Day: October 14, 2022

Bernier, Jean Luc; Houssin, Raymond; Henichart, Jean Pierre published the artcile< Analog of dolastatin 3. Synthesis, proton NMR studies, and spatial conformation>, COA of Formula: C12H18N2O4S, the main research area is dolastatin 3 analog preparation conformation.

Dolastatin 3 analog I was prepared by deblocking Boc-Pro-Leu-Val-(gly)Thz-(gly)Thz-ONSu (II; Boc = Me3CO2C, NSu = succinimido) by HBr/HOAc and cyclizing the resulting H-Pro-Leu-Val-(gly)Thz-(gly)Thz-ONSu.HBr in pyridine. Boc-Gly-NH2 underwent thionation via the Lawesson procedure to give Boc-Gly(S)-NH2, which was cyclized with CH3COCO2Et to give Boc-(gly)Thz-OEt (III). III was Boc-deblocked by HBr/HOAc to give H-(gly)Thz-OEt.HBr (IV), whereas III was saponified to give Boc-(gly)Thz-OH (V). V was coupled with IV by DCC/HOBt to give Boc-(gly)Thz-(gly)Thz-OEt, which was Boc-deblocked and then coupled with Boc-Pro-Leu-Val-OH by DCC/HOBt to give Boc-Pro-Leu-Val-(gly)Thz-(gly)Thz-OEt, which was converted into II. A spatial mol. conformation of I was proposed based on 1H NMR spectroscopy.

Tetrahedron published new progress about Cyclic peptides Role: SPN (Synthetic Preparation), PREP (Preparation). 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, COA of Formula: C12H18N2O4S.

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

Bansal, Akhil; Bali, Alka; Balaini, Ajitesh published the artcile< Synthesis and Evaluation of Substituted Aryl Thiazoles With Antioxidant Potential as Gastro-sparing Anti-inflammatory Agents>, COA of Formula: C9H7N3O2S, the main research area is antioxidant potential gastro sparing antiinflammatory agent aryl thiazole.

NSAIDs are used as first-line drugs for the treatment of various inflammatory disorders. Chronic use of NSAIDs is known to be associated with gastrointestinal and renal toxicity. Local generation of reactive oxygen species finally resulting in cellular apoptosis is one of the accepted mechanisms for NSAID-induced toxicity. The objective of the present study was to design and synthesize a series of 2-methane sulfonamido substituted arylthiazole derivatives by including structural features of combined antiulcer and anti-inflammatory activity utilizing as the structural core, thiazole nucleus with potential for antioxidant effect. Compounds were designed based on three dimensional and field similarity studies. The synthesized compounds were evaluated for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Rofecoxib and indomethacin were taken as standard drugs for comparison. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. The compounds 6 and 7 showed good anti-inflammatory activity comparable to the standard group and were also non ulcerogenic at the test doses. Compounds 1-7 displayed varying degrees of reducing power in the (PFRAP) assay and the methanesulfonamido derivatives 4-7 showed the highest antioxidant activity (EC50 values 3.7-5.1 μmol/mL vs ascorbic acid 7.4 μmol/mL). Theor. ADME profiling of the compounds based on selected physicochem. properties showed excellent compliance with Lipinski′s rule. A series of compounds have been designed and synthesized having dual antioxidant and anti-inflammatory activity with activities comparable to standard drugs.

Letters in Drug Design & Discovery published new progress about Anti-inflammatory agents. 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

Sinenko, V. O.; Slivchuk, S. R.; Pil’o, S. G.; Raenko, G. F.; Brovarets, V. S. published the artcile< Synthesis of new 1,3-thiazole derivatives from 2(5)-hydroxyalkyl-1,3-thiazole-5(2)-carbaldehydes>, Application of C10H9NOS2, the main research area is thiazole preparation; carbaldehyde thiazole acetoacetic ester urea Biginelli; phenylhydrazine isoniazid rhodanine thiazole carbaldehyde condensation.

