Day: October 12, 2022

Ospanov, Meirambek; Sulochana, Suresh P.; Paris, Jason J.; Rimoldi, John M.; Ashpole, Nicole; Walker, Larry; Ross, Samir A.; Shilabin, Abbas G.; Ibrahim, Mohamed A. published the artcile< Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor>, Electric Literature of 1003-32-3, the main research area is pyrrolobenzodiazepine preparation neuroinflammation cannabinoid receptor antineurodegenerative activity pharmacokinetic property; cannabinoid receptors CB1/CB2; central nervous system (CNS); neurodegenerative diseases; neuroinflammation; pharmacokinetics (PK); pyrrolobenzodiazepines; radioligand binding assay.

Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiol. processes. The CB2 subtype is largely localized to immune effectors, including microglia within the central nervous system, where it promotes anti-inflammation. Recently, a rational drug design toward precise modulation of the CB2 active site revealed the novelty of Pyrrolo[2,1-c][1,4]benzodiazepines tricyclic chemotype with a high conformational similarity in comparison to the existing leads. These compounds are structurally unique, confirming their chemotype novelty. In our continuing search for new chemotypes as selective CB2 regulatory mols., following SAR approaches, a total of 17 selected (S,E)-11-[2-(arylmethylene)hydrazono]-PBD analogs were synthesized and tested for their ability to bind to the CB1 and CB2 receptor orthosteric sites. A competitive [3H]CP-55,940 binding screen revealed five compounds that exhibited >60% displacement at 10 μM concentration Further concentration-response anal. revealed two compounds, 4k and 4q, as potent and selective CB2 ligands with sub-micromolar activities (Ki = 146 nM and 137 nM, resp.). In order to support the potential efficacy and safety of the analogs, the oral and i.v. pharmacokinetic properties of compound 4k were sought. Compound 4k was orally bioavailable, reaching maximum brain concentrations of 602 ± 162 ng/g (p.o.) with an elimination half-life of 22.9 ± 3.73 h. Whether administered via the oral or i.v. route, the elimination half-lives ranged between 9.3 and 16.7 h in the liver and kidneys. These compounds represent novel chemotypes, which can be further optimized for improved affinity and selectivity toward the CB2 receptor.

Molecules published new progress about Anti-neurodegenerative agents. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Electric Literature of 1003-32-3.

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

Javadi, Ali; Shockravi, Abbas; Koohgard, Mehdi; Malek, Ali; Shourkaei, Fateme Ahmadi; Ando, Shinji published the artcile< Nitro-substituted polyamides: A new class of transparent and highly refractive materials>, Product Details of C9H7N3O2S, the main research area is nitro polyamide transparent refractive material.

High-refractive-index polyamides (PAs) were developed by introducing nitro groups, thiazole rings, and thioether linkages. The PAs were prepared by the polycondensation of a novel diamine monomer, 5,5′-thiobis(2-amino-4-(3-nitrophenyl)thiazole) (DA), with various aromatic diacids. The bulky pendant nitrophenyl units, as well as the flexible thioether linkage in the diamine, endowed the resulting PAs with excellent solubilities in both amide-type polar aprotic solvents and less polar solvents. The obtained polymers exhibited high heat resistance, with 10% weight loss temperatures exceeding 472 °C under nitrogen and 427 °C in air atm., while their glass transition temperatures were in the range 210-244 °C. The combination of the nitro substituents, thiazole units, and thioether linkages provided PAs with high refractive indexes of up to 1.7660 at 632.8 nm, along with high transparency in the visible region and low birefringences (<0.0081). The structure-property relationships of these PAs due to the presence of nitro groups were also studied by comparing the results with the previously reported analogous polymers. European Polymer Journal published new progress about Birefringence. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Product Details of C9H7N3O2S.

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

Vo, Duc Duy; Tran, Thi Phuong Anh; Staedel, Cathy; Benhida, Rachid; Darfeuille, Fabien; Di Giorgio, Audrey; Duca, Maria published the artcile< Oncogenic MicroRNAs Biogenesis as a Drug Target: Structure-Activity Relationship Studies on New Aminoglycoside Conjugates>, HPLC of Formula: 57493-24-0, the main research area is MicroRNA structure aminoglycoside antitumor neoplasm; RNA structures; biogenesis; cancer; inhibitors; microRNA.

