Category: thiazole

Zhu, Ziqi; Xiao, Jieshuai; Li, Mingjie; Shi, Zhuangzhi published the artcile< Nickel-Catalyzed Intermolecular Asymmetric Addition of Aryl Iodides across Aldehydes>, COA of Formula: C4H3NOS, the main research area is diarylmethanol preparation enantioselective; aryl iodide asym addition aldehyde nickel catalyst; Asymmetric Addition; Chiral Alcohols; Enantioselectivity; Nickel Catalysis.

Enantioenriched alcs. comprise much of the framework of organic mols. Here, the authors first report that chiral nickel complexes can catalyze the intermol. enantioselective addition of aryl iodides across aldehydes to provide diverse optically active secondary alcs. using zinc metal as the reducing agent. This method shows a broad substrate scope under mild reaction conditions and precludes the traditional strategy through the pre-generation of organometallic reagents. Mechanistic studies indicate that an in situ formed arylnickel, instead of an arylzinc, adds efficiently to the aldehydes, forming a new C-C bond and a chiral nickel alkoxide that may be turned over by zinc powder.

Angewandte Chemie, International Editionpublished new progress about Addition reaction catalysts, stereoselective (intermol.). 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

Imadul Islam, Sk; Das, Arindam; Mitra, Rajib Kumar published the artcile< Excited state proton transfer in reverse micelles: Effect of temperature and a possible interplay with solvation>, Related Products of 2591-17-5, the main research area is reverse micelle excited state proton transfer temperature solvation.

Excited state proton transfer (ESPT) is a fundamental process of immense biophys. interest and considering the heterogeneity existing in real biol. environments we investigate the process in a bio-mimicking reverse micellar (RM) systems. We herein report a detailed study on the ESPT process of a photo-acid D-luciferin at different temperatures in RMs composed of: anionic AOT, cationic DDAB, and neutral Igepal-520 using steady state and time resolved fluorescence measurements. We found that with increasing temperature both solvation as well as the ESPT rate accelerate, however, the extent of the increase is RM specific, and they even not complement each other. Our study clearly identifies the pivotal role of solvation, specially in micro-heterogeneous environments, to guide the ESPT process.

Journal of Photochemistry and Photobiology, A: Chemistrypublished new progress about Fluorescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Related Products of 2591-17-5.

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

Xu, Yuan-Yuan; Qian, An-Ran; Cao, Xu-Feng; Ling, Chen-Yu; Cao, Yong-Bing; Wang, Rui-Lian; Li, Yi-Su; Yang, Yu-She published the artcile< Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents>, Computed Properties of 72054-60-5, the main research area is triazole beta lactam derivative preparation antifungal mol docking.

A series of novel triazole derivatives containing γ-lactam I [R = Br, 5-pyrimidinyl, Ph, etc.] was designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and HRMS. The in vitro antifungal activities of the target compounds were evaluated. The results showed that all of the compounds exhibited stronger activity against the six clin. important fungi tested than fluconazole. Compounds I [R = 3-cyano-6-pyridinyl, 4-fluorophenyl] showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2-bromo-5-((2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)-5,6-dihydro-4H-pyrrolo[3,4-d]thiazol-4-one and CYP51 was investigated.

Chinese Chemical Letterspublished new progress about Boronic acids, esters Role: RCT (Reactant), RACT (Reactant or Reagent). 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Computed Properties of 72054-60-5.

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

Melzer, Benedikt C.; Plodek, Alois; Bracher, Franz published the artcile< Functionalization of 4-bromobenzo[c][2,7]naphthyridine via regioselective direct ring metalation. A novel approach to analogs of pyridoacridine alkaloids>, Computed Properties of 1003-32-3, the main research area is pyridoacridine alkaloid analog preparation regioselective; bromobenzo naphthyridine electrophile ring metalation cyclization; alkaloids; cyclization; metalation; naphthyridine; pyridoacridine.

Readily available 4-bromobenzo[c][2,7]naphthyridine undergoes regioselective direct ring metalation at C-5 with TMPMgCl·LiCl at -40°. Quenching with various electrophiles gives a broad range of 5-substituted products, which are building blocks for the synthesis of heterocyclic natural products and analogs thereof. In combination with a Parham-type cyclization a novel approach to pyrido[4,3,2-mn]acridones has been worked out.

Beilstein Journal of Organic Chemistrypublished new progress about Alkaloids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.

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

Wu, Yikang; Sun, Ya-Ping; Yang, Yong-Qing; Hu, Qi; Zhang, Qi published the artcile< Removal of thiazolidinethione auxiliaries with benzyl alcohol mediated by DMAP>, Safety of (S)-4-Benzylthiazolidine-2-thione, the main research area is acylthiazolidinethione benzyl alc substitution DMAP; benzyl ester preparation; DMAP substitution mediator.

In the presence of DMAP, a range of N-acylthiazolidinethiones carrying different substituents were smoothly converted into benzyl esters, e.g., I. All the benzyl esters were obtained in good yields.

Journal of Organic Chemistrypublished new progress about Aldol condensation, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Safety of (S)-4-Benzylthiazolidine-2-thione.

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

Yin, Zhiping; Zhang, Zhuan; Soule, Jean-Francois; Dixneuf, Pierre H.; Wu, Xiao-Feng published the artcile< Iron-catalyzed carbonylative alkyl-acylation of heteroarenes>, HPLC of Formula: 1003-32-3, the main research area is alkyl heteroaryl ketone preparation chemoselective; heteroarene carbon monoxide carbonylative alkyl acylation iron triflate.

