Category: thiazole

Tapadar, Subhasish; He, Rong; Luchini, Doris N.; Billadeau, Daniel D.; Kozikowski, Alan P. published the artcile< Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is histone deacetylase inhibitor preparation isoxazole moiety linker antitumor.

A series of hydroxamic acid based histone deacetylase inhibitors 6-15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micromolar inhibitory activity against five pancreatic cancer cell lines.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

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

Calabretta, Maria Maddalena; Alvarez-Diduk, Ruslan; Michelini, Elisa; Roda, Aldo; Merkoci, Arben published the artcile< Nano-lantern on paper for smartphone-based ATP detection>, Quality Control of 2591-17-5, the main research area is adenosine triphosphate biosensor smartphone paper urinary tract infection; ATP biosensor; Bioluminescence; Luciferase; Paper-based biosensor; Smartphone.

ATP-driven bioluminescence relying on the D-luciferin-luciferase reaction is widely employed for several biosensing applications where bacterial ATP detection allows to verify microbial contamination for hygiene monitoring in hospitals, food processing and in general for cell viability studies. Several ATP kit assays are already com. available but an user-friendly ATP biosensor characterized by low-cost, portability, and adequate sensitivity would be highly valuable for rapid and facile on site screening. Thanks to an innovative freeze-drying procedure, we developed a user-friendly, ready-to-use and stable ATP sensing paper biosensor that can be combined with smartphone detection. The ATP sensing paper includes a lyophilized “”nano-lantern”” with reaction components being rapidly reconstituted by 10μL sample addition, enabling detection of 10-14 mol of ATP within 10 min. We analyzed urinary microbial ATP as a biomarker of urinary tract infection (UTI), confirming the capability of the ATP sensing paper to detect the threshold for positivity corresponding to 105 colony-forming units of bacteria per mL of urine.

Biosensors & Bioelectronics published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Andrade, Carlos Kleber Z.; Rocha, Rafael O.; Vercillo, Otilie E.; Silva, Wender A.; Matos, Ricardo Alexandre F. published the artcile< DCC/DMAP-mediated coupling of carboxylic acids with oxazolidinones and thiazolidinethiones>, Computed Properties of 171877-39-7, the main research area is DCC DMAP mediated coupling carboxylic acid oxazolidinone thiazolidinethione; acylation oxazolidinone thiazolidinethione DMAP catalyst dicyclohexylcarbodiimide reagent.

Dicyclohexylcarbodiimide and catalytic dimethylaminopyridine were successfully used in the coupling of carboxylic acids with oxazolidinones and thiazolidinethiones. The acylated products were obtained in good yields.

Synlett published new progress about Acylation. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Computed Properties of 171877-39-7.

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

Chen, Ning; Du, Hongguang; Liu, Weidong; Wang, Shanshan; Li, Xinyao; Xu, Jiaxi published the artcile< Synthesis and Fungicidal Activity of Simple Structural 1,3-Thiazolidine-2-Thione Derivatives>, Category: thiazole, the main research area is vicinal aminoalc carbon disulfide cyclization coupling; thiazolidinethione preparation SAR antifungal activity.

A series of simple structural 1,3-thiazolidine-2-thione derivatives I and II [R1 = H, (s)-Me, (s)-Ph, etc; R2 = H, Me, (s)-Ph] with various substituents on the S-, N-, 4-, and 5-positions was synthesized with high yields from various vicinal amino alcs. via two steps and screened for their antifungal activity. Bioassay results reveal that some thiazolidine-2-thione derivatives show strong antifungal activities against P. capsici, G. zeae, S. sclerotiorum, A. alternata, B. cinerea, or R. solani. The SAR anal. indicates that N-acyl substituted and 4-alkyl substituents can enhance the antifungal activity. Notably, I [R1 = (s)-iPr, R2 = H] shows excellent activity against B. cinerea and G. zeae with IC50 values at 3.7 μg/mL and 6.5 μg/mL, resp., and I [ R1 = (s)-iBu, R2 = H] shows remarkable fungicidal activity against R. solani, S. sclerotiorum, and G. zeae with IC50 values at 1.0 μg/mL, 12.1 μg/mL, and 11.0 μg/mL, resp.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Category: thiazole.

