Month: October 2022

Aulakh, Virender S.; Ciufolini, Marco A. published the artcile< An improved synthesis of pyridine-thiazole cores of thiopeptide antibiotics>, Synthetic Route of 31825-95-3, the main research area is pyridinethiazole core thiopeptide antiobiotic preparation.

The oxidation of 2-methylthiazoles to 2-formylthiazoles simplifies the implementation of the Bagley variant of the Bohlmann-Rahtz reaction as a key step in a concise route to pyridine cores of thiopeptide antibiotics.

Journal of Organic Chemistry published new progress about Bohlmann-Rahtz reaction. 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Synthetic Route of 31825-95-3.

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

Watthaisong, Pratchaya; Kamutira, Philaiwarong; Kesornpun, Chatchai; Pongsupasa, Vinutsada; Phonbuppha, Jittima; Tinikul, Ruchanok; Maenpuen, Somchart; Wongnate, Thanyaporn; Nishihara, Ryo; Ohmiya, Yoshihiro; Chaiyen, Pimchai published the artcile< Luciferin Synthesis and Pesticide Detection by Luminescence Enzymatic Cascades>, HPLC of Formula: 2591-17-5, the main research area is Dehalogenase; Luciferase; Luciferin; Luminescence; Organophosphate.

D-Luciferin (D-LH2), a substrate of firefly luciferase (Fluc), is important for a wide range of bioluminescence applications. This work reports a new and green method using enzymic reactions (HELP, HadA Enzyme for Luciferin Preparation) to convert 19 phenolic derivatives to 8 D-LH2 analogs with ≈51 % yield. The method can synthesize the novel 5′-methyl-D-LH2 and 4′,5′-dimethyl-D-LH2, which have never been synthesized or found in nature. 5′-Methyl-D-LH2 emits brighter and longer wavelength light than the D-LH2. Using HELP, we further developed LUMOS (Luminescence Measurement of Organophosphate and Derivatives) technol. for in situ detection of organophosphate pesticides (OPs) including parathion, methyl parathion, EPN, profenofos, and fenitrothion by coupling the reactions of OPs hydrolase and Fluc. The LUMOS technol. can detect these OPs at parts per trillion (ppt) levels. The method can directly detect OPs in food and biol. samples without requiring sample pretreatment.

Angewandte Chemie, International Edition published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, HPLC of Formula: 2591-17-5.

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

Abe, Hideki; Hikichi, Takuma; Emori, Kosuke; Yokosuka, Akihito; Mimaki, Yoshihiro; Kobayashi, Toyoharu; Ito, Hisanaka published the artcile< Total Synthesis of Catunaregin and Preliminary Evaluation of Its Antitumor Activity>, Reference of 171877-39-7, the main research area is catunaregin synthesis antitumor.

The total synthesis of catunaregin in both racemic and optically active forms was accomplished. The enantioselective synthesis uses the Evans aldol strategy, with an oxazolidinone or thiazolidinethione as the chiral auxiliary. The key features include a syn-selective aldol reaction to form the Evans-syn or non-Evans-syn product, and a successive ketalization reaction of a furanyl diol derivative under acidic conditions. The biol. properties of the synthetic racemate and both enantiomers were evaluated against A549 and HL-60 human cancer cells.

European Journal of Organic Chemistry published new progress about Aldol addition, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Reference of 171877-39-7.

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

Boga, C.; Del Vecchio, E.; Forlani, L.; Todesco, P. E. published the artcile< Tetrahalomethanes: simple reagents for the synthesis of monohalogenated and mixed dihalogenated aromatic heterocycles via metal-halogen exchange from lithium compounds>, Quality Control of 3034-56-8, the main research area is halogenation aromatic heterocycle; lithium halogen exchange aromatic heterocycle.

Tetrabromo- or tetrachloromethane and 2-lithio derivatives of aromatic heterocycles rapidly produce the corresponding 2-bromo or 2-chloro derivatives in high yields through a metal-halogen exchange mechanism. This kind of reaction was also used to obtain, in good yields, 5-bromo-2-chlorothiazole and 5-bromo-2-chloro-N-methylimidazole.

Journal of Organometallic Chemistry published new progress about Halogenation. 3034-56-8 belongs to class thiazole, and the molecular formula is C3HBrClNS, Quality Control of 3034-56-8.

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

Stoneman, Michael R.; Raicu, Valerica published the artcile< Dielectric spectroscopy based detection of specific and nonspecific cellular mechanisms>, SDS of cas: 2591-17-5, the main research area is dielec spectroscopy GPCR ligand interaction intracellular transport; G protein-coupled receptor; GPCR; dielectric relaxation; dielectric spectroscopy; label-free detection; ligand binding.

