Tag: M.W=200-250

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

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

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

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

Mishra, Deepak; Fatima, Atiya; Rout, Chittaranjan; Singh, Ram published the artcile< An efficient one-pot synthesis of 2-aminothiazole derivatives>, COA of Formula: C9H7N3O2S, the main research area is aminothiazole preparation; haloketone thioamide cyclization.

A highly efficient, rapid and catalyst free protocol has been developed for the synthesis of 2-aminothiazoles I (R = Br, NO2, OCH3, etc.; R1 = Cl, CN, OCH3, etc.) in THF. Reaction was carried out at room temperature and the products were obtained in high yields without further purification

Chemica Sinicapublished new progress about Cyclization. 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

Khiat, Manel; Zradni, Fatima-Zohra; Kasmi-Mir, Souad; Baeza, Alejandro published the artcile< Study of the electrochemical behavior of merocyanine and merocarbocyanine salts and their transformation into π-electron donor molecules, namely tetrathiatetraazafulvalenes>, HPLC of Formula: 10574-69-3, the main research area is tetrathiatetraazafulvalene electrochem preparation cyclic voltammetry voltammogram.

An electrochem. study using cyclic voltammetry method was carried out on some previously prepared merocyanines salts, namely thiazolideniumsulfonate salts and thiazolidenium chloride salts I [R = Ph, Bn; R1 = H, SMe; X = Cl, 4-methylbenzenesulfonate] and merocarbocyanines salts, namely alkylidenthiazolidenium sulfonate salt and alkylidenthiazolidenium chloride salt II [R = n-Pr]. These salts were transformed by dimerization in situ in a voltammetric cell into tetrathiatetraazafulvalenes (TTTAFs) such as III supposed to be π-electron donor mols. due to existing conjugation in their structure. The structure of all new chem. synthesized mols. was confirmed by IR, 1H-NMR, 13C-NMR, and MS. The transformation of salts into TTTAF was confirmed by a reversible voltammogram curve and variation of observed potentials.

Indonesian Journal of Chemistrypublished new progress about Charge transfer complexes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, HPLC of Formula: 10574-69-3.

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

Oishi, Shunsuke; Saito, Susumu published the artcile< Double Molecular Recognition with Aminoorganoboron Complexes: Selective Alcoholysis of β-Dicarbonyl Derivatives>, Reference of 171877-39-7, the main research area is mol recognition aminoorganoboron complex chemoselective regioselective alcoholysis dicarbonyl derivative.

Aminoorganoboron (AOB) complexes recognize alc. and β-dicarbonyl units, and thereby facilitate chemo- and site-selective alcoholysis of the latter. The complex activates both reaction partners. This strategy enables C-C, C-N, and C-O bond cleavage in addition/elimination reactions under near neutral pH conditions and provides a new method for functional group conversions.

Angewandte Chemie, International Editionpublished new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), 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

Yamada, Shinji; Katsumata, Hiroko published the artcile< Asymmetric Acylation of sec-Alcohols with Twisted Amides Possessing Axial Chirality Induced by the Adjacent Asymmetric Center>, HPLC of Formula: 171877-39-7, the main research area is asym acylation secondary alc twisted amide axial chirality; desymmetrization meso diols twisted amide axial chirality.

This paper reports that axially chiral twisted amides serve as asym. acylating agents for sec-alcs. under neutral conditions. Kinetic resolution of various racemic sec-alcs. and desymmetrization of 1,2-, 1,3-, and 1,4-meso-diols were performed by using the twisted amides. The utility of this desymmetrization method was shown by the preparation of the synthetic intermediate for macrolide antibiotic nodusmicin and 18-deoxynargenicin. The stereoselectivity of the acylation reactions is significantly dependent on the bulkiness of both the acyl group and the C-4 substituent of the chiral auxiliary. When an amide possessing an imidazolyl group at C-4 was employed, the stereoselectivity was reversed to give R esters. A possible working model of the acylation reaction is also described on the basis of the structural studies of the twisted amides by IR and 1H and 13C NMR spectroscopies and AM1 calculations These studies suggested a rotamer that is thermodynamically more stable than the others. This rotamer has an axial chirality about its C(O)-N linkage that is induced by the adjacent chiral center. This would enable discrimination of the two enantiomeric hydroxy groups of the racemic alcs. or meso-diols.

Journal of Organic Chemistrypublished new progress about Absolute configuration. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, HPLC of Formula: 171877-39-7.

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

Demekhin, Oleg D.; Burov, Oleg N.; Kletskii, Mikhail E.; Lisovin, Anton V.; Kurbatov, Sergey V.; Bereznyak, Elena A.; Trishina, Alena V. published the artcile< New 13-vinyl derivatives of berberine: synthesis and characterization>, Synthetic Route of 10574-69-3, the main research area is electroneutral vinyl berberine preparation antibacterial SAR density functional theory.

The possibility of obtaining electroneutral substituted 13-vinylberberines I [R = H, CH2C(O)CH3; R1 = dicyanomethyl, 1,3-dimethoxy-1,3-dioxopropan-2-yl, 2,4,6-trioxo-1,3-diazinan-5-yl, etc.] was demonstrated exptl. and via quantum-chem. DFT/B3LYP calculations in the 6-31++G(d,p) basis set. The introduction of pharmacophoric fragments conjugated through vinyl moiety opened new possibilities for structural modification of berberine, enabling pronounced changes in tropicity toward supramol. biol. structures. The newly synthesized 13-vinylberberines I were stable in their reduced form due to significant intramol. electron d. transfer from berberine ring system to the vinyl moiety bearing electron-withdrawing groups. It was demonstrated that berberine derivatives I may exist not only in ion pair form consisting of organic cation and inorganic anion, but also as zwitterionic structures featuring significant intramol. charge transfer. The obtained 13-vinylberberines I exhibited biol. activity against the highly pathogenic Vibrio cholerae.

Chemistry of Heterocyclic Compounds (New York, NY, United States)published new progress about Active methylene compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Synthetic Route of 10574-69-3.

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

Feng, Xixi; Sippel, Claudia; Bracher, Andreas; Hausch, Felix published the artcile< Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands>, Synthetic Route of 171877-39-7, the main research area is crystal structure FKBP protein psychiatric metabolic disorder.

The FK506-binding protein 51 (FKBP51) is a promising drug target for the treatment of stress-related psychiatric or metabolic disorders. Just recently, the first selective ligands for FKBP51 were reported based on an induced fit mechanism, but they are too large for a further drug development process. The authors therefore designed and synthesized a novel series of selective ligands to explore the requirements necessary for binding to the induced-fit conformation. All ligands of this series show no binding toward the structurally very similar antitarget FKBP52. With the cocrystal structure of the best ligand in this novel series the authors confirmed the induced fit mechanism. Furthermore, the structure-affinity relationship provides information about beneficial structural features, which is valuable for the development of improved FKBP51-directed drugs.

Journal of Medicinal Chemistrypublished new progress about Crystal structure. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Synthetic Route of 171877-39-7.

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