Author: tianli

Telegina, Lyudmila N.; Kelbysheva, Elena S.; Strelkova, Tatyana V.; Ezernitskaya, Mariam G.; Smol’yakov, Alexander F.; Borisov, Yurii A.; Loim, Nikolay M. published the artcile< Synthesis and Photochemical Study of Thiazolidine Derivatives of Cymantrene and the Corresponding Dicarbonyl Chelates>, Recommanded Product: 4,5-Dihydrothiazole-2-thiol, the main research area is cymantrenylmethylthio thiazole preparation reaction; thiazolidinethione cymantrenylmethylthio preparation reaction; chelated cymantrenylmethylthio thiazolidine preparation crystal mol structure; photochem thiazolidine derivative cymantrene dicarbonyl chelate.

Isomeric 4,5-dihydro-2-[(cymantrenylmethyl)thio]thiazole (1) and 3-(cymantrenylmethyl)-1,3-thioazolidine-2-thione (2) were synthesized and photochem. behavior and spectral characteristics of tricarbonyl and dicarbonyl complexes were studied. Irradiation of compounds 1 and 2 results in the formation of stable chelates due to coordination of manganese to the donor nitrogen and sulfur atoms of the thiazolidine substituent. Photolysis is accompanied with a color change and the corresponding changes in the UV/Vis spectra depending on the solvent used. In the presence of CO, the dicarbonyl chelates enter the dark reaction to give the parent tricarbonyl complexes thus forming intermol. photochromic systems. Photolysis of the dicarbonyl chelate 5 gives the isomeric chelate 6, which in the course of the dark isomerization transforms into complex 5. Chelates 5 and 6 form an intramol. photochromic pair.

ChemistrySelectpublished new progress about Chelates Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Recommanded Product: 4,5-Dihydrothiazole-2-thiol.

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

Cheng, Lin; Su, Lantian; Tian, Xiaowen; Xia, Fan; Zhao, Chang; Yan, Wei; Shao, Zhenhua published the artcile< A pipeline to investigate the structures and signaling pathways of sphingosine 1-phosphate receptors>, Related Products of 115144-35-9, the main research area is sphingosine 1 phosphate receptor structure signaling pathway investigation.

Lysophospholipids (LPLs) are bioactive lipids that include sphingosine 1-phosphate (S1P), lysophosphatidic acid, etc. S1P, a metabolic product of sphingolipids in the cell membrane, is one of the best-characterized LPLs that regulates a variety of cellular physiol. responses via signaling pathways mediated by sphingosine 1-phosphate receptors (S1PRs). This implicated that the S1P-S1PRs signaling system is a remarkable potential therapeutic target for disorders, including multiple sclerosis (MS), autoimmune disorders, cancer, inflammation, and even COVID-19. S1PRs, a small subset of the class A G-protein coupled receptor (GPCR) family, are composed of five subtypes: S1PR1, S1PR2, S1PR3, S1PR4, and S1PR5. The lack of detailed structural information, however, impedes the drug discovery targeting S1PRs. Here, we applied the cryo-electron microscopy method to solve the structure of the S1P-S1PRs complex, and elucidated the mechanism of activation, selective drug recognition, and G-protein coupling by using cell-based functional assays. Other lysophospholipid receptors (LPLRs) and GPCRs can also be studied using this strategy.

Journal of Visualized Experimentspublished new progress about Autoimmune disease. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, Related Products of 115144-35-9.

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

Ryu, Se Hwan; Ra, Jongmin; Ko, Haye Min published the artcile< Efficient Synthesis of Sulfenamides through Mitsunobu-type Coupling Reaction of Thiols with Amines using Dibenzyl Azodicarboxylate>, Application In Synthesis of 96-53-7, the main research area is sulfenamide preparation; thiol amine Mitsunobu coupling; disulfides preparation.