Using radiofrequency dielec. spectroscopy, we have investigated the impact of the interaction between a G protein-coupled receptor (GPCR), the sterile2 α-factor receptor protein (Ste2), and its cognate agonist ligand, the α-factor pheromone, on the dielec. properties of the plasma membrane in living yeast cells (Saccharomyces cerevisiae). The dielec. properties of a cell suspension containing a saturating concentration of α-factor were measured over the frequency range 40 Hz-110 MHz and compared to the behavior of a similarly prepared suspension of cells in the absence of α-factor. A spherical three-shell model was used to determine the elec. phase parameters for the yeast cells in both types of suspensions. The relative permittivity of the plasma membrane showed a significant increase after exposure to α-factor (by 0.06 ± 0.05). The equivalent experiment performed on yeast cells lacking the ability to express Ste2 showed no change in plasma membrane permittivity. Interestingly, a large change also occurred to the elec. properties of the cellular interior after the addition of α-factor to the cell suspending medium, whether or not the cells were expressing Ste2. We present a number of different complementary experiments performed on the yeast to support these dielec. data and interpret the results in terms of specific cellular reactions to the presence of α-factor.

Sensors published new progress about Cell membrane. 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

Xiao, Yao; Peng, Jinrong; Liu, Qingya; Chen, Lijuan; Shi, Kun; Han, Ruxia; Yang, Qian; Zhong, Lin; Zha, Ruoyu; Qu, Ying; Qian, Zhiyong published the artcile< Ultrasmall CuS@BSA nanoparticles with mild photothermal conversion synergistically induce MSCs-differentiated fibroblast and improve skin regeneration>, Product Details of C11H8N2O3S2, the main research area is copper sulfide BSA nanoparticle MSC fibroblast skin regeneration; CuS@BSA; MSCs; differentiation; photothermal conversion; wound healing..

Mesenchymal stem cell (MSC)-based therapies have been used in skin regeneration due to their ability to differentiate into many cells, promote cytokine secretion and participate in collagen deposition. In this study, we concluded that a CuS@BSA nanoparticles exhibited similar potential in inducing MSCs differentiation to fibroblasts as Cu ions for wound healing. First, we verified the photothermal efficiency of CuS@BSA in vivo and vitro and had no cytotoxicity for MSCs when the temperature was controlled at 42°C by adjusting the power of irradiation at 980 nm. And then we detected the expression of vimentin in MSCs, which further directed the MSCs to fibroblasts through Western blotting and Immunofluorescence when treated with CuS@BSA or pre-heat at 42°C. In addition, we implanted MSCs into the Matrigel or electrospun PLA nanofiber membrane in vitro to evaluating the effect of heating or CuS@BSA on the morphol. change of MSCs by SEM. Finally, we evaluated improving skin regeneration by the combination of preheated-MSCs and CuS@BSA nanoparticles that were encapsulated in Matrigel. The CuS@BSA nanoparticles have good photothermal conversion efficiency. Not only CuS nanoparticles itself or after irradiation at 980 nm stimulated the expressioin of vimentin in MSCs. Besides, the CuS@BSA can promote cell proliferation as Cu ion through the expression of ERK. The combination of the CuS@BSA nanoparticles and thermal treatment synergistically improved the closure of an injured wound in an injured wound model. MSCs combined with CuS@BSA are a promising wound dressing for the reconstruction of full-thickness skin injuries.

Theranostics published new progress about Bioluminescence. 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

Bedford, Simon T.; Benwell, Karen R.; Brooks, Teresa; Chen, Ijen; Comer, Mike; Dugdale, Sarah; Haymes, Tim; Jordan, Allan M.; Kennett, Guy A.; Knight, Anthony R.; Klenke, Burkhard; LeStrat, Loic; Merrett, Angela; Misra, Anil; Lightowler, Sean; Padfield, Anthony; Poullennec, Karine; Reece, Mark; Simmonite, Heather; Wong, Melanie; Yule, Ian A. published the artcile< Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor>, Quality Control of 1003-32-3, the main research area is thienopyrimidine aroyl carbamoyl alkylamino preparation antagonist human adenosine receptor.

The discovery of a novel class of antagonists of the human adenosine A2B receptor, thieno[3,2-d]pyrimidines I (R1 = Ph, 4-MeOC6H4, 2-thienyl, 5-methyl-2-thienyl, 2-thiazolyl, 4-pyridyl, MeNH, 1-pyrrolidinyl, etc.; R2 = H, Et, PhCH2, 3-pyridylmethyl, 3-pyridylcarbonyl, etc.; R3 = H, Cl, H2N, MeNH, EtNH, Me2N) is reported. This low mol. weight scaffold has been optimized to offer derivatives with potential utility for the alleviation of conditions associated with this receptor subtype, such as nociception, diabetes, asthma and COPD. Furthermore, preliminary pharmacokinetic anal. has revealed compounds with profiles suitable for either inhaled or systemic routes of administration.

Bioorganic & Medicinal Chemistry Letters published new progress about Adenosine A2B receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Quality Control of 1003-32-3.

