Day: October 14, 2022

Qin, Xurong; Feng, Boya; Dong, Jiaxing; Li, Xiaoyu; Xue, Ying; Lan, Jingbo; You, Jingsong published the artcile< Copper(II)-catalyzed dehydrogenative cross-coupling between two azoles>, Category: thiazole, the main research area is biazole preparation; azole dehydrogenative coupling copper catalyst.

The copper(II)-catalyzed dehydrogenative coupling between two different azoles for the preparation of unsym. biazoles e. g., I has been developed. The current catalytic system can effectively control the chemoselectivity for heterocoupling over homocoupling.

Journal of Organic Chemistry published new progress about Heterocyclic compounds, nitrogen-oxygen Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Category: thiazole.

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

Saito-Moriya, Ryohei; Nakayama, Jun; Kamiya, Genta; Nobuo Kitada; Obata, Rika; Maki, Shojiro A.; Aoyama, Hiroshi published the artcile< How to select firefly luciferin analogues for in vivo imaging>, Application of C11H8N2O3S2, the main research area is review bioluminescence firefly luciferin analog imaging; bioluminescence imaging; high sensitivity; luciferase; luciferin analogue; multicolor; near-infrared light.

A review. Bioluminescence reactions are widely applied in optical in vivo imaging in the life science and medical fields. Such reactions produce light upon the oxidation of a luciferin (substrate) catalyzed by a luciferase (enzyme), and this bioluminescence enables the quantification of tumor cells and gene expression in animal models. Many researchers have developed single-color or multicolor bioluminescence systems based on artificial luciferin analogs and/or luciferase mutants, for application in vivo bioluminescence imaging (BLI). In the current review, we focus on the characteristics of firefly BLI technol. and discuss the development of luciferin analogs for high-resolution in vivo BLI. In addition, we discuss the novel luciferin analogs TokeOni and seMpai, which show potential as high-sensitivity in vivo BLI reagents.

International Journal of Molecular Sciences published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

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

Yu, Ming; Lizarzaburu, Mike; Motani, Alykhan; Fu, Zice; Du, Xiaohui; Liu, Jiwen; Jiao, Xianyun; Lai, SuJen; Fan, Peter; Fu, Angela; Liu, Qingxiang; Murakoshi, Michiko; Nara, Futoshi; Oda, Kozo; Okuyama, Ryo; Reagan, Jeff D.; Watanabe, Nobuaki; Yamazaki, Mami; Xiong, Yumei; Zhang, Ying; Zhuang, Run; Lin, Daniel C.-H.; Houze, Jonathan B.; Medina, Julio C.; Li, Leping published the artcile< Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies>, SDS of cas: 1003-32-3, the main research area is amrinone phenylalanine carboxylic acid preparation GPR142 agonist structure design; pharmacokinetics bioavailability diabetes amrinone phenylalanine carboxylic acid antidiabetic prodrug; glucose tolerance insulin secretagogue human islet transplant CYP450 hERG; GPR142 agonist; aminopyrazole−phenylalanine; human islet transplant; insulin secretagogue; oral glucose tolerance test; prodrug; type 2 diabetes.

Herein, we report the lead optimization of amrinone-phenylalanine based GPR142 agonists. Structure-activity relationship studies led to the discovery of aminopyrazole-phenylalanine carboxylic acid I, which exhibited good agonistic activity, high target selectivity, desirable pharmacokinetic properties, and no cytochrome P 450 or hERG liability. Compound I, together with its orally bioavailable Et ester prodrug II, were found to be suitable for in vivo proof-of-concept studies. Compound II displayed good efficacy in a mouse oral glucose tolerance test (OGTT). CompoundI showed GPR142 dependent stimulation of insulin secretion in isolated mouse islets and demonstrated a statistically significant glucose lowering effect in a mouse model bearing transplanted human islets.

ACS Medicinal Chemistry Letters published new progress about Antidiabetic agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, SDS of cas: 1003-32-3.

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

Shvets, A. A.; Nelyubina, Yu. V.; Lyssenko, K. A.; Kurbatov, S. V. published the artcile< Synthesis of bis-spiro-fused thiapyrrolizidinooxindoles by 1,3-dipolar cycloaddition>, Product Details of C10H9NOS2, the main research area is thiaproline azomethine ylide arylidenerhodanine regioselective diastereoselective dipolar cycloaddition; spiro thiapyrrolizidine oxindole regioselective diastereoselective preparation.

The 1,3-dipolar cycloaddition of an unstabilized azomethine ylide, generated in situ from isatin and thiaproline, to arylidene derivatives of rhodanine affords bis-spiro-fused thiapyrrolizidinooxindoles. The 1,3-dipolar addition reactions under consideration are fully regio- and diastereoselective.

Russian Chemical Bulletin published new progress about 1,3-Dipolar cycloaddition reaction (stereoselective). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Product Details of C10H9NOS2.

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

Yu, Mohan; Liu, Ya-Jun published the artcile< Same Luciferin in Different Luciferases Emitting Different-Color Light. A Theoretical Study on Beetle Bioluminescence>, Electric Literature of 2591-17-5, the main research area is luciferase bioluminescence luciferin Phrixotrix.

Bioluminescent beetles, firefly, click beetle, and railroad worm, naturally emit different-color light via the identical luciferin and bioluminescence (BL) mechanisms. Railroad worm especially emits two colors of light in its dorsal-lateral and cephalic lanterns. Four computational models of bioluminophore (oLu) in luciferases of red-emitting, yellow-green-emitting, red-emitting with addnl. loop, and red-emitting without C-terminal were built in this paper. To unveil the details of this luciferase effect at the mol. and electronic-state levels, second-order multiconfigurational perturbation calculations were performed following mol. dynamic simulations and time-dependent d. functional calculations for the above four oLu-luciferase systems. Via a systematic anal. on properties of oLu at the first singlet state (S1-oLu) in different luciferases, one clearly see the details of the microenvironment and secondary structure of luciferase affecting the excited-state property of S1-oLu, which ultimately result in the variant color of light emission. Typically, the increase in charge transfer of S1-oLu leads to the longer wavelength BL.

Journal of Chemical Theory and Computation published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Electric Literature of 2591-17-5.

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

Zaveri, Mehul; Kawathekar, Neha published the artcile< Synthesis, characterization and antimalarial activity of some new 3-benzyl-2-thioxothiazolidin-4-one derivatives>, Category: thiazole, the main research area is benzyl thioxothiazolidinone preparation antimalarial.

In present investigation, a series of new 3-benzyl-2-thioxothiazolidin-4-one I (Ar = Ph, 2-pyrrolyl, 4-pyridyl, etc.) derivatives, have been synthesized using conventional and microwave-assisted technique. These compounds were evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum. The result of antimalarial activity revealed that six compounds I (Ar = Ph, 2-furanyl, 2-pyridyl, 4-pyridyl, 4-Me2NC6H4, 2-HOC6H4) exhibited IC50 values ranging from 0.8-1.2 μg/mL, four compounds I (Ar = 4-ClC6H4, 4-FC6H4, 2-indolyl, 3-O2NC6H4) displayed antimalarial activity IC50 values in the range of 0.7-0.8 μg/mL. Compound I (Ar = 2-pyrrolyl) showed most significant result with maximum IC50 value of 0.7 μg/mL, thus it could be identified as structural lead for further development of new antimalarial agents.

International Journal of Pharmacy and Pharmaceutical Research published new progress about Antimalarials. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Category: thiazole.

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>, Synthetic Route of 57493-24-0, 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 Technology published 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, Synthetic Route of 57493-24-0.

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