Category: 2010-06-2

On September 1, 2019, Sami, Yuichi; Morita, Masataka; Kubota, Hirokazu; Hirabayashi, Ryoji; Seo, Ryushi; Nakagawa, Nobuaki published an article.Synthetic Route of 2010-06-2 The title of the article was Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit. And the article contained the following:

Novel oral TRPV4 inhibitors were prepared and their potential for pain management in osteoarthritis discussed. 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 oral trpv4 inhibitor preparation analgesic osteoarthritis, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 2010-06-2

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

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

Manwatkar, H. P.; Gedam, S. D.; Bhaskar, C. S.; Dhonde, M. G.; Thakare, Sanjay R. published an article in 2020, the title of the article was Synthesis and properties of amino and thiol functionalized graphene oxide.Application of 2010-06-2 And the article contains the following content:

Graphite, an allotrope of carbon, has been extensively researched in varied fields of science due to its typical structure and properties. Many researchers have transformed graphene from graphite in many ways. Functionalized graphene have immense importance because of advancement of properties for technol. applications. =N- and -S- fabricated graphene oxide composite was prepared The amino and thiol functionalized graphene oxide with improved properties is expected to adsorb heavy and toxic metals like Pb, Cd, Hg, and Ag from aqueous solutions The synthesized composite was confirmed and characterized by various characterization techniques like FTIR, SEM, TEM and XRD. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Application of 2010-06-2

The Article related to graphene oxide amino phenylthiazole, Surface Chemistry and Colloids: Other and other aspects.Application of 2010-06-2

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

On December 23, 2021, Come, Jon H.; Senter, Timothy J.; Clark, Michael P.; Court, John J.; Gale-Day, Zachary; Gu, Wenxin; Krueger, Elaine; Liang, Jianglin; Morris, Mark; Nanthakumar, Suganthini; O′Dowd, Hardwin; Maltais, Francois; Iyer, Ganesh; Andreassi, John; Boucher, Christina; Considine, Tony; Moody, Cameron S.; Taylor, William; Mohanty, Arun K.; Huang, Yulin; Zuccola, Harmon; Coll, Joyce; Bonanno, Kenneth C.; Gagnon, Kevin J.; Gan, Lu; Lu, Fan; Gao, Hong; Chakilam, Ananthisrinivas; Engtrakul, Juntyma; Song, Bin; Crawford, Dan; Doyle, Elisabeth; Kramer, Tal; Vought, Bryan; Phillips, Jonathan; Kemper, Raymond; Sanders, Martin; Swett, Rebecca; Furey, Brinley; Winquist, Ray; Bunnage, Mark E.; Jackson, Katrina L.; Charifson, Paul S.; Magavi, Sanjay S. published an article.Category: thiazole The title of the article was Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1. And the article contained the following:

Accumulation of very long chain fatty acids (VLCFAs) due to defects in ATP binding cassette protein D1 (ABCD1) is thought to underlie the pathologies observed in adrenoleukodystrophy (ALD). Pursuing a substrate reduction approach based on the inhibition of elongation of very long chain fatty acid 1 enzyme (ELOVL1), we explored a series of thiazole amides that evolved into compound 27-a highly potent, central nervous system (CNS)-penetrant compound with favorable in vivo pharmacokinetics. Compound 27 (I) selectively inhibits ELOVL1, reducing C26:0 VLCFA synthesis in ALD patient fibroblasts, lymphocytes, and microglia. In mouse models of ALD, compound 27 treatment reduced C26:0 VLCFA concentrations to near-wild-type levels in blood and up to 65% in the brain, a disease-relevant tissue. Preclin. safety findings in the skin, eye, and CNS precluded progression; the origin and relevance of these findings require further study. ELOVL1 inhibition is an effective approach for normalizing VLCFAs in models of ALD. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole

The Article related to elovl1 inhibitor vlcfa adrenoleukodystrophy, Placeholder for records without volume info and other aspects.Category: thiazole

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

Nizamuddin, Nd; Abdul ahad, Hindustan; Devanna, Nayakanti published an article in 2020, the title of the article was Molecular docking studies of N-methyl- 2, 3 -disubstituted quinazolin-4-ones scaffold.Name: 4-Phenylthiazol-2-amine And the article contains the following content:

In recent days, synthesis of anticancer mols. having both low adverse effects and specific protein targeting are seldom. Synthesis of anticancer mols. having both low adverse effects and specific protein targeting is challenging. The main objective of our study was to develop mols. that can target activated protein kinase P38 alpha and activin receptor (ALK2) kinase for treating carcinoma. P38 alpha is involved in cell differentiation, apoptosis, and autophagy. Activin receptor (ALK2) kinase is responsible for mutations of cancerous cells. The synthesis of N-Me – 2, 3 -Disubstituted Quinazolin-4-Ones was carried out by refluxing of 1-methyl-2-(pyridinyl)-1,2-dihydro-4H-3,1-benzoxazin-4-one with 4-substituted phenyl-1,3-thiazol-2-amines. The mol. docking of 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazolin-4(1H)-one (5Da1-5Dk11) and 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-4-yl)-2,3-dihydroquinazolin-4(1H)-one (5Ea1-5Ek11) derivatives were carried out using Schrodinger Glide (version 2020_1) software. Twenty-two quinazoline-4-one derivatives were docked into selective P38 alpha and ACVR1 (ALK2) kinase with PDB code 3GC7, 6GI6. Based on the docking score, comparison between quinazolin-4-one derivatives, co-crystallized Ligands interaction was evaluated using 5-Fluorouracil as standard Best activity was found in compounds 5Df6, 5Dd4, 5Ed4 and 5Ef6 with ACVR1 (ALK2) kinase with score of -8.223, -7.936, -8.123, -7.907 and 5Df6, 5Dh8, 5Eb2 and 5Ee5 with P38alpha with score of -7.19, -7.027, -6.698, -6.789 Kcal/mol against enzymes responsible for treatment for cancer compare with reference drug score -5.765 and -6.195. This study will help in the design and development of a drug that gives room for the synthesis of a new selective ACVR1 (ALK2) kinase and P38alpha enzyme inhibitor with predetermined affinity and activity of the compound The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Name: 4-Phenylthiazol-2-amine

The Article related to methyl disubstituted quinazolinone scaffold mol docking, Placeholder for records without volume info and other aspects.Name: 4-Phenylthiazol-2-amine

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

On December 31, 2019, Rudrapal, Mithun; Sowmya, Mullapudi P. K. published an article.Related Products of 2010-06-2 The title of the article was Design, synthesis, drug-likeness studies and bio-evaluation of some new chalconeimines. And the article contained the following:

Newly designed chalconeimines were synthesized, characterized and evaluated for their in vitro antioxidant and antibacterial effectiveness. Results of antioxidant activity assay reveal that all the tested compounds possess good to moderate antioxidant activity which is lower in comparison to that of a standard drug (gallic acid). On the other hand, all the synthesized compounds were found to exhibit a considerably wider spectrum of antibacterial activity, but it was also narrower in comparison to that of a standard drug (ciprofloxacin). Elucidation of structure-activity relationships revealed that electron donating groups (-OH, -OCH3) contribute more to antioxidant potency, whereas electron withdrawing groups (-Cl) impart better antibacterial effectiveness. Moreover, results of drug-likeness studies indicate that a reasonable correlation exists between the drug-like properties and antioxidant activity of the synthesized chalconeimines. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Related Products of 2010-06-2

The Article related to chalconeimine drug design synthesis antioxidant antibacterial, Placeholder for records without volume info and other aspects.Related Products of 2010-06-2

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

On March 31, 2022, Siutkina, A. I.; Chashchina, S. V.; Makhmudov, R. R.; Novikova, V. V.; Chernov, I. N.; Igidov, N. M. published an article.Synthetic Route of 2010-06-2 The title of the article was Synthesis, analgesic and antimicrobial activity of N-hetarylamides of 2-(2-(diarylmethylene)hydrazono)-5,5-dimethyl-4-oxohexanoic acid. And the article contained the following:

New N-hetaryl substituted 2-((diarylmethylene)hydrazono)-5,5-dimethyl-4-oxohexanamides were obtained in 4 steps: a) Claisen condensation between pinacolone and di-Et oxalate in the presence of sodium methylate; b) the condensation of pivaloyl pyruvic acid with diarylmethylene hydrazones to form 2-diarylmethylenehydrazono-4-oxo-5,5-dimethylhexanoic acid; c) intramol. cyclization of hydrazonoacids in hydrazonofuranones; d) decyclization of the latter under the action of heterocyclic amines. Isolation of N-hetaryl-2-((diarylmethylene)hydrazono)-5,5-dimethyl-4-oxohexanamides was carried out by filtration of the resulting precipitate with subsequent recrystallization from ethanol or propane-2-ol. The structure of the obtained compounds was confirmed by the methods of 1H and 13C NMR spectroscopy and elemental anal. It is established that the obtained substituted hetarylamides exist in solutions of deuterated chloroform and DMSO in hydrazonoform. The analgesic and antimicrobial activity of the synthesized compounds was evaluated. Analgesic activity was studied by the “hot plate” thermal irritation method on outbred white mice of both sexes with i.p. injection. Antimicrobial activity of synthesized compounds was established via two-fold serial dilutions method in a liquid growth medium against two strains – S. aureus ATCC 6538-P and E. soli ATCC 25922. The studied compounds showed pronounced analgesic activity significantly exceeding that of the comparison drug metamizole sodium, and in some cases corresponding to the action of the reference diclofenac sodium. Therefore, pronounced analgesic activity accompanied with weak antimicrobial activity of the synthesized hetarylamides determines the prospects for the development of a new pharmacol. active substance with analgesic properties. 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 staphylococcus escherichia pain analgesics antimicrobial nhetarylamide, Placeholder for records without volume info and other aspects.Synthetic Route of 2010-06-2

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

On February 28, 2022, Alamiery, Ahmed; Mohamad, Abu Bakar; Kadhum, Abdul Amir H.; Takriff, Mohd S. published an article.Electric Literature of 2010-06-2 The title of the article was Comparative data on corrosion protection of mild steel in HCl using two new thiazoles. And the article contained the following:

This data article includes data described in the investigation report entitled “The synergistic role of azomethine group and triazole ring at improving the anti-corrosive performance of 2-amino-4-phenylthiazole” (Alamiery et al., 2021). In this data article, a comprehensive effect of 2-Amino-4-phenyl-N-benzylidene-5-(1,2,4-triazol-1-yl)thiazole (APNT) and 2-amino-4-phenylthiazole (APT) and optimized process parameter of the inhibitor in 1 M HCl solution was presented using gravimetric techniques and D. functional theory. The presence of the inhibitors influenced the corrosion resistance of mild steel (MS). Inhibition efficiencies values of 98.1% and 94.74% were recorded as results of inhibition of the MS by the inhibiting compounds APNT and ATP resp. DFT studies observed that the presence of benzylidene to the APNT and the substitution of a triazole in the thiazole ring are adsorption sites that increase the interaction of the APNT mols. with the iron atoms on the MS surface. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Electric Literature of 2010-06-2

The Article related to mild steel hydrogen chloride thiazole corrosion protection, corrosion, hydrochloric acid, inhibitor, mild steel, Placeholder for records without volume info and other aspects.Electric Literature of 2010-06-2

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

On September 21, 2021, Kshirsagar, Rajendra R.; Gadekar, Pradip K.; Khedkar, Vijay M.; Vijayakumar, Vijayaparthasarathi published an article.Electric Literature of 2010-06-2 The title of the article was Design, Synthesis, and the Effects of (E)-9-Oxooctadec-10-en-12-ynoic Acid Analogues to Promote Glucose Uptake. And the article contained the following:

(E)-9-Oxooctadec-10-en-12-ynoic acid is found to mediate its antidiabetic activity by increasing insulin-stimulated glucose uptake in L6 myotubes by activating the phosphoinositide 3-kinase (PI3K) pathway. A simultaneous study of site-specific modification followed by structure-activity relationship provides a tremendous scope for exploiting the bioactivity of the parent mol. Therefore, in the present study, we focused on site-specific modification of (E)-9-oxooctadec-10-en-12-ynoic acid (1) to generate multiple derivatives and extensive structure-activity relationship (SAR) studies. We have done structural base design and synthesized a series of amides from acid compound 1. Compound 1 consists of an acid functionality, which is known for its metabolism-related liabilities. The SAR has been generated using scaffolds of different antidiabetic drugs such as biguanides, sulfonylureas, thiazolidinediones/glitazones, peroxisome proliferator-activated receptors, K + ATP, α-glucosidase inhibitors, and others. Furthermore, the study demonstrates and explains the promising derivatives and importance of SAR of the compound (E)-9-oxooctadec-10-en-12-ynoic acid. In order to gain mechanistic insights, a mol. docking study was performed against PI3K, which could identify the binding modes and thermodn. interactions governing the binding affinity. According to our research,some compounds are the best compounds from the series having EC50 values of 15.47, 8.89, 7.00, 13.99, 8.70, 12.27, and 16.14μM, resp. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Electric Literature of 2010-06-2

The Article related to oxooctadecenynoic acid analog preparation antidiabetic activity, General Organic Chemistry: Synthetic Methods and other aspects.Electric Literature of 2010-06-2

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