Author: tianli

Roe, Caroline; Hobbs, Heather; Stockman, Robert A. published the artcile< One-Pot Synthesis of Chiral Nonracemic Amines>, Computed Properties of 1003-32-3, the main research area is chiral nonracemic amine preparation green chem; sulfinamide preparation green chem; oxathiazolidine oxide.

One-pot five-component reactions of oxathiazolidine-S-oxides with mesitylmagnesium bromide, lithium bis(trimethylsilyl)amide, aldehydes and Grignard reagents afford chiral nonracemic amines or sulfinamides in good yields and high stereoselectivities.

Journal of Organic Chemistry published new progress about Amines Role: SPN (Synthetic Preparation), 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

Li, Fuying; Zhu, Qingzhang; Zhang, Yi; Feng, Ying; Leng, Ying; Zhang, Ao published the artcile< Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators>, Category: thiazole, the main research area is antidiabetic glucokinase activator thiazole arylacetamide derivative.

A series of N-thiazole substituted arylacetamides were designed on the basis of metabolic mechanism of the aminothiazole fragment as glucokinase (GK) activators for the treatment of type 2 diabetes. Instead of introducing a substituent to block the metabolic sensitive C-5 position on the thiazole core directly, a wide variety of C-4 or both C-4 and C-5 substitutions were explored. Compound R-9k bearing an iso-Pr group as the C-4 substituent was found possessing the highest GK activation potency with an EC50 of 0.026 μM. This compound significantly increased both glucose uptake and glycogen synthesis in rat primary cultured hepatocytes. Moreover, single oral administration of compound R-9k exerted significant reduction of blood glucose levels in both ICR and ob/ob mice. These promising results indicated that compound R-9k is a potent orally active GK activator, and is warranted for further investigation as a new anti-diabetic treatment.

Bioorganic & Medicinal Chemistry published new progress about Antidiabetic agents. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Category: thiazole.

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

Seganish, W. Michael; Bercovici, Ana; Ho, Ginny D.; Loozen, Hubert J. J.; Timmers, Cornelis M.; Tulshian, Deen published the artcile< A synthesis of dihydroimidazo[5,1-a]isoquinolines using a sequential Ugi-Bischler-Napieralski reaction sequence>, Application In Synthesis of 1003-32-3, the main research area is isonitrile aldehyde carboxylate ammonia sequential Ugi Bischler Napieralski; hydroimidazoisoquinoline preparation.

A flexible route to analogs of dihydroimidazo[5,1-a]isoquinolines was described. The synthesis hinges on a sequential Ugi coupling, followed by a Bischler-Napieralski reaction to form the imidazole-isoquinoline core. This route facilitates the introduction of a range of substitutions throughout the C framework.

Tetrahedron Letters published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Application In Synthesis of 1003-32-3.

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

Moody, Christopher J.; Bagley, Mark C. published the artcile< Total synthesis of (+)-nostocyclamide>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is nostocyclamide total synthesis.

A total synthesis of the naturally occurring macrocyclic bisthiazole-oxazole nostocyclamide is described.

Synlett published new progress about 96929-05-4. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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

Nagaladinne, Nizamuddin; Abdul Ahad, Hindustan; Nayakanti, Devanna published the artcile< Design, synthesis and molecular modelling studies of 1-methyl-3-(4-substituted phenyl-1,3- thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazolin-4(1H)-ones as potent anticancer agents>, Product Details of C9H7N3O2S, the main research area is methyl phenyl thiazolyl pyridinyl dihydroquinazolinone preparation antitumor SAR ADMET; mol modeling methyl phenyl thiazolyl pyridinyl dihydroquinazolinone preparation.

