Day: October 20, 2022

Devi, N. S.; Devi, Nirada published the artcile< Organocatalytic synthesis of N-substituted 5-arylidene rhodanines>, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is rhodanine aryl aldehyde proline catalyst diastereoselective aldol condensation; arylidenerhodanine preparation green chem.

A simple and efficient synthesis of N-substituted 5-arylidene rhodanines was developed via aldol condensation of N-substituted rhodanines with aromatic aldehydes using L-proline as the catalyst in water at room temperature The attractive features of this protocol were simple exptl. procedures, cleaner reactions, column free, high yield and avoids the use of toxic solvents.

Asian Journal of Chemistry published new progress about Aldol condensation catalysts, stereoselective. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Recommanded Product: 3-Benzyl-2-thioxothiazolidin-4-one.

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

Ulven, Elisabeth Rexen; Quon, Tezz; Sergeev, Eugenia; Barki, Natasja; Brvar, Matjaz; Hudson, Brian D.; Dutta, Palash; Hansen, Anders Hoejgaard; Bielefeldt, Line Oe.; Tobin, Andrew B.; McKenzie, Christine J.; Milligan, Graeme; Ulven, Trond published the artcile< Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators>, COA of Formula: C4H3NOS, the main research area is fatty acid receptor FFAR3 tetrahydroquinolone allosteric modulator.

Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized tool compounds has however impeded progress. Herein, we report structure-activity relationship of an allosteric modulator series and characterization of physicochem. and pharmacokinetic properties of selected compounds, including previous and new tools. Two representatives, 57 (TUG-1907) and 63 (TUG-2015), showed improved solubility and preserved potency. Of these, 57, with EC50 = 145 nM and a solubility of 33μM, showed high clearance in vivo but is a preferred tool in vitro. In contrast, 63, with EC50 = 162 nM and a solubility of 9μM, showed lower clearance and seems better suited for in vivo studies. Using 57, we demonstrate for the first time that FFA3 activation leads to calcium mobilization in murine dorsal root ganglia.

Journal of Medicinal Chemistry published new progress about Allosteric modulators. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, COA of Formula: C4H3NOS.

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

Hagiya, Kazutake; Mitsui, Sunao; Taguchi, Hiroaki published the artcile< A facile and selective synthetic method for the preparation of aromatic dialdehydes from diesters via the amine-modified SMEAH reduction system>, Application In Synthesis of 20582-55-2, the main research area is facile synthetic preparation aromatic dialdehyde diester amine SMEAH reduction.

A new reduction system employing N-methylpiperazine-modified sodium bis(2-methoxyethoxy)aluminum hydride (NMP-SMEAH) for the conversion of aromatic diesters to dialdehydes is described. The method is plain and efficient, and can be carried out under mild and operationally simple conditions applicable for large scale productions.

Synthesis published new progress about Dialdehydes Role: SPN (Synthetic Preparation), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Application In Synthesis of 20582-55-2.

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

Khan, Muhammad Amir; Ali, Shaukat; Shamim, Sumbul; Ahmed, Nazia; Hussain, Mushtaq; Farooq, Saba; Khan, Sadaf published the artcile< Antimicrobial and synergistic activity of thiazoline derivatives in combination with conventional antibiotics against multidrug resistant Staphylococcus aureus isolated from abscess drainage samples>, Product Details of C3H5NS2, the main research area is staphylococcus aureus thiazoline antimicrobial drainage sample.

Emergence and spread of multidrug resistant (MDR) Staphylococcus aureus strains is becoming major challenge in treatment of soft tissue infections. This study aimed to explore antimicrobial and synergistic antimicrobial potential of three com. available thiazoline derivatives (2-amino-2-thiazoline, 2-thiazoline-2-thiol and 2-acetyl-2-thiazoline) against MDR Staphylococcus aureus strains isolated from abscess drainage samples (n = 20). MDR Staphylococcus aureus isolates were identified by Kirby-Bauer disk diffusion assay and were further subjected to mol. identification by 16srRNA amplification and DNA sequencing. Min. Inhibitory Concentration (MIC) values of test compounds and antibiotics (0.25-512μg/mL) were measured and subsequently, synergism assay was performed to calculate Fractional Inhibitory Concentration (FIC) index. Out of twenty Staphylococcus aureus isolates, sixteen (80%) were found to be MDR whereas four (20%) were Non-MDR. Moxifloxacin and vancomycine were found most effective antibiotics, inhibiting 100% (n = 20) and 95% (n = 19) strains resp. Antimicrobial activity of 2-amino-2-thiazoline (MIC: 32μg/mL), 2-thiazoline-2-thiol (MIC: 64μg/mL) and 2-acetyl-2-thiazoline (MIC: 32μg/mL) was found significant against all ten tested MDR strains. Synergistic combinations of thiazoline derivatives with test antibiotics reduced MIC values significantly. Therefore, combination of tested thiazoline derivatives with antibiotics could be used as alternative therapeutic approach to treat soft tissue infections caused by MDR Staphylococcus aureus after further pre-clin. and clin. studies.

