Tag: M.W=200-250

Deng, Xiao-Bing; Chen, Ning; Wang, Zhi-Xin; Li, Xin-Yao; Hu, Hong-Yan; Xu, Jia-Xi published the artcile< A Convenient Synthesis of Thiazolidin-2-ones from Thiazolidine-2-thiones: Antibiotic Activity and Revisiting the Mechanism>, Reference of 171877-39-7, the main research area is thiazolidinone preparation antifungal antibacterial activity; thiazolidinethione bromoethanol reactant thiazolidinone preparation.

Various substituted thiazolidin-2-ones were synthesized from the corresponding thiazolidine-2-thiones with bromoethanol in ethanol with sodium ethoxide as a base. The optimal reaction conditions and mechanism were reinvestigated in detail. The bioassay indicated that (S)-4-iso-butylthiazolidin-2-one and (S)-4-benzylthiazolidin-2-one show certain inhibitive activities against Candida albicans and Escherichia coli.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Antibacterial agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Villa, Reymundo; Mandel, Alexander L.; Jones, Brian D.; La Clair, James J.; Burkart, Michael D. published the artcile< Structure of FD-895 Revealed through Total Synthesis>, SDS of cas: 171877-39-7, the main research area is FD895 synthesis structure antitumor.

The total synthesis of FD-895 (I) was completed through a strategy that featured the use of a tandem esterification ring-closing metathesis (RCM) process to construct the 12-membered macrolide and a modified Stille coupling to append the side chain. These studies combined with detailed anal. of all four possible C16-C17 stereoisomers were used to confirm the structure of FD-895 and identify an analog with an enhanced subnanomolar bioactivity.

Organic Letters published new progress about Absolute configuration. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, SDS of cas: 171877-39-7.

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

Malik, G. M.; Patel, Sandip K.; Patel, Pratixa K.; Zadafiya, S. K. published the artcile< Synthesis, characterization and microbial studies of 2-amino-4-(3'-nitrophenyl)thiazole based bisazo disperse dyes and their dyeing performance on polyester fibers>, COA of Formula: C9H7N3O2S, the main research area is aminonitrophenyl thiazolebisazo disperse dye polyester fiber microbial dyeing property; dyeing dye polyester fiber.

In the present study various substituted bisazo disperse dyes 2-(1′-substituted Ph azo)-4-(3′-nitrophenyl)-5-(2”,4”-dinitro Ph azo)thiazole derivatives have been synthesized using substituted 3°-amine, 2-amino-4-(3′-nitrophenyl)thiazole and 2,4-dinitroaniline. These were characterized using elemental anal., 1H NMR (NMR) and IR spectra. Their dyeing performance on polyester fiber was assessed and fastness properties of these dyes were evaluated by applying them to polyester fiber. These dyes exhibited moderate to good anti-bacterial and anti-fungal activities.

International Journal of Chemistry (Mumbai, India) published new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, COA of Formula: C9H7N3O2S.

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

Vo, Duc Duy; Tran, Thi Phuong Anh; Staedel, Cathy; Benhida, Rachid; Darfeuille, Fabien; Di Giorgio, Audrey; Duca, Maria published the artcile< Oncogenic MicroRNAs Biogenesis as a Drug Target: Structure-Activity Relationship Studies on New Aminoglycoside Conjugates>, HPLC of Formula: 57493-24-0, the main research area is MicroRNA structure aminoglycoside antitumor neoplasm; RNA structures; biogenesis; cancer; inhibitors; microRNA.

MicroRNAs (miRNAs) are a recently discovered category of small RNA mols. that regulate gene expression at the posttranscriptional level. Accumulating evidence indicates that miRNAs are aberrantly expressed in a variety of human cancers and that the inhibition of these oncogenic miRNAs could find application in the therapy of different types of cancer. Herein, the authors describe the synthesis and biol. evaluation of new small-mol. drugs that target oncogenic miRNAs production In particular, the authors chose to target two miRNAs (i.e., miRNA-372 and -373) implicated in various types of cancer, such as gastric cancer. Their precursors (premiRNAs) are overexpressed in cancer cells and lead to mature miRNAs after cleavage of their stem-loop structure by the enzyme Dicer in the cytoplasm. Some of the newly synthesized conjugates can inhibit Dicer processing of the targeted premiRNAs in vitro with increased efficacy relative to the previous results (D.D. Vo et al., ACS Chem. Biol. 2014, 9, 711-721) and, more importantly, to inhibit proliferations of adenocarcinoma gastric cancer (AGS) cells overexpressing these miRNAs, thus representing promising leads for future drug development.

Chemistry – A European Journal published new progress about Aminoglycosides Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, HPLC of Formula: 57493-24-0.