The present study involved the design, synthesis, characterization and mol. docking studies of biol. active 1-methyl-3-(4-substituted phenyl-1,3-thiazol-2-yl)-2-(pyridin-3-yl)-2,3-dihydroquinazoline-4-(1H)-ones I [R = 2-OH, 3-NH2, 4-Cl, etc.] which were synthesized by condensation of 2-amino-4-substituted phenylthiazoles with N-methylbenzoxazin-4-one. The N-methylbenzoxazin-4-one and 2-amino-4-substituted phenylthiazoles were synthesized from N-methylanthranilic acid with pyridine3-carboxylic acid and substituted aldehydes with thiourea, resp. The ADME properties determined the synthetic accessibility of compounds I by in silico Swiss ADME. The colorectal anticancer screening of compounds I was done by using cell HT-29 human colorectal adenocarcinoma based on mol. docking studies on 3GC7-the structure of p38alpha in complex with dihydroquinazolinone. Finally, compounds I [R = 4-Me, 3-NH2, 2,4-(OH)2, 2,4-(Cl)2] exhibited better activity at a concentration < 10μg/mL when compared to 5-fluorouracil. The ADME properties revealed that all the compounds I were within the range and docking studies showed the highest binding with glide score -7.19 and -7.027 Kcal/mol compared to the target protein -10.67 Kcal/mol. Asian Journal of Chemistry published new progress about Antitumor agents. 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

Barton, Anne; Breukelman, Stephen P.; Kaye, Perry T.; Meakins, G. Denis; Morgan, David J. published the artcile< The preparation of thiazole-4- and -5-carboxylates, and an infrared study of their rotational isomers>, Safety of Ethyl 4-methylthiazole-5-carboxylate, the main research area is cyclocondensation thiourea bromomethyloxopentanoate; isobutyraldehyde chloroacetate cyclocondensation thiourea; aminoispropylthiazolecarboxylate methyl; butylthiazolecarboxylate ethyl; thiazolecarboxylate preparation rotational isomerism IR.

A general procedure is reported for the preparation of thiazole-4- and -5-carboxylates containing alkyl and halo substituents. Treatment of Me2CHCHO and Cl2CHCO2Me with NaOMe in Et2O at 0°, followed by addition of (H2N)2CS and 4 h reflux in MeOH gave the aminothiazole I. The thiazole II was prepared by treatment of EtO2CCHBrCOCMe3 with (H2N)2CS in refluxing EtOH for 1 h, followed by deamination with NaNO2-H3PO2. Both series of esters show IR carbonyl doublets caused by rotational isomerism; the more intense absorptions of the 4-carboxylates are at lower wave number, whereas those of the 5-carboxylates are the higher wave number component. In both series, the stronger bands arise from the thermochem. more stable forms. For the 4-carboxylates, these forms are the carbonyl O,S-syn-s-trans-rotamers.

Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Safety of Ethyl 4-methylthiazole-5-carboxylate.

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

Endo, Mizuki; Ozawa, Takeaki published the artcile< Advanced bioluminescence system for in vivo imaging with brighter and red-shifted light emission>, SDS of cas: 2591-17-5, the main research area is review luciferase luciferin bioluminescence resonance energy transfer; bioluminescence; bioluminescence resonance energy transfer; luciferase; luciferin.

A review. In vivo bioluminescence imaging (BLI), which is based on luminescence emitted by the luciferase-luciferin reaction, has enabled continuous monitoring of various biochem. processes in living animals. Bright luminescence with a high signal-to-background ratio, ideally red or near-IR light as the emission maximum, is necessary for in vivo animal experiments Various attempts have been undertaken to achieve this goal, including genetic engineering of luciferase, chem. modulation of luciferin, and utilization of bioluminescence resonance energy transfer (BRET). In this review, we overview a recent advance in the development of a bioluminescence system for in vivo BLI. We also specifically examine the improvement in bioluminescence intensity by mutagenic or chem. modulation on several beetle and marine luciferase bioluminescence systems. We further describe that intramol. BRET enhances luminescence emission, with recent attempts for the development of red-shifted bioluminescence system, showing great potency in in vivo BLI. Perspectives for future improvement of bioluminescence systems are discussed.

International Journal of Molecular Sciences published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

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

Kikelj, D.; Urleb, U. published the artcile< Product class 17: thiazoles>, Quality Control of 96929-05-4, the main research area is review thiazole preparation.

A review of synthetic methods to prepare thiazoles as well as reactive modifications of thiazole moieties.

Science of Synthesis published new progress about Cyclization. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Quality Control of 96929-05-4.

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>, Quality Control of 57493-24-0, 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, Quality Control 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>, SDS of cas: 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, SDS of cas: 171877-39-7.

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