MicroRNAs (miRNAs) are a recently discovered category of small RNA mols. that regulate gene expression at the posttranscriptional level. Accumulating evidence indicates that miRNAs are aberrantly expressed in a variety of human cancers and that the inhibition of these oncogenic miRNAs could find application in the therapy of different types of cancer. Herein, the authors describe the synthesis and biol. evaluation of new small-mol. drugs that target oncogenic miRNAs production In particular, the authors chose to target two miRNAs (i.e., miRNA-372 and -373) implicated in various types of cancer, such as gastric cancer. Their precursors (premiRNAs) are overexpressed in cancer cells and lead to mature miRNAs after cleavage of their stem-loop structure by the enzyme Dicer in the cytoplasm. Some of the newly synthesized conjugates can inhibit Dicer processing of the targeted premiRNAs in vitro with increased efficacy relative to the previous results (D.D. Vo et al., ACS Chem. Biol. 2014, 9, 711-721) and, more importantly, to inhibit proliferations of adenocarcinoma gastric cancer (AGS) cells overexpressing these miRNAs, thus representing promising leads for future drug development.

Chemistry – A European Journal published new progress about Aminoglycosides Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 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

Stroet, Marcus C. M.; de Blois, Erik; Haeck, Joost; Seimbille, Yann; Mezzanotte, Laura; de Jong, Marion; Loewik, Clemens W. G. M.; Panth, Kranthi M. published the artcile< In vivo evaluation of gallium-68-labeled IRDye800CW as a necrosis avid contrast agent in solid tumors>, Category: thiazole, the main research area is gallium68 irdye800cw necrosis contrast agent solid tumor.

Necrosis only occurs in pathol. situations and is directly related to disease severity and, therefore, is an important biomarker. Tumor necrosis occurs in most solid tumors due to improperly functioning blood vessels that cannot keep up with the rapid growth, especially in aggressively growing tumors. The amount of necrosis per tumor volume is often correlated to rapid tumor proliferation and can be used as a diagnostic tool. Furthermore, efficient therapy against solid tumors will directly or indirectly lead to necrotic tumor cells, and detection of increased tumor necrosis can be an early marker for therapy efficacy. We propose the application of necrosis avid contrast agents to detect therapy-induced tumor necrosis. Herein, we advance gallium-68-labeled IRDye800CW, a near-IR fluorescent dye that exhibits excellent necrosis avidity, as a potential PET tracer for in vivo imaging of tumor necrosis. We developed a reliable labeling procedure to prepare [68Ga]Ga-DOTA-PEG4-IRDye800CW ([68Ga]Ga-1) with a radiochem. purity of >96% (radio-HPLC). The prominent dead cell binding of fluorescence and radioactivity from [68Ga]Ga-1 was confirmed with dead and alive cultured 4T1-Luc2 cells. [68Ga]Ga-1 was injected in 4T1-Luc2 tumor-bearing mice, and specific fluorescence and PET signal were observed in the spontaneously developing tumor necrosis. The i.p. injection of D-luciferin enabled simultaneous bioluminescence imaging of the viable tumor regions. Tumor necrosis binding was confirmed ex vivo by colocalization of fluorescence uptake with TUNEL dead cell staining and radioactivity uptake in dichotomized tumors and frozen tumor sections. Our presented study shows that [68Ga]Ga-1 is a promising PET tracer for the detection of tumor necrosis.

Contrast Media & Molecular Imaging published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

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

Dong, Jiaxing; Huang, Yumin; Qin, Xurong; Cheng, Yangyang; Hao, Jing; Wan, Danyang; Li, Wei; Liu, Xingyan; You, Jingsong published the artcile< Palladium(II)-Catalyzed Oxidative C-H/C-H Cross-Coupling between Two Structurally Similar Azoles>, Application In Synthesis of 20582-55-2, the main research area is azole palladium copper cocatalyst oxidative cross coupling; double carbon hydrogen activation azole cross coupling.

A widely functional-group tolerant, selective and rapid oxidative cross-coupling between two structurally similar azoles has been carried out by using a palladium/copper co-catalytic twofold C-H activation method.

Chemistry – A European Journal published new progress about Azoles 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, Application In Synthesis of 20582-55-2.

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

Malik, G. M.; Patel, Sandip K.; Patel, Pratixa K.; Zadafiya, S. K. published the artcile< Synthesis, characterization and microbial studies of 2-amino-4-(3'-nitrophenyl)thiazole based bisazo disperse dyes and their dyeing performance on polyester fibers>, COA of Formula: C9H7N3O2S, the main research area is aminonitrophenyl thiazolebisazo disperse dye polyester fiber microbial dyeing property; dyeing dye polyester fiber.

In the present study various substituted bisazo disperse dyes 2-(1′-substituted Ph azo)-4-(3′-nitrophenyl)-5-(2”,4”-dinitro Ph azo)thiazole derivatives have been synthesized using substituted 3°-amine, 2-amino-4-(3′-nitrophenyl)thiazole and 2,4-dinitroaniline. These were characterized using elemental anal., 1H NMR (NMR) and IR spectra. Their dyeing performance on polyester fiber was assessed and fastness properties of these dyes were evaluated by applying them to polyester fiber. These dyes exhibited moderate to good anti-bacterial and anti-fungal activities.

