Day: October 26, 2022

On July 31, 2009, Yotnoi, Bunlawee; Limtrakul, Jumras; Prior, Timothy; Rujiwatra, Apinpus published an article.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Preparation and Characterization of Bis(μ-1,2-diaminoethane)cobalt(II) Hexavanadate: A Layered Polyoxovanadate Pillared by a Cobalt Coordination Complex. And the article contained the following:

The first example of polyoxovanadate layered framework with a cobalt coordination complex as a pillaring unit, CoII(μ-C2N2H8)2[VIV4VV2O14], was readily synthesized under hydrothermal conditions. The structure can be solved and refined in monoclinic P21/n with a 9.143(3), b 6.5034(11), c 15.874(4) Å, β = 101.90(2), V = 923.6(4) Å3 and Z = 2. The crystal structure comprises two-dimensional {VIV4VV2O14}2- layers extending parallel to [101], constructed from tetrahedral {VVO4} and square pyramidal {VIVO5} building units. Adjacent layers are linked through the octahedral {CoIIO2(μ-C2N2H8)2} pillars, within which the CoII resides on an inversion center. The structure displays N-H···O and C-H···O hydrogen bonding between the ethylenediamine and vanadium oxide layers. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to cobalt diaminoethane bridge layered polyoxovanadate pillared complex hydrothermal preparation, crystal structure cobalt diaminoethane bridge layered polyoxovanadate pillared complex and other aspects.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

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 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 August 26, 2003, Bizzarro, Fred Thomas; Corbett, Wendy Lea; Grippo, Joseph Francis; Haynes, Nancy-Ellen; Holland, George William; Kester, Robert Francis; Mahaney, Paige Erin; Sarabu, Ramakanth published a patent.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of cycloalkylheteroaryl propionamides as glucokinase activators for treatment of type II diabetes. And the patent contained the following:

Title compounds [I; R1, R2 = H, halo, amino, hydroxyamino, NO2, cyano, sulfonamido, perfluoroalkyl, alkylthio, alkylsulfonyl, alkylsulfinyl, etc.; R3 = alkyl, cycloalkyl; R4 = certain un- or monosubstituted 5- and 6-membered heteroaromatic rings connected by a ring C atom; R4 (claims) = un- or monosubstituted triazine, pyrazine, or pyridazine; and their pharmaceutical acceptable salts], were prepared via amidation, for use as glucokinase activators for treatment of type II diabetes. Thus, the invention compound N-(5-chlorothiazol-2-yl)-3-cyclopentyl-2(R)-[4-(methanesulfonyl)phenyl]propionamide (II) was prepared by addition of 3-cyclopentyl-2(R)-[4-(methanesulfonyl)phenyl]propionic acid (preparation given) to a stirred mixture of triphenylphosphine and N-bromosuccinimide in methylene chloride at 0°, followed by stirring at room temperature for 30 min, addition of a solution of 2-amino-5-chlorothiazole hydrochloride and pyridine in methylene chloride, and stirring at 25° overnight. All of the exemplified compounds I activated glucokinase in vitro, exhibiting an SC1.5 ≤ 30 μM. Selected invention compounds exhibited glucokinase activator activity in vivo when administered orally to mice. Thus, I are expected to increase insulin secretion in the treatment of type II diabetes. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to cycloalkylheteroaryl propionamide preparation thiazolyl glucokinase activator diabetes, antidiabetic thiazole pyrazine pyridazine pyridine pyrimidine glucokinase activator preparation and other aspects.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

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

Hussein, Awaz Jamil; Azeez, Hashim Jalal published an article in 2013, the title of the article was Synthesis and antimicrobial activity of some new thiazolidin-4-one derivatives of 4-(6-methylbenzo[d]thiazol-2-yl)benzamine.COA of Formula: C14H12N2S And the article contains the following content:

A number of derivatives of 2-(substituted phenyl)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl)thiazolidin-4-one were synthesized from the reaction of 4-(6-methylbenzo[d]thiazol-2-yl)benzenamine with different substituted benzaldehydes followed by cyclocondensation reaction of the prepared imines with 2-mercaptoacetic acid in high yields. Furthermore, the structures of the newly synthesized compounds were confirmed by FT-IR, 13C-NMR, 13C-DEPT, and 1H-NMR spectral data. The imines and thiazolidin-4-one derivatives were evaluated for their antibacterial activity against Escherichia coli as gram neg. and Staphylococcus aureus as gram pos., the results have shown significant activity against both types of bacteria. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).COA of Formula: C14H12N2S

The Article related to benzothiazolylaniline aryl aldehyde condensation, schiff base preparation antibacterial cyclization mercaptoacetate, aryl benzothiazolylphenyl thiazolidinone preparation antibacterial and other aspects.COA of Formula: C14H12N2S

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

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 May 16, 2022, Kong, Weixi; Liu, Yunting; Huang, Chen; Zhou, Liya; Gao, Jing; Turner, Nicholas J.; Jiang, Yanjun published an article.Reference of 2-Acetylthiazole The title of the article was Direct Asymmetric Reductive Amination of Alkyl (Hetero)Aryl Ketones by an Engineered Amine Dehydrogenase. And the article contained the following:

The direct asym. reductive amination of heteroaryl ketones has been a long-standing synthetic challenge. Here we report the engineering of an amine dehydrogenase (AmDH) from Jeotgalicoccus aerolatus for the asym. synthesis of chiral α-(hetero)aryl primary amines in excellent conversions (up to 99%) and enantioselectivities (up to 99% ee). The best AmDH variant (Ja-AmDH-M33) exhibited high activity and specificity toward alkyl (hetero)aryl ketones, even for those bearing a bulky alkyl chain. An efficient directed evolution approach based on mol. docking was implemented to enlarge the active pocket with a more hydrophobic entrance, which is responsible for the high activity. The Ja-AmDH-M33 was also used for preparative-scale synthesis of pharmaceutically relevant amines and a key intermediate of chiral pincer ligands, which highlighted its practical application in synthetic chem. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Reference of 2-Acetylthiazole

The Article related to jeotgalicoccus amination alkyl aryl ketone amine dehydrogenase mutation, alkyl (hetero)aryl ketones, amine dehydrogenase, asymmetric reductive amination, chiral amines, directed evolution and other aspects.Reference of 2-Acetylthiazole

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

On March 20, 2012, Murray, Anthony; Lau, Jesper; Vedsoe, Per published a patent.Synthetic Route of 859522-19-3 The title of the patent was Urea glucokinase activators. And the patent contained the following:

This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Synthetic Route of 859522-19-3

The Article related to arylcyclopentylmethylureidothiazolylthioalkanoate preparation glucokinase activator, diabetes hyperglycemia obesity dyslipidemia treatment thiazolylthioalkanoate ureido aryl cyclopentylmethyl and other aspects.Synthetic Route of 859522-19-3

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