Reactions of substituted 2-hydroxyalkyl-1,3-thiazole-5-carbaldehydes and 5-hydroxyalkyl-1,3-thiazole-2-carbaldehydes with phenylhydrazine, isoniazid, N-substituted rhodanines were performed as well as Biginelli reaction with acetoacetic ester and urea. As a result, new 1,3-thiazole derivatives were obtained. They are of interest as potential bioactive substances.

Russian Journal of General Chemistry published new progress about Aldehydes 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

Peixoto, Philippe A.; Richard, Jean-Alexandre; Severin, Rene; Chen, David Y.-K. published the artcile< Total Synthesis of Echinopines A and B: Exploiting a Bioinspired Late-Stage Intramolecular Cyclopropanation [Erratum to document cited in CA155:510334]>, COA of Formula: C10H11NS2, the main research area is erratum echinopine A B synthesis intramol cyclopropanation.

On page 5724, citations were omitted from reference 1; the omitted citations are given.

Organic Letters published new progress about Cycloisomerization. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, COA of Formula: C10H11NS2.

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

Ye, Sen; Hananya, Nir; Green, Ori; Chen, Hansen; Zhao, Angela Qian; Shen, Jiangang; Shabat, Doron; Yang, Dan published the artcile< A Highly Selective and Sensitive Chemiluminescent Probe for Real-Time Monitoring of Hydrogen Peroxide in Cells and Animals>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is Chemiluminescent probe hydrogen peroxide bioimaging imaging agent; bioimaging; chemiluminescence; fluorescent probes; hydrogen peroxide; imaging agents.

Selective and sensitive mol. probes for hydrogen peroxide (H2O2), which plays diverse roles in oxidative stress and redox signaling, are urgently needed to investigate the physiol. and pathol. effects of H2O2. A lack of reliable tools for in vivo imaging has hampered the development of H2O2 mediated therapeutics. By combining a specific tandem Payne/Dakin reaction with a chemiluminescent scaffold, H2O2-CL-510 was developed as a highly selective and sensitive probe for detection of H2O2 both in vitro and in vivo. A rapid 430-fold enhancement of chemiluminescence was triggered directly by H2O2 without any laser excitation. Arsenic trioxide induced oxidative damage in leukemia was successfully detected. In particular, cerebral ischemia-reperfusion injury-induced H2O2 fluxes were visualized in rat brains using H2O2-CL-510, providing a new chem. tool for real-time monitoring of H2O2 dynamics in living animals.

Angewandte Chemie, International Edition published new progress about Biological imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

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

Pil’o, S. G.; Brovarets, V. S.; Romanenko, E. A.; Drach, B. S. published the artcile< Reaction of 3,3-dichloro-2-[(dichloroacetyl)amino]acrylonitrile with amines>, Electric Literature of 10574-69-3, the main research area is oxazolecarbonitrile derivative preparation hydrolysis condensation reaction; polychlorinated enamidonitrile heterocyclization amine.

Polychlorinated enamidonitrile Cl2C:C(CN)NHCOCHCl2 readily reacts with primary aromatic amines, dialkylamines, piperidine, and morpholine. The reaction is accompanied by complete elimination of chlorine atoms as chloride ions with formation of 4-cyanooxazoles having the corresponding amine residue in position 5 of the ring and a CH:N or diaminomethyl moiety in position 2. The structure of 5-arylamino(dialkylamino)-4-cyano-2-formyloxazoles was confirmed by their acid hydrolysis, as well as by condensation with phenylhydrazine, N-alkylrhodanines, and Et acetoacetate in the presence of urea.

Russian Journal of General Chemistry (Translation of Zhurnal Obshchei Khimii) published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Electric Literature of 10574-69-3.

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

Zhu, Peng-Wei; Yang, Yan-Tong; Li, Yang; Zhu, Jie; Wu, Lei published the artcile< Electrochemical Oxidative C-H Phosphonylation of thiazole derivatives in ambient conditions>, HPLC of Formula: 20582-55-2, the main research area is electrochem oxidative phosphonylation thiazole green chem; organophosphorus phosphine oxide preparation green electrochem.