S-H activation reaction of thiols employing dibenzyl azodicarboxylate (DBAD) had been developed for the preparation of sulfenamides I [R = H; R1 = Et, Bn, cyclopropyl, cyclopentyl, cyclohexyl; RR1 = (CH2)4, (CH2)6, (CH2)2O(CH2)2, etc.; X = O, S]. The dehydrogenation of thiols and amines under these reaction conditions involved the formation of dibenzyl hydrazine-1,2-dicarboxylate, which led to the S-N bond formation reaction. The reaction proceeded efficiently with release of dibenzyl hydrazine-1,2-dicarboxylate and afforded various sulfenamides I in good to excellent yields.

Asian Journal of Organic Chemistrypublished new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Banerjee, Janmajoy; Mariappan, G.; Nepal, Aswini Kumar; Dahal, Prassana; Khanal, Hemanta published the artcile< Conventional methods of synthesis of novel amino(phenyl)thiazoles and their antibacterial and local anesthetics screening>, COA of Formula: C9H7N3O2S, the main research area is acetamide thiazolylamino preparation anesthetic antibacterial.

Cyclocondensation of thiourea and substituted acetophenones RCOMe [R = Ph, 3-O2NC6H4, 4-O2NC6H4, 4-MeOC6H4, 2,5-(MeO)2C6H3] led to the formation of the corresponding 2-amino-4-R-thiazoles, which on further reaction with N-Ph 2-chloroacetamide gave N-Ph (thiazolylamino)acetamides I. The synthesized compounds I were investigated for their antibacterial activity by cup plate method against four bacterial strains. All the synthesized compounds exhibited mild to good antibacterial activities with I [R = 2,5-(MeO)2C6H3] showing promising activity against all strains of bacteria. The compounds I were also screened for local anesthetics activity taking lidocaine as standard, and all the compounds showed moderate activities.

International Journal of Pharmacy and Technologypublished 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, COA of Formula: C9H7N3O2S.

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

Zhang, Zhi-Hua; Wu, Hong-Mei; Deng, Sai-Nan; Cai, Xiao-Yu; Yao, Yu; Mwenda, Muriira Cyrus; Wang, Jin-Yin; Cai, Dong; Chen, Yu published the artcile< Design, synthesis, and anticancer activities of novel 2-amino-4-phenylthiazole scaffold containing amide moieties>, Application of C9H7N3O2S, the main research area is morpholinoacetamido thiazolylphenyl benzamide preparation anticancer activity.

Appropriately substituted 2-amino-4-phenylthiazole derivatives I (R = 3-CH3C6H4, 4-BrC6H4, 2-furyl, cyclohexyl, CH3OCH2, ClCH2, etc.) were designed and synthesized according to the structural characteriztics of crizotinib. The target compounds I were evaluated for their in vitro antiproliferative activity against A549, HeLa, HT29, and Karpas299 human cancer cell lines. Based on results of biol. studies, some of these compounds exhibited significant antiproliferative activity. Compound I (R = 3,4-Cl2C6H3) possessed outstanding growth inhibitory effects on the four cell lines, especially for HT29 cell with IC50 value of 2.01 μM. Along with the biol. assay data, a mol. docking study suggests that the target compounds were a potential inhibitor.

Journal of Chemistrypublished new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application of C9H7N3O2S.

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

Zhang, Xiaolin; Yang, Hongxia Ou; Ding, Yonghong published the artcile< The synthesis and characterization of potential novel active compounds, 2-aminothiazole derives Schiff bases>, Electric Literature of 57493-24-0, the main research area is aromatic ketone thiourea cyclocondensation; aminothiazole preparation condensation aryl aldehyde; Schiff base preparation.

Some 4-substituted-2-aminothiazoles were prepared starting from aromatic ketones and thiourea in the presence of powered iodine. Then treating 4-substituted-2-aminothiazole with substituted benzaldehyde gave corresponding 2-aminothiazole derivatives Schiff bases in good yield.

Advanced Materials Research (Durnten-Zurich, Switzerland)published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (heteroaryl). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Electric Literature of 57493-24-0.

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

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

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

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