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

Javadi, Ali; Shockravi, Abbas; Koohgard, Mehdi; Malek, Ali; Shourkaei, Fateme Ahmadi; Ando, Shinji published the artcile< Nitro-substituted polyamides: A new class of transparent and highly refractive materials>, Product Details of C9H7N3O2S, the main research area is nitro polyamide transparent refractive material.

High-refractive-index polyamides (PAs) were developed by introducing nitro groups, thiazole rings, and thioether linkages. The PAs were prepared by the polycondensation of a novel diamine monomer, 5,5′-thiobis(2-amino-4-(3-nitrophenyl)thiazole) (DA), with various aromatic diacids. The bulky pendant nitrophenyl units, as well as the flexible thioether linkage in the diamine, endowed the resulting PAs with excellent solubilities in both amide-type polar aprotic solvents and less polar solvents. The obtained polymers exhibited high heat resistance, with 10% weight loss temperatures exceeding 472 °C under nitrogen and 427 °C in air atm., while their glass transition temperatures were in the range 210-244 °C. The combination of the nitro substituents, thiazole units, and thioether linkages provided PAs with high refractive indexes of up to 1.7660 at 632.8 nm, along with high transparency in the visible region and low birefringences (<0.0081). The structure-property relationships of these PAs due to the presence of nitro groups were also studied by comparing the results with the previously reported analogous polymers. European Polymer Journal published new progress about Birefringence. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

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

El-Dash, Yara; Elzayat, Emad; Abdou, Amr M.; Hassan, Rasha A. published the artcile< Novel thienopyrimidine-aminothiazole hybrids: Design, synthesis, antimicrobial screening, anticancer activity, effects on cell cycle profile, caspase-3 mediated apoptosis and VEGFR-2 inhibition>, Reference of 57493-24-0, the main research area is arylthiazolyl benzothienylpyrimidinylthioacetamide preparation antitumor activity VEGFR2 inhibition; structure arylthiazolyl benzothienylpyrimidinylthioacetamide antitumor activity VEGFR2 inhibition; lack antibacterial activity arylthiazolyl benzothienylpyrimidinylthioacetamide; antifungal activity arylthiazolyl benzothienylpyrimidinylthioacetamide; Aminothiazole; Anti-proliferative; Antimicrobial activity; Cell cycle arrest profile; Phosphorylated VEGFR-2, Caspase-3; Synthesis; Thienopyrimidine; VEGFR-2.

A series of novel hybrid compounds of hexahydrobenzo[4,5]thieno[2,3-d]pyrimidine with aminothiazole scaffolds I (R = H, Br, O2N; R1 = H, Cl, Br; R2 = H, Me) were synthesized. The synthesized compounds were evaluated for their cytotoxic activity against the NCI-60 human tumor cell line panel. Compounds I (R = H; R1 = Cl; R2 = H) (II), I (R = Br; R1 = ; R2 = H) (III) and I (R = R1 = R2 = H) exhibited significant antiproliferative activities at 10-5 M dose. II exhibited excellent cytotoxic activity against CNS cancer cell lines including SNB-75 and SF-295 as well as renal cancer cell line CAKI-1 when compared with sorafenib as standard anticancer drug. In addition, III showed almost comparable anticancer activity to sorafenib against SNB-75 cell line and displayed moderate activity against SF-295 and CAKI-1 cell lines in comparison to sorafenib. II inhibited the vascular endothelial growth factor receptor 2 (VEGFR-2) with IC50 of 62.48 ± 3.7 nM and decreased both total VEGFR-2 and phosphorylated VEGFR-2 in treated SNB-75 cells suggesting its ability to down regulate cell proliferation, growth, and survival.. The flow cytometric anal. showed that II displayed its cytotoxic activity through the reduction of the cellular proliferation and induction of cell cycle arrest at the G2/M phase. II clearly boosted the level of the apoptotic caspase-3. All the synthesized compounds were also screened for their antibacterial and antifungal activity against four pathogenic strains of both Gram-pos. and Gram-neg. as well as Candida albicans. III exhibited antifungal activity against Candida albicans compared to nystatin as the standard antifungal compound

Bioorganic Chemistry published new progress about Antitumor agents. 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

Su, H.; Yang, J.-H.; Lu, C.-F.; Chen, Z.-X.; Yang, G.-C. published the artcile< A study of the alkylation and acylation of N-acylthiazolidinethione>, Reference of 171877-39-7, the main research area is acylthiazolidinethione alkylation acylation.

