Author: tianli

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

Muthyala, Manoj Kumar; Kumar, Anil published the artcile< A novel and efficient one pot synthesis of 2,4-disubstituted thiazoles and oxazoles using phenyltrimethylammonium tribromide in ionic liquid>, COA of Formula: C9H7N3O2S, the main research area is amide ketone cyclization phenylmethylammonium tribromide ionic liquid; urea ketone cyclization phenylmethylammonium tribromide ionic liquid; oxazole green preparation; thiazole green preparation.

A novel and efficient 1-pot procedure was described for synthesis of 2,4-disubstituted thiazoles and oxazoles from substituted ketones using phenyltrimethylammonium tribromide as in-situ brominating agent followed by reaction with thioamide/thiourea and amides/ureas, resp. in [bmim][BF4] ionic liquid The advantages of the procedure include avoiding the handling of lacrymetric compounds and hazardous and toxic organic solvents along with good to excellent yields of the products.

Journal of Heterocyclic Chemistry published 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

Felts, Andrew S.; Rodriguez, Alice L.; Morrison, Ryan D.; Blobaum, Anna L.; Byers, Frank W.; Daniels, J. Scott; Niswender, Colleen M.; Conn, P. Jeffrey; Lindsley, Craig W.; Emmitte, Kyle A. published the artcile< Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5>, Name: 4-Cyclopropylthiazol-2-amine, the main research area is pyrimidinylmethylquinolinecarboxamide preparation neg allosteric modulator glutamate receptor mGluR5; Central nervous system (CNS); G protein-coupled receptor (GPCR); Metabotropic glutamate receptor subtype 5 (mGlu(5)); Negative allosteric modulator (NAM); Quinoline.

Based on previous work that established fused heterocycles as viable alternatives for the picolinamide core of the authors’ lead series of mGlu5 neg. allosteric modulators (NAMs), the authors designed a novel series of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide mGlu5 NAMs. These new quinoline derivatives also contained carbon linkers as replacements for the diaryl ether oxygen atom common to the authors’ previously published chemotypes. Compounds were evaluated in a cell-based functional mGlu5 assay, and an exemplar analog 27 (6-(difluoro(pyrimidin-5-yl)methyl)-N-(4-methylthiazol-2-yl)quinoline-8-carboxamide) was >60-fold selective vs. the other seven mGlu receptors. Selected compounds were also studied in metabolic stability assays in rat and human S9 hepatic fractions and exhibited a mixture of P 450- and non-P 450-mediated metabolism

Bioorganic & Medicinal Chemistry Letters published new progress about Allosterism. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Name: 4-Cyclopropylthiazol-2-amine.

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

Morciano, Giampaolo; Imamura, Hiromi; Patergnani, Simone; Pedriali, Gaia; Giorgi, Carlotta; Pinton, Paolo published the artcile< Measurement of ATP concentrations in mitochondria of living cells using luminescence and fluorescence approaches>, Reference of 2591-17-5, the main research area is ATP; Bioluminescence; Biosensor; FRET; Fluorescence; Live cell imaging; Luciferase assay; Mitochondria.

Adenosine 5′-triphosphate (ATP) is the central metabolite in the energy metabolism of cells and is hydrolyzed to ADP and inorganic phosphate to provide free energy in various cellular processes. ATP also functions as an intracellular signaling mol. Thus, it is important to know the ATP concentration within cells to understand cellular activities. Here, we describe two methods to detect ATP concentrations in the cytoplasm and mitochondrial matrix using genetically encoded luminescent or fluorescent biosensors. These methods enable quant. investigation of ATP concentration dynamics in living cells, single cells and cell populations.

Methods in Cell Biology published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Reference of 2591-17-5.

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

Fu, Xiao-Pu; Xuan, Qing-Qing; Liu, Li; Wang, Dong; Chen, Yong-Jun; Li, Chao-Jun published the artcile< Dual C-H activations of electron-deficient heteroarenes: palladium-catalyzed oxidative cross coupling of thiazoles with azine N-oxides>, Quality Control of 20582-55-2, the main research area is palladium catalyst oxidative cross coupling thiazole azine oxide; thiazolylpyridine oxide preparation.

The palladium-catalyzed, copper-promoted cross-dehydrogenative-coupling (CDC) of electron-deficient thiazoles with azine N-oxides through dual C-H activations was developed. It was found that copper(II) pivalate was an efficient dual-function reagent for the oxidative cross-coupling reactions, playing the roles of both an oxidant and a C-H bond activation promoter. E.g., in presence of Pd(OAc)2 and copper(II) pivalate, oxidative coupling of pyridine N-oxide and 6-methylbenzothiazole gave 70% 2-thiazolylpyridine derivative (I). This methodol. provides a simple way to construct the 2-thiazolylpyridine moiety.

