Category: 2010-06-2

On April 30, 2019, Gong, Weinan; Xu, Bin; Yin, Xiaoshuang; Liu, Ying; Chen, Yun; Yang, Wenzhong published an article.Computed Properties of 2010-06-2 The title of the article was Halogen-substituted thiazole derivatives as corrosion inhibitors for mild steel in 0.5 M sulfuric acid at high temperature. And the article contained the following:

The inhibitory effects of three halogen-substituted thiazole derivatives named 2-amino-4-(4-fluorophenyl)-thiazole (FPT), 2-amino-4-(4-chlorophenyl)-thiazole (CPT) and 2-amino-(4-bromophenyl)-thiazole (BPT) on mild steel corrosion were investigated in 0.5 M H2SO4 from 30°C to 60°C. Electrochem. measurements demonstrated that these thiazoles can effectively inhibit the corrosion of mild steel in 0.5 M H2SO4 solution at 30°C. With the increase of temperature, the inhibition efficiency (η) of FPT at 60°C reduced to 22.62% while those of CPT and BPT under the same temperature were nearly unchanged, which were as high as 95.16% and 95.45%, resp. The adsorptions of three thiazoles on the surface of mild steel were all found to adhere to Langmuir adsorption isotherm at 30°C while only CPT and BPT obeyed at 60°C. Quantum calculations results indicated that CPT and BPT had the better adsorption ability on mild steel than FPT. Mol. dynamic stimulations were taken out to investigate the adsorption configurations of three thiazoles on the surface of Fe (0 0 1) at 30°C and 60°C, and the results implied that the binding energy of protonated BPT and CPT were nearly unchanged at studied temperatures while that of protonated FPT apparently became lower at 60°C. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Computed Properties of 2010-06-2

The Article related to halogen substituted thiazole derivative corrosion inhibitor mild steel temperature, Ferrous Metals and Alloys: Corrosion (If The Primary Interest Is In The Metal), Erosion, Cavitation, Tribology, and Oxidation and other aspects.Computed Properties of 2010-06-2

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

Abdallah, Amira E. M.; Mohareb, Rafat M.; Helal, Maher H. E.; Mofeed, Germeen J. published an article in 2021, the title of the article was Synthesis and anticancer evaluations of novel thiazole derivatives derived from 4-phenylthiazol-2-amine.Application of 2010-06-2 And the article contains the following content:

Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chem. reagents was studied. The structure of the newly synthesized compounds was established based on elemental anal. and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds displayed higher efficiency than the reference doxorubicin. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application of 2010-06-2

The Article related to heteroaryl thiozole preparation antitumor cytotoxicity structure activity relationship, thiazolopyrimidine preparation antitumor cytotoxicity structure activity relationship and other aspects.Application of 2010-06-2

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

On January 1, 2019, Chen, Lingfeng; Chen, Hongjin; Chen, Pengqin; Zhang, Wenxin; Wu, Chao; Sun, Chuchu; Luo, Wu; Zheng, Lulu; Liu, Zhiguo; Liang, Guang published an article.HPLC of Formula: 2010-06-2 The title of the article was Development of 2-amino-4-phenylthiazole analogues to disrupt myeloid differentiation factor 88 and prevent inflammatory responses in acute lung injury. And the article contained the following:

The synthesis of 47 new analogs by modifying different sites on this lead compound and assessed their anti-inflammatory activities in lipopolysaccharide-induced mouse primary peritoneal macrophages (MPMs) was described. The most promising compound I was found to effectively interact with MyD88 protein and prevented formation of the MyD88 homodimeric complex. Furthermore, compound I showed in-vivo anti-inflammatory activity in LPS-caused model of acute lung injury. This work provided new candidates as MyD88 inhibitors to combat inflammation diseases. 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 piperazinyl phenylthiazolylpropanamide preparation myd88 protein homodimerization inhibitor antiinflammatory, 2-amino-4-phenylthiazole, acute lung injury, anti-inflammation, macrophages, myd88 and other aspects.HPLC of Formula: 2010-06-2

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

On June 15, 2021, Hassan, Abdelfattah; Badr, Mohamed; Hassan, Heba A.; Abdelhamid, Dalia; Abuo-Rahma, Gamal El-Din A. published an article.Category: thiazole The title of the article was Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition. And the article contained the following:

A new series of 2-(4-(2-oxo-1,2-dihydroquinolin-4-yl)piperazin-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives were synthesized and evaluated for anticancer activity. All target compounds showed anticancer activity higher than that of their 2-oxo-4-piperazinyl-1,2-dihydroquinolin-2(1H)-one precursors. Multidose testing of target compounds was performed against breast cancer T-47D cell line. Five compounds showed higher cytotoxic activity than Staurosporine. The dihalogenated derivative showed the best cytotoxic activity with IC50 2.73 +/= 0.16μM. In addition, the VEGFR-2 inhibitory activity of all synthetic compounds was evaluated. Two compounds of 6-fluoro-4-(piperazin-1-yl)quinolin-2(1H)-ones showed inhibitory activity comparable to sorafenib with IC50 46.83 +/= 2.4, 51.09 +/= 2.6 and 51.41 +/= 2.3 nM, resp. The cell cycle anal. of two compounds namely, 2-(4-(6-fluoro-2-oxo-1,2-dihydroquinolin-4-yl)piperazin-1-yl)-N-(4-phenylthiazol-2-yl)acetamide and N-(4-(4-chlorophenyl)thiazol-2-yl)-2-(4-(2-oxo-1-phenyl-1,2-dihydroquinolin-4-yl)piperazin-1-yl)acetamide revealed that the arrest of cell cycle occurred at S phase. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to piperazinylquinolinone thiazole preparation docking anticancer vegfr 2 inhibition human, 4-phenylthiazole, 4-piperazinylquinolin‐2(1h)-one, angiogenesis, breast cancer, vegfr‐2 inhibitors and other aspects.Category: thiazole

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

Vibhute, Prashant K.; Aghao, Arvind K.; Jadhav, Satish B.; Dawane, Bhaskar S. published an article in 2021, the title of the article was Design, synthesis and characterization of some novel thiazole and quinoline containing schiff bases and evaluation of their in-vitro anti-inflammatory and antimicrobial activity.Category: thiazole And the article contains the following content:

A novel and eco-friendly series of quinoline based Schiff bases I [R = H, 4-Cl, 4-Br, etc.] in PEG-400 were synthesized. It contd. two pharmacol. active nucleus i.e. 8-hydroxyquinoline and 4-substituted phenylthiazole. The targeted compounds were obtained in good yield by reacting 2-amino-4-substituted phenylthiazole with 8-hydroxyquinoline-2-carbaldehyde which was obtained by oxidative product of 8-hydroxy-2-Me quinoline. The mol. structures of the synthesized compounds I were confirmed by physicochem. properties and spectral characteristics (IR, NMR, elemental anal. and Mass spectra). The synthesized compounds I were screened for the in-vitro anti-inflammatory and antimicrobial activity. Thiazole quinoline Schiff base could be a promising mol. in developing area of antimicrobial agents for modern pharmacologists and chemists. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to hydroxyquinoline carbaldehyde phenylthiazole diastereoselective schiff imination green chem, phenylthiazolyliminomethyl quinolinol preparation antiinflammatory antibacterial antifungal and other aspects.Category: thiazole

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

On December 31, 2021, Lemilemu, Fitsum; Bitew, Mamaru; Demissie, Taye B.; Eswaramoorthy, Rajalakshmanan; Endale, Milkyas published an article.HPLC of Formula: 2010-06-2 The title of the article was Synthesis, antibacterial and antioxidant activities of Thiazole-based Schiff base derivatives: a combined experimental and computational study. And the article contained the following:

Thiazole-based Schiff base compounds display significant pharmacol. potential with an ability to modulate the activity of many enzymes involved in metabolism They also demonstrated to have antibacterial, antifungal, anti-inflammatory, antioxidant, and antiproliferative activities. In this work, conventional and green approaches using ZnO nanoparticles as catalyst were used to synthesize thiazole-based Schiff base compounds Among the synthesized compounds, 11 showed good activities towards Gram-neg. E. coli (14.40 ± 0.04), and Gram-pos. S. aureus (15.00 ± 0.01 mm), resp., at 200 μg/mL compared to amoxicillin (18.00 ± 0.01 mm and 17.00 ± 0.04). Compounds 7 and 9 displayed better DPPH radical scavenging potency with IC50 values of 3.6 and 3.65 μg/mL, resp., compared to ascorbic acid (3.91 μg/mL). The binding affinity of the synthesized compounds against DNA gyrase B is within – 7.5 to – 6.0 kcal/mol, compared to amoxicillin (- 6.1 kcal/mol). The highest binding affinity was achieved for compounds 9 and 11 (- 6.9, and – 7.5 kcal/mol, resp.). Compounds 7 and 9 displayed the binding affinity values of – 5.3 to – 5.2 kcal/mol, resp., against human peroxiredoxin 5. These values are higher than that of ascorbic acid (- 4.9 kcal/mol), in good agreement with the exptl. findings. In silico cytotoxicity predictions showed that the synthesized compounds LD (LD50) value are class three (50 ≤ LD50 ≤ 300), indicating that the compounds could be categorized under toxic class. D. functional theory calculations showed that the synthesized compounds have small band gap energies ranging from 1.795 to 2.242 eV, demonstrating that the compounds have good reactivities. The synthesized compounds showed moderate to high antibacterial and antioxidant activities. The in vitro antibacterial activity and mol. docking anal. showed that compound 11 is a promising antibacterial therapeutics agent against E. coli, whereas compounds 7 and 9 were found to be promising antioxidant agents. Moreover, the green synthesis approach using ZnO nanoparticles as catalyst was found to be a very efficient method to synthesize biol. active compounds compared to the conventional method. 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 thiazole schiff base derivative antibacterial antioxidant activity computational biol, antibacterial, antioxidant, dft analysis, drug likeness, molecular docking, schiff base, thiazole and other aspects.HPLC of Formula: 2010-06-2

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

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

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