyl; A = specified hydroxyquinolone, hydroxypyrazolone, hydroxypyrrolone, hydroxypyridone, etc. residues], were prepared as hepatitis C virus NS5B RNA polymerase inhibitors (no data). Thus, title compound (II) was prepared in 5 steps from 2-aminothiophenol, Et 4-chloroacetoacetate, and 1-isoamylisatoic anhydride. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Recommanded Product: Benzo[d]thiazol-6-ylmethanol

The Article related to benzothiazine dioxide preparation antiviral, hcv infection treatment benzothiazine dioxide preparation, hepatitis c virus polymerase inhibitor benzothiazine dioxide preparation and other aspects.Recommanded Product: Benzo[d]thiazol-6-ylmethanol

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

Wei, Meng; Liu, Xiaochang; Xie, Peng; Lei, Yuanhua; Yu, Haojie; Han, Aiyun; Xie, Libin; Jia, Hongliang; Lin, Shaohua; Bai, Yueyu; Sun, Baozhong; Zhang, Songshan published an article in 2022, the title of the article was Characterization of Volatile Profiles and Correlated Contributing Compounds in Pan-Fried Steaks from Different Chinese Yellow Cattle Breeds through GC-Q-Orbitrap, E-Nose, and Sensory Evaluation.Category: thiazole And the article contains the following content:

This study focused on characterizing the volatile profiles and contributing compounds in pan-fried steaks from different Chinese yellow cattle breeds. The volatile organic compounds (VOCs) of six Chinese yellow cattle breeds (bohai, jiaxian, yiling, wenshan, xinjiang, and pingliang) were analyzed by GC-Q-Orbitrap spectrometry and electronic nose (E-nose). Multivariate statistical anal. was performed to identify the differences in VOCs profiles among breeds. The relationship between odor-active volatiles and sensory evaluation was analyzed by partial least square regression (PLSR) to identify contributing volatiles in pan-fried steaks of Chinese yellow cattle. The results showed that samples were divided into two groups, and 18 VOCs were selected as potential markers for the differentiation of the two groups by GC-Q-Orbitrap combined multivariate statistical anal. YL and WS were in one group comprising mainly aliphatic compounds, while the rest were in the other group with more cyclic compounds Steaks from different breeds were better differentiated by GC-Q-Orbitrap in combination with chemometrics than by E-nose. Six highly predictive compounds were selected, including 3-methyl-butanal, benzeneacetaldehyde, 2-ethyl-6-methyl-pyrazine, 2-acetylpyrrole, 2-acetylthiazole, and 2-acetyl-2-thiazoline. Sensory recombination difference and preference testing revealed that the addition of highly predictive compounds induced a perceptible difference to panelists. This study provides valuable data to characterize and discriminate the flavor profiles in pan-fried steaks of Chinese yellow cattle. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Category: thiazole

The Article related to benzeneacetaldehyde panfried steak gc qorbitrap, chinese yellow cattle, e-nose, gc-q-orbitrap, multivariate statistical analysis, sensory evaluation, volatile organic compounds and other aspects.Category: thiazole

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

On January 27, 1998, Iwasaki, Fumiaki; Miharu, Michiko published a patent.SDS of cas: 64987-16-2 The title of the patent was Preparation of 2-aminothiazoleacetic acids as intermediates for cephem antibiotics.. And the patent contained the following:

Title compounds I (R1 = H; X = two H, O, NOR2; R2 = H, alkyl, OH-protecting group; R3 = NH2-protecting group) are prepared by reaction of heterocycles I (R3 = H; R1 = CO2H-protecting group; X, R2, = same as above) with NH2-protecting agents in organic solvents incompatible with H2O, saponification of thiazoles I (R1 = CO2H-protecting group; R3 = NH2-protecting group; R2, X = same as above) (II) with basic aqueous solution, dissolution of II alkali metal salts in basic aqueous solution, neutralizing them with acids, and isolation. I (R3 = H, X = two H, R1 = Et) was treated with (t-BuO)2CO in PhMe in the presence of 4-N,N-dimethylaminopyridine at 50° for 7 h, saponified with NaOH in H2O at 20° for 1 h, and neutralized with HCl in H2O at ≤20° to give 82.5% I (R1 = H, X = two H, R3 = t-BuO2C). 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 amino protecting agent condensation thiazoleacetate, thiazoleacetate saponification base aqueous solution, aminothiazoleacetic acid preparation cephem antibiotic intermediate and other aspects.SDS of cas: 64987-16-2

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S.; Salzmann, Thomas; Armistead, David published a patent.Computed Properties of 64987-16-2 The title of the patent was Preparation of benzothiazoles and thiazolopyridines as sirtuin modulators. And the patent contained the following:

The title compounds I [X7-X10 = N, CR20 or CR11 (wherein R20 = H or solubilizing group; R11 = H, (un)substituted alkyl); R19 = phenylene, pyridylene, etc.; R21 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R31 = (un)substituted monocyclic or bicyclic (hetero)aryl; with proviso] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a multi-step synthesis of II, starting from 4-aminopyridin-3-yl diisopropylcarbamodithioate and 3-nitrobenzoyl chloride, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Computed Properties of 64987-16-2

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, benzothiazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.Computed Properties of 64987-16-2

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

On October 15, 2020, Mourad, Ahmed A. E.; Mourad, Mai A. E. published an article.Category: thiazole The title of the article was Enhancing insulin sensitivity by dual PPARγ partial agonist, β-catenin inhibitor: Design, synthesis of new α-phthalimido-o-toluoyl-2-aminothiazole hybrids. And the article contained the following:

We aimed at synthesizing novel partial PPARγ agonists with β-catenin inhibitory activity which was enhanced insulin sensitivity and avoid the side effects of full PPARγ agonists. We synthesized novel series of α-phthlimido-o-toluoyl-2-aminothiazoles I [R1=R2=R3=R4 = H; R2 = H, Me, MeO, Cl, etc.] hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids I on PPARγ activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBPα, PPARγ and PPARγ targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPARγ and β-catenin protein levels were evaluated in 3T3-L1cells. In addition, mol. docking studies with PPARγ LBD, physicochem. properties and structure activity relationship of the novel hybrids I were also studied. Three of the synthesized hybrids I showed partial PPARγ agonistic activity and distinct PPARγ binding pattern. These compounds I modulated PPARγ gene expression and PPARγ target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds I reduced β-catenin protein level which reflected in increased both PPARγ gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. This synthesized compounds act as novel partial PPARγ agonists and β-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to dioxoisoindolinylmethyl phenylthiazolyl benzamide preparation peroxisome proliferator activated receptor agonist, 2-aminothiazole, partial pparγ agonist, thiazolidinediones, wnt/β-catenin inhibitor, α-phthlimido-o-toluoyl and other aspects.Category: thiazole

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