Tetrahedron published new progress about Isotope effect. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Quality Control of 20582-55-2.

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

Wu, Xiongyu; Oehrngren, Per; Ekegren, Jenny K.; Unge, Johan; Unge, Torsten; Wallberg, Hans; Samuelsson, Bertil; Hallberg, Anders; Larhed, Mats published the artcile< Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic. [Erratum to document cited in CA148:321837]>, Safety of 4-(Thiazol-2-yl)benzaldehyde, the main research area is erratum tertiary alc derivative crystal structure HIV1 protease inhibitor; tertiary alc derivative preparation HIV1 protease inhibitor erratum.

A printing problem relating to Scheme 3 on page 1055 resulted in the following errors; The corrected manuscript was reposted on March 14, 2008. On page 1054, left column, lines 29-30, 34-35, and 37-38, and in the right column, line 4, should indicated “”Scheme 3″” instead of “”Scheme UNDEFINED: PLEASE CHECK””. On page 1054, right column, line 5 ia the title to Scheme 3 appearing on page 1055; line 6-13 are the footnotes to Scheme 3. On page 1055, Table 1 should be in the right column while Scheme 3 should be in the left with the title “”Scheme 3. Synthesis of Inhibitors 12a-w and 13-15″” with its footnotes.

Journal of Medicinal Chemistry published new progress about AIDS (disease). 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Safety of 4-(Thiazol-2-yl)benzaldehyde.

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

Jin, Minye; Glaeser, Alisa; Paez, Julieta I. published the artcile< Redox-triggerable firefly luciferin-bioinspired hydrogels as injectable and cell-encapsulating matrices>, Product Details of C11H8N2O3S2, the main research area is luciferin bioinspired hydrogel injectable cell encapsulating matrix.

Stimuli-responsive hydrogels are smart materials that respond to variations caused by external stimuli and that are currently exploited for biomedical applications such as biosensing, drug delivery and tissue engineering. The development of stimuli-responsive hydrogels with defined user control is relevant to realize materials with advanced properties. Recently, our group reported firefly luciferin-inspired hydrogel matrixes for 3D cell culture. This platform exhibited advantages like rapid gelation rate and tunability of mech. and biol. properties. However, this first mol. design did not allow fine control of the gelation onset, which restricts application as a cell-encapsulating matrice with injectable and processable properties. In this article, we endow the firefly luciferin-inspired hydrogels with redox-triggering capability, to overcome the limitations of the previous system and to widen its application range. We achieve this goal by introducing protected macromers as hydrogel polymeric precursors that can be activated in the presence of a mild reductant, to trigger gel formation in situ with a high degree of control. We demonstrate that the regulation of mol. parameters (e.g., structure of the protecting group, reductant type) and environmental parameters (e.g., pH, temperature) of the deprotection reaction can be exploited to modulate materials properties. This redox-triggerable system enables precise control over gelation onset and kinetics, thus facilitating its utilization as an injectable hydrogel without neg. impacting its cytocompatibility. Our findings expand the current toolkit of chem.-based stimuli-responsive hydrogels.

Polymer Chemistry published new progress about Biocompatibility, cytocompatibility. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Product Details of C11H8N2O3S2.

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

Moree, Wilna J.; Jovic, Florence; Coon, Timothy; Yu, Jinghua; Li, Bin-Feng; Tucci, Fabio C.; Marinkovic, Dragan; Gross, Raymond S.; Malany, Siobhan; Bradbury, Margaret J.; Hernandez, Lisa M.; O’Brien, Zhihong; Wen, Jianyun; Wang, Hua; Hoare, Samuel R. J.; Petroski, Robert E.; Sacaan, Aida; Madan, Ajay; Crowe, Paul D.; Beaton, Graham published the artcile< Novel benzothiophene H1-antihistamines for the treatment of insomnia>, Computed Properties of 1003-32-3, the main research area is benzothiophene preparation H1 antihistamine treatment insomnia.

SAR of lead benzothiophene H1-antihistamine I (R = 2-pyridyl) was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans were identified. Had a suitable human half-life as demonstrated in a human microdose study, but variability in pharmacokinetic profile, attributed to metabolic clearance, prevented further development of this compound I (R = 1-pyrazolyl) demonstrated lower predicted clearance in preclin. studies, and may represent a more suitable backup compound

Bioorganic & Medicinal Chemistry Letters published new progress about Histamine H1 receptor antagonists. 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