Studying the alkylation and acylation of N-acylthiazolidinethione, the desired α-alkylated products and C-acylated products are not obtained, but rather the S-alkylated products and O-acylated products were obtained. The possible mechanism proposed shows that the deprotonation agent and electrophilic species are responsible for the stability of enolates. The enolates derived from N-acylthiazolidinethiones are decomposed in the presence of base, but they are comparatively stable in the presence of Lewis acid. When electrophilic reagent is alkyl halide, the enolate decomposition is the dominating pathway, and affords the S-alkylated products; and when electrophilic reagent is acyl chloride, the formation of a highly ordered chelated transition-state is the dominating pathway, and affords the O-acylated products.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Roever, Stephan; Cesura, Andrea M.; Huguenin, Philipp; Kettler, Rolf; Szente, Andre published the artcile< Synthesis and Biochemical Evaluation of N-(4-Phenylthiazol-2-yl)benzenesulfonamides as High-Affinity Inhibitors of Kynurenine 3-Hydroxylase>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is phenylthiazolylbenzensulfonamide preparation kynurenine hydroxylase inhibitor; thiazolylbenzensulfonamide preparation kynurenine hydroxylase inhibitor; structure activity phenylthiazolylbenzenesulfonamide kynurenine hydroxylase inhibitor.

The synthesis, structure-activity relationship (SAR), and biochem. characterization of N-(4-phenylthiazol-2-yl)benzenesulfonamides as inhibitors of kynurenine 3-hydroxylase is described. Thiazolbenzenesulfonamides I (IC50 = 37 nM, Ro-61-8048) and and II (IC50 = 19 nM) were high-affinity inhibitors of this enzyme in vitro. In addition, both compounds blocked rat and gerbil kynurenine 3-hydroxylase after oral administration, with ED50’s in the 3-5 μmol/kg range in gerbil brain. In a microdialysis experiment in rats, I dose dependently increased kynurenic acid concentration in the extracellular hippocampal fluid. A dose of 100 μmol/kg po led to a 7.5-fold increase in kynurenic acid outflow. These new compounds should allow detailed investigation of the pathophysiol. role of the kynurenine pathway after neuronal injury.

Journal of Medicinal Chemistry published new progress about Structure-activity relationship, enzyme-inhibiting. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Safety of 2-Amino-4-(3-nitrophenyl)thiazole.

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

Munive, Laura; Rivas, Veronica M.; Ortiz, Aurelio; Olivo, Horacio F. published the artcile< Oxazolidine-2-thiones and Thiazolidine-2-thiones as Nucleophiles in Intermolecular Michael Additions>, Reference of 171877-39-7, the main research area is thiazolidinethione crotonylthiazolidinethione stereoselective Michael addition; oxazolidinethione crotonyloxazolidinethione stereoselective Michael addition.

Conjugate addition of thiazolidinethiones and oxazolidinethiones to N-crotonylthiazolidinethiones and -oxazolidinethiones was observed in the presence of excess triethylamine in dichloromethane. The addition takes place by the nitrogen of the heterocycle with high diastereoselectivity. It was observed that the stereoselective addition occurs on the anti-s-cis conformation of the N-enoyl sulfur-containing heterocycle.

Organic Letters published new progress about Amino amides Role: SPN (Synthetic Preparation), PREP (Preparation). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Koohgard, Mehdi; Hosseinpour, Zeinab; Sarvestani, Abdollah Masoudi; Hosseini-Sarvari, Mona published the artcile< ARS-TiO2 photocatalyzed direct functionalization of sp2 C-H bonds toward thiocyanation and cyclization reactions under visible light>, Quality Control of 57493-24-0, the main research area is thiocyanation cyclization visible light ARS photocatalyst regioselective.

An ARS-TiO2 photocatalyst has been prepared by a simple method through stirring a mixture of ARS and TiO2 at room temperature in the dark to extend the photocatalytic response of titanium dioxide toward the visible light spectrum. The synergic effect of ARS and TiO2 in the photocatalyst system has catalyzed direct C-H functionalization of sp2 C-H bonds toward thiocyanation and cyclization reactions. Several aromatic and heteroaromatic scaffolds (2-phenylamino-thiazoles I (R = H, 2-Cl, 4-Ph, etc.), phenols R1OH (R1 = Ph, 3-ethylphenyl, 2-formylphenyl, etc.), anilines R2C6H4N(R3)(R4) (R2 = 2-Me, 3-Cl, 3-OMe, etc.; R3 = H, Me, Et, Ph; R4 = H, Me, Et), indoles II (R5 = H, Me; R6 = H, Me; R7 = H, 5-MeO, 6-methoxycarbonyl, 5-Br, 5-Me) and pyrroles such as 1H-pyrrole and 1-methyl-1H-pyrrole) were treated with the ammonium thiocyanate at room temperature Thiocyanation of phenol and synthesis of 2-aminobenzothiazole derivatives III (R8 = Me, I, prop-1-en-2-yl, etc.) under visible light are presented.

Catalysis Science & Technology published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Quality Control of 57493-24-0.

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