Pakistan Journal of Pharmaceutical Sciences published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Product Details of C3H5NS2.

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

Raut, Dattatraya G.; Kadu, Vikas D.; Sonawane, Vikas D.; Bhosale, Raghunath B. published the artcile< Synthesis of thiazole scaffolds by novel method and their In Vitro anthelmintic activity against Indian adult earthworm>, Application of C9H7N3O2S, the main research area is Pheretima anthelmintic thiazole scaffold synthesis.

A highly efficient and facile method has been described for the synthesis of substituted thiazoles and 2-aminothiazoles from phenacyl halide and thiourea in methanol using iodine as a catalyst at ambient temperature and product obtained in excellent yield within short time. The formation of these compounds was confirmed by IR, 1H NMR, 13C NMR and mass spectroscopy. The synthesized different substituted thiazoles (3a-3g) were taken for anthelmintic activity against Indian earthworm Pheretima posthuma at two concentration (50 mg/mL and 100 mg/mL) and results were expressed in terms of time for paralysis and time for death of worms. The albendazole (20 mg/mL) was used as reference standard The products were evaluated for anthelmintic activity to develop anthelmintic agent. Some of the compounds showed good anthelmintic activity (3g) as compared to albendazole.

European Journal of Biomedical and Pharmaceutical Sciences published new progress about Anthelmintics. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application of C9H7N3O2S.

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

Ghorbani-Vaghei, Ramin; Alavinia, Sedigheh; Merati, Zohreh; Izadkhah, Vida published the artcile< MNPs@SiO2-Pr-AP: A new catalyst for the synthesis of 2-amino-4-aryl thiazole derivatives>, Reference of 57493-24-0, the main research area is aminopyridine functionalized silica supported iron oxide nanoparticle catalyst preparation; aryl thiazole green preparation; acetophenones thiourea condensation functionalized silica supported magnetic nanoparticle catalyst.

Magnetically recoverable nano-magnetic catalyst supported with functionalized (n-propyl)-4-amino-pyridine silica (MNPs@SiO2-Pr-AP) was synthesized and characterized using different techniques. A simple and efficient synthesis of 2-amino-4-aryl thiazoles I [R = H, 4-Cl, 3-NO2, etc, X = CH, N] was described via condensation of acetophenones and thiourea using three different types of catalytic systems including N,N,N’,N’-tetrabromobenzene-1,3-disulfonamide [TBBDA], poly(N,N’-dibromo-N-ethylbenzene-1,3-disulfonamide) [PBBS] and a combination of TBBDA and MNPs@SiO2-Pr-AP. The results showed that, the use of TBBDA along with the MNPs@SiO2-Pr-AP gains the highest yields of the products in the shortest reaction time.

Applied Organometallic Chemistry published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Reference of 57493-24-0.

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

Fereidoonnezhad, Masood; Ahmadi Mirsadeghi, Hasti; Abedanzadeh, Sedigheh; Yazdani, Alireza; Alamdarlou, Arsalan; Babaghasabha, Mojgan; Almansaf, Zainab; Faghih, Zeinab; McConnell, Zachary; Shahsavari, Hamid R.; Beyzavi, M. Hassan published the artcile< Synthesis and biological evaluation of thiolate gold(I) complexes as thioredoxin reductase (TrxR) and glutathione reductase (GR) inhibitors>, COA of Formula: C3H5NS2, the main research area is gold thiolate complex preparation antitumor thioredoxin glutathione reductase; crystal structure gold thiolate complex.

New gold(I) thiolate complexes [(PPh2py)Au(SR)] (PPh2py = 2-(diphenylphosphino)pyridine and SR = the deprotonated form of pyridine-2-thiol (HSpy, 1a), pyrimidine-2 thiol (HSpyN, 1b), benzothiazole-2-thiol (HSbt, 1c) and 2-thiazoline-2-thiol (HSt, 1d)) were prepared by the reaction of chloro gold complex [(PPh2py)AuCl], A, with the corresponding in situ generated thiolate salt (through a nucleophilic substitution reaction) under inert conditions. All complexes were characterized by NMR spectroscopy and the structures of 1b and 1d were further identified by single crystal x-ray determination An in vitro cytotoxicity evaluation against five human cancer cell lines including A549 (nonsmall cell lung cancer), SKOV3 (human ovarian cancer), MCF-7 (human breast cancer), SW1116 (colon cancer) and HeLa (cervical cancer) demonstrated the promising antitumor effects of 1b in comparison with standard auranofin and cisplatin. The effects of these compounds on the proliferation of nontumoral breast cell line MCF-12A showed good selectivity among tumorigenic and nontumorigenic cell lines. 1B effectively produces cell death by inducing apoptosis in the MCF-7 human breast cancer cell line. These complexes inhibit both cytosolic (TrxR1) and mitochondrial (TrxR2) thioredoxin reductases as well as glutathione reductase (GR).

