Day: October 17, 2022

Farmer, Luc J.; Bemis, Guy; Britt, Shawn D.; Cochran, John; Connors, Martin; Harrington, Edmund M.; Hoock, Thomas; Markland, William; Nanthakumar, Suganthini; Taslimi, Paul; Ter Haar, Ernst; Wang, Jian; Zhaveri, Darshana; Salituro, Francesco G. published the artcile< Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)>, Electric Literature of 20582-55-2, the main research area is pyrimidine phenylamino thiazolyl derivative preparation tyrosine kinase inhibition SAR; phenylamino pyrimidine thiazole derivative preparation mast cell degranulation inhibition.

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead, I, were prepared and evaluated for biol. activity. Lead optimization provided compounds with nanomolar Ki’s against SYK and potent inhibition in mast cell degranulation assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Animal gene, c-src Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Electric Literature of 20582-55-2.

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

Bi, Huihua; Zhou, Yu; Jiang, Wei; Liu, Jie published the artcile< Electrophotocatalytic C-H Hydroxyalkylation of Heteroaromatics with Aldehydes>, Synthetic Route of 20582-55-2, the main research area is heteroarene electrochem photochem Minisci hydroxyalkylation aldehyde; alc heteroaryl preparation.

A radical hydroxyalkylation of N-heteroaromatics with aldehydes is reported. The constructive merging of photochem. and electrochem. is the key for the success of this atom-economical Minisci method. This protocol highlights the utility of electrophotocatalysis to promote a practical and general synthesis of secondary alcs. in good yields from readily available N-heteroaromatics and aldehydes under mild reaction conditions.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Synthetic Route of 20582-55-2.

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

Zielonka, Jacek; Podsiadly, Radoslaw; Zielonka, Monika; Hardy, Micael; Kalyanaraman, Balaraman published the artcile< On the use of peroxy-caged luciferin (PCL-1) probe for bioluminescent detection of inflammatory oxidants in vitro and in vivo - Identification of reaction intermediates and oxidant-specific minor products>, HPLC of Formula: 115144-35-9, the main research area is inflammatory oxidant bioluminescence probe peroxy caged luciferin; Bioluminescence; Boronate probes; Luciferin; Spin traps.

Peroxy-caged luciferin (PCL-1)(I) probe was first used to image hydrogen peroxide in living systems (Van de Bittner et al., 2010 [9]). Recently this probe was shown to react with peroxynitrite more potently than with hydrogen peroxide (Sieracki et al., 2013 [11]) and was suggested to be a more suitable probe for detecting peroxynitrite under in vivo conditions. In this work, we investigated in detail the products formed from the reaction between PCL-1 and hydrogen peroxide, hypochlorite, and peroxynitrite. HPLC anal. showed that hydrogen peroxide reacts slowly with PCL-1, forming luciferin as the only product. Hypochlorite reaction with PCL-1 yielded significantly less luciferin, as hypochlorite oxidized luciferin to form a chlorinated luciferin. Reaction between PCL-1 and peroxynitrite consists of a major and minor pathway. The major pathway results in luciferin and the minor pathway produces a radical-mediated nitrated luciferin. Radical intermediate was characterized by spin trapping. We conclude that monitoring of chlorinated and nitrated products in addition to bioluminescence in vivo will help identify the nature of oxidant responsible for bioluminescence derived from PCL-1.

Free Radical Biology & Medicine published new progress about Bioluminescence. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, HPLC of Formula: 115144-35-9.

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

Nath, J. P.; Dash, Manjula; Satrusallya, S. C.; Mahapatra, G. N. published the artcile< Synthesis of some 7-substituted 8-hydroxyquinoline derivatives of thiazoles and oxazoles as potential pesticides>, Safety of 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is hydroxyquinoline fungicide bactericide pesticide preparation; aminomethylhydroxyquinoline thiazolyl oxazolyl; Mannich hydroxyquinoline.