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

Rinaldi, Marta; Tintori, Cristina; Franchi, Luigi; Vignaroli, Giulia; Innitzer, Anna; Massa, Silvio; Este, Jose A.; Gonzalo, Encarna; Christ, Frauke; Debyser, Zeger; Botta, Maurizio published the artcile< A Versatile and Practical Synthesis toward the Development of Novel HIV-1 Integrase Inhibitors>, Safety of 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is preparation antiviral HIV1 integrase inhibitor.

As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their capacity to inhibit the catalytic activity of HIV-1 integrase. Biol. evaluations revealed that some of the synthesized compounds possess good inhibitory potency in enzymic assays and are able to inhibit viral replication in MT-4 cells at low micromolar concentrations Finally, docking studies were conducted to analyze the binding mode of the synthesized compounds within the DNA binding site of integrase in order to refine their structure-activity relationships.

ChemMedChem published new progress about Antiviral agents. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Safety of 3-Benzyl-2-thioxothiazolidin-4-one.

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

Kamble, Sonali S.; Hese, Shrikant V.; Dawane, Bhaskar S.; Gacche, Rajesh N. published the artcile< Anti-breast cancer and antiangiogenic potential of substituted thiazolo[2,3-b] quinazoline derivatives: synthesis, in vitro and in vivo analysis>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is thiazolo quinazoline derivative antibreast cancer antiangiogenic potential.

Herein, a series of novel substituted thiazolo[2,3-b]quinazoline derivatives has been synthesized. The capability of the synthesized compounds 3a-i to hinder the viability of human breast cancer cell line (MCF-7) was assessed. The compounds were evaluated as possible inhibitors of angiogenesis by using in vivo chorioallantoic membrane (CAM) model. Amongst the compounds 3a-i screened, 3d and 3f exhibited excellent cytotoxicity with IC50 values 6.0±0.03μM & 5.0±0.36μM resp. Compounds were further tested to evaluate potential to inhibit the pro-angiogenic cytokines associated with tumor development. Both the compounds were found to be potent antiangiogenic agents against VEGF, TNFa, IL6, TGFb, and EGF. The outcome of the present study reveals that, compound 3d and 3f showed the promising inhibitory activity on the viability of MCF-7 cells. In the in vivo CAM model, treatment with all the compounds resulted in the significant decrease in blood vessels d. The findings of the study suggest that, compounds 3d & 3f may act as potential anti-breast cancer and antiangiogenic agents.

Chemistry & Biology Interface published new progress about Angiogenesis. 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

Marwaha, Tejinder Kaur; Madgulkar, Ashwini; Bhalekar, Mangesh; Asgaonkar, Kalyani published the artcile< Molecular docking, synthesis, and characterization of chitosan-graft-2-mercaptobenzoic acid derivative as potential drug carrier>, COA of Formula: C3H5NS2, the main research area is docking chitosan mercaptobenzoic acid derivative drug carrier.

Chitosan is a hydrophilic polymer with prominent mucoadhesive properties. However, it forms weak hydrogen bonds with mucin thus limiting its mucoadhesion and exhibit reduced bioavailability due to its short retention time in the body. The aim of the present study was to synthesize and characterize novel thiolated chitosan with improved functional property. A unique approach of using mol. docking to select ligand to chem. modify chitosan has been employed in the present research. A set of ligands were screened virtually using docking anal. and 2-mercapto benzoic acid showed the lowest glide score of -4.31 Kcal/Mol thus displayed better binding interaction with chitosan. Based on the docking results, the best-fit ligand was selected for wet laboratory synthesis. 2-Mercapto benzoic acid was covalently attached to chitosan via formation of an amide bond and the reaction was mediated by carbodiimide and N-hydroxysuccinimide. The synthesized polymer was in turn evaluated for zeta potential, Fourier transformed IR, differential scanning calorimetry, mol. weight that confirmed conjugation of chitosan with the thiol ligand. The prepared thiomer was further subjected to mucoadhesion studies and displayed better mucoadhesion properties as compared to unmodified chitosan. Thus, the potential of the novel thiomer can be further explored as an excipient for drug delivery system with an emphasis on mucoadhesion.