We herein report a direct electrochem. dehydrogenative C-H phosphonylation of thiazoles derivatives with H2 evolution. Employing electricity as the green and sole oxidant, cheap metal as electrode, the anodic oxidation together with cathodic hydrogen evolution process provides a green and efficient strategy for C-H phosphonylation. A diverse range of phosphorus products were constructed under external metal and oxidant-free conditions at ambient temperature, featuring atom economy, simple operation and wide reaction scope.

Molecular Catalysis published new progress about Electricity. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, HPLC of Formula: 20582-55-2.

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

Fang, Zhen; Liu, Yang; Zhang, Rong; Chen, Qiang; Wang, Tianqi; Yang, Wei; Fan, Yan; Yu, Chundong; Xiang, Rong; Yang, Shengyong published the artcile< Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D>, COA of Formula: C10H7NOS, the main research area is histone lysine demethylase KDM4D inhibitor arylpyrrolidinmethylphenol; 2-OG noncompetitive Inhibitor; Epigenetics; KDM4D; Structure-activity relationship.

Histone lysine demethylase 4D (KDM4D) plays an important role in the regulation of tumorigenesis, progression and drug resistance and has been considered a potential target for cancer treatment. However, there is still a lack of potent and selective KDM4D inhibitors. In this investigation, we report a new class of KDM4D inhibitors containing the 2-(aryl(pyrrolidine-1-yl)methyl)phenol scaffold, identified through AlphaLisa-based screening, structural optimization, and structure-activity relationship analyses. Among these inhibitors, 24s (I) was the most potent, with an IC50 value of 0.023 ± 0.004μM. This compound exhibited more than 1500-fold selectivity towards KDM4D vs. KDM4A as well as other JMJD subfamily members, indicating good selectivity for KDM4D. Kinetic anal. indicated that 24s did not occupy the 2-oxoglutarate binding pocket. In an in vitro assay, 24s significantly suppressed the proliferation and migration of colorectal cancer (CRC) cells. Overall, this study has identified a good tool compound to explore the biol. function of KDM4D and a good lead compound for drug discovery targeting KDM4D.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, COA of Formula: C10H7NOS.

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

Yan, Gang; Hao, Lina; Niu, Yan; Huang, Wenjie; Wang, Wei; Xu, Fengrong; Liang, Lei; Wang, Chao; Jin, Hongwei; Xu, Ping published the artcile< 2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies>, Application In Synthesis of 57493-24-0, the main research area is thiazolyl imidazolyl acetamide preparation mol docking BACE1 inhibitor human; Alzheimer’s disease; BACE-1 inhibitors; BBB; Docking study; PAMPA; Permeability; Surface Plasmon Resonance (SPR).

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives, I (R1 = Ph, 4-MeC6H4, 2-O2NC6H4, etc.; R2 = 2-MeOC6H4,3-MeOC6H4, 4-MeOC6H4, 3-EtOC6H4), II (R3 = Ph, 3,5-Cl2-4-NH2Ph; R4 = 3-MeOPh, 3-EtOPh), were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biol. evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog II (R3 = Ph; R4 = 3-EtOC6H4) (IC50 = 4.6 μM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.

European Journal of Medicinal Chemistry published new progress about Alzheimer disease. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application In Synthesis of 57493-24-0.

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

Crimmins, Michael T.; Christie, Hamish S.; Hughes, Colin O. published the artcile< Synthesis and diastereoselective aldol reactions of a thiazolidinethione chiral auxiliary>, Category: thiazole, the main research area is thiazolidinethione chiral auxiliary; propanoyl thiazolidinethione syn aldol.

Thiazolidinethione chiral auxiliary I (R = H) is prepared from (S)-phenylalaninol and carbon disulfide. Propanoylated I [R = C(O)CH2CH3] can be used for either Evans syn aldol reactions or non-Evans syn aldol reactions with a variety of aldehydes, in good yield with good stereoselectivity.

Organic Syntheses published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Category: thiazole.

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