Mannich reaction of 8-hydroxyquinoline with PhCHO and I (R = H, Cl, Br; R1 = Ph, 4-ClC6H4, 4-BrC6H4, 4-HOC6H4, 4-MeO(C6H4, 3-O2NC6H4, 4-O2NC6H4, 4-MeC6H4, α-,β-naphthyl; X = O, S) gave the title compounds (II). II showed bactericidal and fungicidal activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Fungicides. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Safety of 2-Amino-4-(3-nitrophenyl)thiazole.

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

Patel, Snahel; Harris, Seth F.; Gibbons, Paul; Deshmukh, Gauri; Gustafson, Amy; Kellar, Terry; Lin, Han; Liu, Xingrong; Liu, Yanzhou; Liu, Yichin; Ma, Changyou; Scearce-Levie, Kimberly; Ghosh, Arundhati Sengupta; Shin, Young G.; Solanoy, Hilda; Wang, Jian; Wang, Bei; Yin, Jianping; Siu, Michael; Lewcock, Joseph W. published the artcile< Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)>, Application In Synthesis of 324579-90-0, the main research area is preparation pyrazolylpyridinamine leucine zipper kinase inhibitor.

Recent data suggest that inhibition of dual leucine zipper kinase (DLK, MAP3K12) has therapeutic potential for treatment of a number of indications ranging from acute neuronal injury to chronic neurodegenerative disease. Thus, high demand exists for selective small mol. DLK inhibitors with favorable drug-like properties and good CNS penetration. Herein the authors describe a shape-based scaffold hopping approach to convert pyrimidine 1 to a pyrazole core with improved physicochem. properties. The authors also present the first crystal structures of DLK. By utilizing a combination of property and structure-based design, the authors identified inhibitor I, a potent, selective, and brain-penetrant inhibitor of DLK with activity in an in vivo nerve injury model.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Application In Synthesis of 324579-90-0.

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

Zhu, Yan-Ping; Yuan, Jing-Jing; Zhao, Qin; Lian, Mi; Gao, Qing-He; Liu, Mei-Cai; Yang, Yan; Wu, An-Xin published the artcile< I2/CuO-catalyzed tandem cyclization strategy for one-pot synthesis of substituted 2-aminothiazole from easily available aromatic ketones/α,β-unsaturated ketones and thiourea>, Category: thiazole, the main research area is aminothiazole preparation thiourea aromatic ketone butenone cyclization.

A concise and efficient one-pot process from easily available Me ketones or unsaturated Me ketones and thiourea was developed for the synthesis of 2-aminothiazoles with I2/CuO as catalyst. The method gave the E-isomers of 4-ethenyl-2-aminothiazoles. All these target mols. were characterized by NMR, HRMS and IR spectra.

Tetrahedron published new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Category: thiazole.

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

Kitir, Betul; Baldry, Mara; Ingmer, Hanne; Olsen, Christian A. published the artcile< Total synthesis and structural validation of cyclodepsipeptides solonamide A and B>, Name: (S)-4-Benzylthiazolidine-2-thione, the main research area is cyclodepsipeptide solonamide A B total enantioselective synthesis antimicrobial; macrocycle virulence gene expression Staphylococcus aureus inhibitor cyclodepsipeptide; hydroxy acid stereoselective aldol reaction esterification acylation macrolactamization.

Microorganisms are an attractive source of new natural products with antimicrobial properties, and the marine environment constitutes a prolific resource of bioactive microorganisms. During a global research expedition (Galathea III), two depsipeptides, solonamide A and solonamide B, were isolated from the marine bacterium Photobacterium halotolerance and were found to inhibit virulence gene expression in the serious human pathogen, Staphylococcus aureus. They act by interfering with the agr quorum sensing system and show resemblance to the endogenous S. aureus quorum sensing peptide, autoinducing peptide I (AIP-I). To enable more comprehensive studies, we embarked on the chem. synthesis of solonamides A and B. The key synthetic steps were formation of the (R)-β-hydroxy-fatty-acids by stereoselective aldol reactions and a cyclative macrolactamization, which proceeded under highly dilute conditions. Thus, the first total syntheses of the solonamides corroborated the originally assigned structures, and by changing the stereochem. of the auxiliary in the aldol steps we gained access to the natural products as well as their β3-epimers.