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

Chadha, Ridhima; Das, Abhishek; Debnath, Anil K.; Kapoor, Sudhir; Maiti, Nandita published the artcile< 2-thiazoline-2-thiol functionalized gold nanoparticles for detection of heavy metals, Hg(II) and Pb(II) and probing their competitive surface reactivity: A colorimetric, surface enhanced Raman scattering (SERS) and x-ray photoelectron spectroscopic (XPS) study>, Category: thiazole, the main research area is colorimetry SERS 2thiazoline2thiol gold nanoparticles heavy metals surface reactivity.

A novel 2-thiazoline-2-thiol functionalized gold (Au-TT) nanosensor was developed for the selective and sensitive detection of toxic heavy metal ions, Hg(II) and Pb(II) by colorimetry, and for studying its competitive surface reactivity using SERS and XPS. The detection mechanism and surface reactivity is based on competitive binding affinity of thiocarbonyl S or thiazoline ring N/S atom with the metal ions and the nanoparticles (NPs). Due to diff ;erences in the binding affinities of the metal ions towards the active binding sites of TT, addition of different metal ions resulted in variation of color and SERS spectral features. Of the various metal ions studied, viz. Cu(II), Cd(II), Co(II), Zn(II), Ni(II), Hg(II), Pb(II), Ca(II), Fe(II), Mn(II) and Sn(II), only Hg(II) and Pb(II) showed distinctive colorimetric and SERS spectral response that was quantified using XPS. This study, thus, realizes a selective and sensitive visual based nanosensor for Hg(II) and Pb(II) with limit of detection (LOD) of ∼ 0.1 ppm. SERS revealed the formation of Hg(TT)2 and Pb(TT)2 complexes on the Au NPs surface with the former remaining bonded to the NPs, resulting in enhanced Raman intensity for the 1026 cm-1 band, while the latter gets desorbed from the surface leading to reduced SERS intensity.

Colloids and Surfaces, A: Physicochemical and Engineering Aspects published new progress about Affinity. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Category: thiazole.

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

Yu, Xiaoling; Zhang, Bingbing; Shan, Guangsheng; Wu, Yue; Yang, Feng-Ling; Lei, Xinsheng published the artcile< Synthesis of the molecular hybrid inspired by Largazole and Psammaplin A>, SDS of cas: 96929-05-4, the main research area is macrocyclic depsipeptide hybrid thiol synthesis HDAC inhibitor antitumor agent; natural product largazole psammaplin A drug design; methylcysteine acylation cyclocondensation thiazole thiazoline hydrolysis; malic acid cyclocondensation trichloro ethanediol esterification amidation; macrolactamization protective group.

One important class of HDAC (histone deacetylation enzymes) inhibitors is the sulfur-containing marine natural products with structural diversity. Inspired by two structurally distinguishing examples, Largazole and Psammaplin A, which possess macrocyclic depsipeptide and simple linear amide scaffold resp., we designed one novel mol. hybrid by replacing the alkene moiety in Largazole with a semirigid amide bond. This hybrid compound has been synthesized from L-malic acid in 10 steps with an overall yield of 7%. The preliminary biol. assays suggest that the replacement of trans olefin moiety with amide bond will lead to an unbeneficial effect on the inhibition against HDACs.

Tetrahedron published new progress about (Fluorenylmethoxy)carbonyl group. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, SDS of cas: 96929-05-4.

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

Ikeda, Yuma; Nomoto, Takahiro; Hiruta, Yuki; Nishiyama, Nobuhiro; Citterio, Daniel published the artcile< Ring-Fused Firefly Luciferins: Expanded Palette of Near-Infrared Emitting Bioluminescent Substrates>, Quality Control of 2591-17-5, the main research area is ring fused firefly luciferin near IR emitting bioluminescence substrate.

Firefly bioluminescence is broadly applied as a noninvasive imaging modality in the biomedical research field. One limitation in firefly bioluminescence imaging is the limited variety of luciferins emitting in the near-IR (NIR) region (650-900 nm), where tissue penetration is high. Herein, we describe a series of structure-inherent NIR emitting firefly luciferin analogs, NIRLucs, designed through a ring fusion strategy. This strategy resulted in pH-independent structure-inherent NIR emission with a native firefly luciferase, which was theor. supported by quantum chem. calculations of the oxidized form of each luciferin. When applied to cells, NIRLucs displayed dose-independent improved NIR emission even at low concentrations where the native D-luciferin substrate does not emit. Addnl., excellent blood retention and brighter photon flux (7-fold overall, 16-fold in the NIR spectral range) than in the case of D-luciferin have been observed with one of the NIRLucs in mice bearing s.c. tumors. We believe that these synthetic luciferins provide a solution to the longstanding limitation in the variety of NIR emitting luciferins and pave the way to the further development of NIR bioluminescence imaging platforms.

Analytical Chemistry (Washington, DC, United States) published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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