International Journal of Chemistry (Mumbai, India) published new progress about Antibacterial 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

Majstrowicz, Katarzyna; Honnert, Ulrike; Nikolaus, Petra; Schwarz, Vera; Oeding, Stefanie J.; Hemkemeyer, Sandra A.; Baehler, Martin published the artcile< Coordination of mitochondrial and cellular dynamics by the actin-based motor Myo19>, Application of C22H23F2N3O2S, the main research area is actin motor myosin mitochondrial cellular dynamic coordination; Cell adhesion; Mitochondria; Mitosis; Myosin.

Myosin XIX (Myo19) is an actin-based motor that competes with adaptors of microtubule-based motors for binding to the outer mitochondrial transmembrane proteins Miro1 and Miro2 (collectively Miro, also known as RhoT1 and RhoT2, resp.). Here, we investigate which mitochondrial and cellular processes depend on the coordination of Myo19 and microtubule-based motor activities. To this end, we created Myo19-deficient HEK293T cells. Mitochondria in these cells were not properly fragmented at mitosis and were partitioned asym. to daughter cells. Respiratory functions of mitochondria were impaired and ROS generation was enhanced. On a cellular level, cell proliferation, cytokinesis and cell-matrix adhesion were neg. affected. On a mol. level, Myo19 regulates focal adhesions in interphase, and mitochondrial fusion and mitochondrially associated levels of fission protein Drp1 and adaptor proteins dynactin and TRAK1 at prometaphase. These alterations were due to a disturbed coordination of Myo19 and microtubulebased motor activities by Miro.

Journal of Cell Science published new progress about Bacteriophage Miro1. 2222768-84-3 belongs to class thiazole, and the molecular formula is C22H23F2N3O2S, Application of C22H23F2N3O2S.

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

Huang, David S.; Wong, Henry L.; Georg, Gunda I. published the artcile< Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin>, Reference of 171877-39-7, the main research area is pironetin analog preparation anticancer structure activity ovarian cancer; Cytotoxicity; Pironetin; Structure-activity; Synthesis; Tubulin.

Pironetin is an α-tubulin-binding natural product with potent antiproliferative activity against several cancer cell lines that inhibits cell division by forming a covalent adduct with α-tubulin via a Michael addition into the natural product’s α,β-unsaturated lactone. We designed and prepared analogs carrying electron-withdrawing groups at the α-position (C2) of the α,β-unsaturated lactone with the goal to generate potent and selective binding analogs. We prepared derivatives I (R = F, Me, Cl, Br, Ph) containing halogens, a Ph, and a Me group at the C2 position to evaluate the structure-activity relationship at this position. Testing of the analogs in ovarian cancer cell lines demonstrated 100-1000-fold decreased antiproliferative activity.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 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

Ren, Qi; Dai, Lu; Zhang, Hui; Tan, Wenfei; Xu, Zhengshuang; Ye, Tao published the artcile< Total synthesis of largazole>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is largazole asym total synthesis.

The stereocontrolled total synthesis of largazole was accomplished starting from 3-[(tert-butyldimethylsilyl)oxy]propanol in 5.8% overall yield, unambiguously confirming its structure. Key steps included the use of the Nagao thiazolidinethione auxiliary for a diastereoselective acetate aldol reaction, thiazoline-thiazole formation, and macrolactamization by use of the Mukaiyama reagent.

Synlett published new progress about Aldol addition, stereoselective. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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

Love, Anna C.; Prescher, Jennifer A. published the artcile< Seeing (and Using) the Light: Recent Developments in Bioluminescence Technology>, Quality Control of 2591-17-5, the main research area is review luciferase luciferin bioluminescence optical imaging; bioluminescence; imaging; luciferase; luciferin; optogenetics.

A review. Bioluminescence has long been used to image biol. processes in vivo. This technol. features luciferase enzymes and luciferin small mols. that produce visible light. Bioluminescent photons can be detected in tissues and live organisms, enabling sensitive and noninvasive readouts on physiol. function. Traditional applications have focused on tracking cells and gene expression patterns, but new probes are pushing the frontiers of what can be visualized. The past few years have also seen the merger of bioluminescence with optogenetic platforms. Luciferase-luciferin reactions can drive light-activatable proteins, ultimately triggering signal transduction and other downstream events. This review highlights these and other recent advances in bioluminescence technol., with an emphasis on tool development. We showcase how new luciferins and engineered luciferases are expanding the scope of optical imaging. We also highlight how bioluminescent systems are being leveraged not just for sensing-but also controlling-biol. processes.

Cell Chemical Biology 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