Herein, an efficient carbonylative protocol for the introduction of an alkyl-acyl group into heteroarenes from cyclobutanone oximes is presented. In the presence of Fe(OTf)2 catalyst, proceeds via intermol. alkyl-acylation of different heteroarenes. A broad range of alkyl heteroaryl ketones are synthesized with excellent functional group tolerance with good chemoselectivity.

Journal of Catalysispublished new progress about Acylation (alkyl-). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, HPLC of Formula: 1003-32-3.

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

Moghimi, S.; Heravi, M. M.; Oskooie, H. A.; Beheshtiha, Y. S. published the artcile< A novel un-catalyzed and solvent-free method for the synthesis of 2-thioxothiazolidin-4-ones>, Application of C10H9NOS2, the main research area is rhodanine preparation catalyst solvent free; primary amine carbon disulfide chloroacetyl chloride multicomponent re??action.

An easy and highly efficient one-pot, three-component synthesis of rhodanines was reported. The reaction of primary amines, carbon disulfide and chloroacetyl chloride proceeded in the absence of solvent and catalyst affording 2-thioxothiazolidin-4-ones in good to excellent yields.

Scientia Iranica, Transaction C: Chemistry, Chemical Engineeringpublished new progress about Primary amines Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Application of C10H9NOS2.

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

Lerner, Claude G.; Hajduk, Philip J.; Wagner, Rolf; Wagenaar, Frank L.; Woodall, Charlotte; Gu, Yu-Gui; Searle, Xenia B.; Florjancic, Alan S.; Zhang, Tianyuan; Clark, Richard F.; Cooper, Curt S.; Mack, Jamey C.; Yu, Liping; Cai, Mengli; Betz, Steven F.; Chovan, Linda E.; McCall, J. Owen; Black-Schaefer, Candace L.; Kakavas, Stephan J.; Schurdak, Mark E.; Comess, Kenneth M.; Walter, Karl A.; Edalji, Rohinton; Dorwin, Sarah A.; Smith, Richard A.; Hebert, Eric J.; Harlan, John E.; Metzger, Randy E.; Merta, Philip J.; Baranowski, John L.; Coen, Michael L.; Thornewell, Susan J.; Shivakumar, Annapur G.; Saiki, Anne Y.; Soni, Niru; Bui, Mai; Balli, Darlene J.; Sanders, William J.; Nilius, Angela M.; Holzman, Thomas F.; Fesik, Stephen W.; Beutel, Bruce A. published the artcile< From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae>, Synthetic Route of 1003-32-3, the main research area is antibacterial biphenyl preparation structure activity HI0065 ATP binding protein; drug discovery target antibacterial NMR screen.

As part of a fully integrated and comprehensive strategy to discover novel antibacterial agents, NMR- and mass spectrometry-based affinity selection screens were performed to identify compounds that bind to protein targets uniquely found in bacteria and encoded by genes essential for microbial viability. A biphenyl acid lead series emerged from an NMR-based screen with the Haemophilus influenzae protein HI0065, a member of a family of probable ATP-binding proteins found exclusively in eubacteria. The structure-activity relationships developed around the NMR-derived biphenyl acid lead were consistent with on-target antibacterial activity as the Staphylococcus aureus antibacterial activity of the series correlated extremely well with binding affinity to HI0065, while the correlation of binding affinity with B-cell cytotoxicity was relatively poor. Although further studies are needed to conclusively establish the mode of action of the biphenyl series, these compounds represent novel leads that can serve as the basis for the development of novel antibacterial agents that appear to work via an unprecedented mechanism of action. Overall, these results support the genomics-driven hypothesis that targeting bacterial essential gene products that are not present in eukaryotic cells can identify novel antibacterial agents.

Chemical Biology & Drug Designpublished new progress about Antibacterial agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Synthetic Route of 1003-32-3.

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>, Category: thiazole, 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 Journalpublished 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, Category: thiazole.

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

Moszczynski-Petkowski, Rafal; Majer, Jakub; Borkowska, Malgorzata; Bojarski, Lukasz; Janowska, Sylwia; Matloka, Mikolaj; Stefaniak, Filip; Smuga, Damian; Bazydlo, Katarzyna; Dubiel, Krzysztof; Wieczorek, Maciej published the artcile< Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines>, COA of Formula: C4H3NOS, the main research area is triazolopyridine pyrazolopyridine benzodiazole imidazopyrimidine preparation PDE10A enzyme inhibitor; 1H-1,3-benzodiazoles; Imidazo[1,2-a]pyrimidines; PDE10A.

New compounds containing [1,2,4]triazolo[1,5-a]pyridine I (R = 5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl, 4,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl, 4-methylquinazolin-2-yl; R1 = Ph, pyrimidin-2-yl), pyrazolo[1,5-a]pyridine II (R = 5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl, 4,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl; R1 = phenyl), 1H-1,3-benzodiazole III (R1 = 2-methoxyphenyl, pyridin-2-yl, 1,3-oxazol-4-yl, etc.; R2 = H, Me) and imidazo[1,2-a]pyrimidine IV backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines III and IV showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.

European Journal of Medicinal Chemistrypublished new progress about Benzimidazoles Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 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