Journal of Applied Polymer Science published new progress about Differential scanning calorimetry. 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

Vafina, G. F.; Guryanova, T. S. published the artcile< Synthesis of S-Containing Maleopimaric Acid Derivatives>, Related Products of 96-53-7, the main research area is maleopimaric acid thio analog preparation.

New S-containing maleopimaric acid derivatives were synthesized. The structures of all synthesized compounds were elucidated using NMR spectroscopy and elemental analyses.

Chemistry of Natural Compounds published new progress about Diterpenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Related Products of 96-53-7.

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

Din Reshi, Noor U.; Senthurpandi, Dineshchakravarthy; Samuelson, Ashoka G. published the artcile< Asymmetric transfer hydrogenation of ketones using Ru(0) nanoparticles modified by Chiral Thiones>, Electric Literature of 171877-39-7, the main research area is ketone asym transfer hydrogenation; oxazolidinethione thiozolidinethione ruthenium half sandwich complex catalyst preparation.

The catalytic asym. transfer hydrogenation (ATH) of acetophenone in isopropanol by Ru(0) nanoparticles (NPs) obtained by the in-situ reduction of Ru(II) half-sandwich complexes of chiral 2-oxazolidinethiones and 2-thiozolidinethiones was examined and compared with the catalytic activity of Ru(0) NPs formed in-situ by the reduction of [Ru(p-cymene)(Cl)2]2 in presence of optically active ligands such as (S)-4-isobutylthiazolidine-2-thione, (S)-4-isopropyl-2(-2-pyridinyl)-2-oxazoline, (8S, 9R)-(-)-cinchonidine, (S)-leucinol, (S)-phenylalaninol, and (S)-leucine. Three of the best catalytic systems were then examined for ATH of thirteen aromatic ketones with different electronic and steric properties. A maximum of 24% ee was obtained using NPs generated from the Ru (II) half-sandwich complex with (S)-4-isobutylthiazolidine-2-thione in the TH of acetophenone. The NPs were characterized by TEM and DLS measurements. Kinetic studies and poisoning experiments confirmed that the reaction is catalyzed by the chiral NPs formed in-situ. Complete characterization of the complexes, including the X-ray crystallog. characterization of two complexes, was also carried out.

Applied Organometallic Chemistry published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Electric Literature of 171877-39-7.

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

Vydzhak, R. N.; Brovarets, V. S.; Pil’o, S. G.; Drach, B. S. published the artcile< Synthesis and Transformations of Two Types of 4-Phosphorylated Aldehydes of the Oxazole Series>, Name: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is formylpiperidinyloxazolyl phosphonate preparation; formyloxazolyl phosphonate preparation; piperidinyl formyloxazolyl phosphonate preparation; morpholinyl formyloxazolyl phosphonate preparation; phosphonium oxothiazolylideneoxazolyl preparation; thiazolylhydrazonooxazolyl phosphonate preparation.

The reaction of 2,2-dichloro-N-(1,2,2,2-tetrachloroethyl)acetamide with trialkyl phosphites and triphenylphosphine gave [2,2-dichloro-1-[(dichloroacetyl)amino]ethenyl]triphenylphosphonium chloride and [2,2,2-trichloro-1-(dichloroacetyl)amino]phosphonic acid di-Me ester and [2,2,2-trichloro-1-(dichloroacetyl)amino]phosphonic acid di-Et ester. Cyclocondensation of the latter in the presence of amines gave [2-formyl-5-(1-piperidinyl)-4-oxazolyl]phosphonic acid di-Me ester (I), [2-formyl-5-(1-piperidinyl)-4-oxazolyl]phosphonic acid di-Et ester (II) and [2-formyl-5-(4-morpholinyl)-4-oxazolyl]phosphonic acid di-Me ester (III) and [2-formyl-5-(4-morpholinyl)-4-oxazolyl]phosphonic acid di-Et ester (IV). Their structure of products was determined by spectroscopy and also by chem. transformations into phenylhydrazones, thiosemicarbazones, aminals, and other functional derivatives of I-IV.

Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) published new progress about Condensation reaction. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Name: 3-Benzyl-2-thioxothiazolidin-4-one.

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