New Journal of Chemistry published new progress about Colon neoplasm. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, COA of Formula: C3H5NS2.

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

Guimaraes, Daniel Silqueira Martins; Luz, Leticia Silveira de Sousa; Batista do Nascimento, Sara; Silva, Lorena Rabelo; Martins, Natalia Rezende de Miranda; Goncalves de Almeida, Heloisa; Reis, Vitoria de Souza; Maluf, Sarah El Chamy; Budu, Alexandre; Marinho, Juliane Aparecida; Abramo, Clarice; Carmona, Adriana Karaoglanovic; Goulart da Silva, Marina; Rodrigues da Silva, Gisele; Kemmer, Victor Matheus; Butera, Anna Paola; Ribeiro-Viana, Renato Marcio; Gazarini, Marcos Leoni; Nascimento, Clebio Soares Jr.; Guimaraes, Luciana; Vieira dos Santos, Fabio; Victor de Castro, Whocely; Viana, Gustavo Henrique Ribeiro; Alves de Brito, Cristiana Ferreira; Varotti, Fernando de Pilla published the artcile< Improvement of antimalarial activity of a 3-alkylpiridine alkaloid analog by replacing the pyridine ring to a thiazole-containing heterocycle: Mode of action, mutagenicity profile, and Caco-2 cell-based permeability>, Application In Synthesis of 96-53-7, the main research area is colorectal adenocarcinoma cell permeability mutagenicity alkylpiridine alkaloid analog antimalarial; 3-Alkylpyridine marine alkaloid analogs; Antiplasmodial activity; Ferriprotoporphyrin-IX; Malaria; Plasmodium falciparum; Thiazole.

The development of new antimalarial drugs is urgent to overcome the spread of resistance to the current treatment. Herein we synthesized the compound 3, a hit-to-lead optimization of a thiazole based on the most promising 3-alkylpyridine marine alkaloid analog. Compound 3 was tested against Plasmodium falciparum and has shown to be more potent than its precursor (IC50 values of 1.55 and 14.7μM, resp.), with higher selectivity index (74.7) for noncancerous human cell line. This compound was not mutagenic and showed genotoxicity only at concentrations four-fold higher than its IC50. Compound 3 was tested in vivo against Plasmodium berghei NK65 strain and inhibited the development of parasite at 50 mg/kg. In silico and UV-vis approaches determined that compound 3 acts impairing hemozoin crystallization and confocal microscopy experiments corroborate these findings as the compound was capable of diminishing food vacuole acidity. The assay of uptake using human intestinal Caco-2 cell line showed that compound 3 is absorbed similarly to chloroquine, a standard antimalarial agent. Therefore, we present here compound 3 as a potent new lead antimalarial compound

European Journal of Pharmaceutical Sciences published new progress about Antimalarials. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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

Singh, Kamaljit; Singh, Sarbjit; Mahajan, Aman; Taylor, John A. published the artcile< Monoazo disperse dyes. Part 3: synthesis and fastness properties of some novel 4,5-disubstituted thiazolyl-2-azo disperse dyes>, Application In Synthesis of 57493-24-0, the main research area is disperse blue azo dye preparation polyester application.

Novel blue disperse dyes from 5-nitro-2-aminothiazole diazo components have been prepared using m-aminoacetanilide-derived coupling components. These dyes have been characterized using a range of spectroscopic techniques and exhibit interesting fastness behavior on dyed polyester.

Coloration Technology published new progress about Disperse azo dyes. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application In Synthesis of 57493-24-0.

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

Li, Xianlin; Tu, Zhenchao; Li, Hua; Liu, Chunping; Li, Zheng; Sun, Qiao; Yao, Yiwu; Liu, Jinsong; Jiang, Sheng published the artcile< Biological evaluation of new largazole analogues: Alteration of macrocyclic scaffold with Click chemistry>, Product Details of C12H18N2O4S, the main research area is cyclic peptide design synthesis largazole HDAC inhibitor structure activity; mol docking largazole HDAC enzyme active site crystal structure; thiazole ester Corey Fuchs reaction cycloaddition Click chem macrocyclization; HDAC inhibitor; click chemistry; largazole; macrocycles; peptides.

We report the design, synthesis, and biol. evaluation of a new series of largazole analogs in which a 4-methylthiazoline moiety was replaced with a triazole and tetrazole ring, resp. Compound (I) bearing a tetrazole ring was identified to show much better selectivity for HDAC1 over HDAC9 than largazole (10-fold). This work could serve as a foundation for further exploration of selective HDAC inhibitors using a largazole mol. scaffold.

ACS Medicinal Chemistry Letters published new progress about Azide-alkyne 1,3-dipolar cycloaddition reaction. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Product Details of C12H18N2O4S.

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