Tetrahedron published new progress about Acylation. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Name: (S)-4-Benzylthiazolidine-2-thione.

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

Brito, Camila C. Bitencourt; Carneiro da Silva, Helder Vinicius; Brondani, Daci Jose; Rodolfo de Faria, Antonio; Ximenes, Rafael Matos; Mangueira da Silva, Ivanildo; de Albuquerque, Julianna F. C.; Castilho, Marcelo Santos published the artcile< Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors>, HPLC of Formula: 57493-24-0, the main research area is thiazole derivative preparation LbSOD inhibitor Leishmaniasis; Leishmania; superoxide dismutase; thermal shift assay; thiazole derivatives.

Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geog. distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites and human host. Despite the differences between SOD of Leishmania braziliensis and human make this enzyme a promising target for drug development efforts. No medicinal chem. effort has been made to identify LbSOD inhibitors. Herein, we show that thermal shift assays (TSA) and fluorescent protein-labeled assays (FPLA) can be employed as primary and secondary screens to achieve this goal. Moreover, we show that thiazole derivatives bind to LbSOD with micromolar affinity.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Leishmaniasis. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, HPLC of Formula: 57493-24-0.

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

Isbrandt, Eric S.; Nasim, Amrah; Zhao, Karen; Newman, Stephen G. published the artcile< Catalytic Aldehyde and Alcohol Arylation Reactions Facilitated by a 1,5-Diaza-3,7-diphosphacyclooctane Ligand>, Related Products of 1003-32-3, the main research area is aryl iodide aldehyde nickel diazadiphosphacyclooctane catalyst reductive Heck arylation; primary alc aryliodide nickel diazadiphosphacyclooctane catalyst reductive Heck arylation; secondary alc preparation.

A catalytic method to access secondary alcs. by the coupling of aryl iodides was reported. Either aldehydes or alcs. can be used as reaction partners, making the transformation reductive or redox-neutral, resp. The reaction was mediated by a Ni catalyst and a 1,5-diaza-3,7-diphosphacyclooctane. This P2N2 ligand, which was previously been unrecognized in cross-coupling and related reactions, was found to avoid deleterious aryl halide reduction pathways that dominate with more traditional phosphines and NHCs. An interrupted carbonyl-Heck type mechanism was proposed to be operative, with a key 1,2-insertion step forging the new C-C bond and forming a nickel alkoxide that may be turned over by an alc. reductant. The same catalyst was also found to enable synthesis of ketone products from either aldehydes or alcs., demonstrating control over the oxidation state of both the starting materials and products.

Journal of the American Chemical Society published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Related Products of 1003-32-3.

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

Mann, Joseph L.; Grosskopf, Abigail K.; Smith, Anton A. A.; Appel, Eric A. published the artcile< Highly Branched Polydimethylacrylamide Copolymers as Functional Biomaterials>, Application of C3H5NS2, the main research area is branched polydimethylacrylamide copolymer biomaterial.

Controlled radical polymerization of vinyl monomers with multivinyl cross-linkers leads to the synthesis of highly branched polymers with controlled spatial d. of functional chain ends. The resulting polymers synthesized in this manner have large dispersities resulting from a mixture of unreacted primary chains, low mol. weight branched species, and high mol. weight highly branched species. Through the use of fractional precipitation, we present a synthetic route to high mol. weight highly branched polymers that are absent of low mol. weight species and that contain reactivity toward amines for controlled postpolymn. modification. The controlled spatial d. of functional moieties on these high mol. weight macromol. constructs enable new functional biomaterials with the potential for application in regenerative medicine, immunoengineering, imaging, and controlled drug delivery.

Biomacromolecules published new progress about Biocompatibility. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application of C3H5NS2.

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