Tag: 200-300

Kucukbay, F. Zehra; Bugday, Nesrin; Kucukbay, Hasan; Tanc, Muhammet; Supuran, Claudiu T. published an article in 2016, the title of the article was Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives.Electric Literature of 92-36-4 And the article contains the following content:

N-protected amino acids I [Pg = Cbz, Boc, R = H, Me; Pg =Boc, R = CH2Ph] were reacted with substituted benzothiazoles to give the corresponding N-protected amino acid-benzothiazole conjugates II [Pg = Cbz, R = H; Pg = Boc, R = H, CH2Ph], III [Pg = Cbz, R = H, Me; Pg = Boc, R = H, CH2Ph] and IV [Pg = CBz, R = H, Me; Pg = Boc, R = H, Me, CH2Ph] (60-89%). Their structures were confirmed by proton NMR (1H NMR), carbon-13 NMR (13C NMR), IR and elemental anal. Their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were determined against two cytosolic human isoforms (hCA I and hCA II), one membrane-associated (hCA IV) and one transmembrane (hCA XII) enzyme by a stopped-flow CO2 hydrase assay method. The new compounds showed rather weak, micromolar inhibitory activity against most of these enzymes. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Electric Literature of 92-36-4

The Article related to amino acid benzothiazole amide preparation carbonic anhydrase inhibition, amino acid-benzothiazole conjugates, benzothiazole, carbonic anhydrase, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Electric Literature of 92-36-4

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

On November 24, 2017, Liu, Denggui; Yang, Kunyu; Zhou, Wei; Chen, Hao; Zeng, Qingdong published a patent.Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Preparation of 2-(4-methyl-1-oxo-2-penten-1-yl)-4-thiazolecarboxylic acid ethyl ester. And the patent contained the following:

The invention discloses a preparation method of anti-cancer medicament intermediate, using glyceraldehyde acetonide and L-cysteine hydrochloride as raw materials, through steps such as cyclization, oxidation, de-propylidene, reoxidizing, and halohydrin to obtain an intermediate compound, which was further reacted with isobutyric aldehyde through Wittig, and compound 2-(4-methyl-1-oxo-2-penten-1-yl)-4-thiazolecarboxylic acid Et ester is obtained. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to thiazolecarboxylic acid ethyl ester preparation, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

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

White, Lisa J.; Boles, Jessica E.; Hilton, Kira L. F.; Ellaby, Rebecca J.; Hiscock, Jennifer R. published an article in 2020, the title of the article was Towards the application of supramolecular self-associating amphiphiles as next-generation delivery vehicles.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole And the article contains the following content:

Herein, we present a series of supramol. self-associating amphiphilic (SSA) salts and establish the potential for these mol. constructs to act as next-generation solution-state mol. delivery vehicles. We characterize the self-association of these SSAs, both alone and when co-formulated with a variety of drug(like) competitive guest species. Single crystal X-ray diffraction studies enable the observation of hydrogen-bonded self-association events in the solid state, while high resolution mass spectrometry confirms the presence of anionic SSA dimers in the gas-phase. These same anionic SSA dimeric species are also identified within a competitive organic solvent environment (DMSO-d6/0.5% H2O). However, extended self-associated aggregates are observed to form under aqueous conditions (H2O/5.0% EtOH) in both the absence and presence of these competitive guest species. Finally, through the completion of these studies, we present a framework to support others in the characterization of such systems. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to drug delivery self associating amphiphile, amphiphile, drug delivery, hydrogen bond, supramolecular chemistry, Pharmaceuticals: Formulation and Compounding and other aspects.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On January 22, 2011, Zanda, Matteo; Sani, Monica; Lazzari, Paolo published a patent.Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Pharmaceutical compositions comprising tubulysin compounds. And the patent contained the following:

The present invention relates to synthetic tubulysin compounds having a high cytotoxicity, with antimitotic and/or antiangiogenic properties, the corresponding solvates and pharmaceutically acceptable salts thereof, their use for the treatment of tumors and/or diseases associated to angiogenesis, and a process for their preparation with high yield. Pharmaceutical compositions comprising tubulysin compounds or their conjugates with polymers or biomols., e.g., proteins, hormones, aptamers, polysaccharides, antibodies and fragments thereof, peptides, vitamins, etc., are disclosed. Thus, (2S,4R)-4-[2-[(1R,3R)-1-acetoxy-3-[(2S,3R)-N-benzyl-3-methyl-2-(1-methylpiperidine-2-carboxamido)pentanamido]-4-methylpentyl]thiazole-4-carboxamido]-2-methyl-5-phenylpentanoic acids was prepared and formulated into nanoparticles of polylactate-polyglycolate copolymer. The high cytotoxicity of the compound against 3 tumor cell lines (HL60, HT29 and A2780) was demonstrated. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to tubulysin compound preparation antitumor antimitotic angiogenesis inhibitor pharmaceutical, Pharmaceuticals: Formulation and Compounding and other aspects.Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

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

On June 24, 2010, Tzanopoulou, Stamatia; Sagnou, Marina; Paravatou-Petsotas, Maria; Gourni, Eleni; Loudos, George; Xanthopoulos, Stavros; Lafkas, Daniel; Kiaris, Hippokratis; Varvarigou, Alexandra; Pirmettis, Ioannis C.; Papadopoulos, Minas; Pelecanou, Maria published an article.Application of 92-36-4 The title of the article was Evaluation of Re and 99mTc Complexes of 2-(4′-Aminophenyl)benzothiazole as Potential Breast Cancer Radiopharmaceuticals. And the article contained the following:

The synthesis of M(I)(CO)3(NNO) (M = Re, 99mTc) complexes conjugated to the antitumor agent 2-(4′-aminophenyl)benzothiazole and to its 6-Me derivative, as well as their in vitro and in vivo biol. evaluation as breast cancer radiopharmaceuticals, is reported. The Re complexes displayed under the fluorescence microscope clear uptake by the sensitive to the 2-(4′-aminophenyl)benzothiazole pharmacophore breast cancer cell lines MCF-7 and T47D, while uptake by less sensitive lines and by normal fibroblasts was much weaker. In accordance, uptake of the corresponding radioactive 99mTc complexes was clearly higher in the breast cancer cell lines MCF-7 and MDA-231 compared to normal fibroblasts. Biodistribution of the 99mTc complexes in SCID mice bearing MCF-7 xenografts showed appreciable tumor uptake. A tumor/muscle ratio of 2.2 was measured for the complex conjugated to 2-(4′-aminophenyl)benzothiazole that led to successful tumor imaging. The results render the 2-(4′-aminophenyl)benzothiazole complexes potential candidates for imaging (99mTc) and targeted radiotherapy (188Re) of breast cancer. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Application of 92-36-4

The Article related to rhenium technetium aminophenyl benzothiazole preparation breast cancer imaging radiotherapy, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Application of 92-36-4

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

On April 30, 2015, Ambure, Pravin; Roy, Kunal published an article.Category: thiazole The title of the article was Exploring Structural Requirements of Imaging Agents Against Aβ Plaques in Alzheimer’s Disease: A QSAR Approach. And the article contained the following:

Exploring mol. imaging agents against the beta amyloid (Aβ) plaques for an early detection of Alzheimer’s disease (AD) is one of the emerging research areas in medicinal chem. In the present in-silico study, a congeneric series of 44 imaging agents, including 17 positron emission tomog. (PET) and 27 single photon emission computed tomog. (SPECT) imaging agents, was utilized to understand the structural features required for having essential binding affinity against Aβ plaques. Here, 2D-quant. structure-activity relationship (2D-QSAR) and group-based QSAR (G-QSAR) models have been developed using genetic function approximation (GFA) and validated using various statistical metrics. Both the models showed satisfactory performance signifying the reliability and robustness of the developed QSAR models. The vital information gained from both the QSAR models will be useful in developing new PET and SPECT imaging agents and also in predicting their binding affinity against Aβ plaques. The results of this study would be important in view of the widespread clin. applicability of the SPECT imaging agents, especially in the developing countries. In this study, we have also designed some imaging agents based on the information provided by the models. Some of these designed compounds were predicted to be similar to or more active than the most active imaging agents present in the original dataset. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Category: thiazole

The Article related to amyloid beta plaque alzheimer disease radiodiagnostic pet spect qsar, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Category: thiazole

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

On August 15, 2010, Hu, Wan-Ping; Chen, Yin-Kai; Liao, Chao-Cheng; Yu, Hsin-Su; Tsai, Yi-Min; Huang, Shu-Mei; Tsai, Feng-Yuan; Shen, Ho-Chuan; Chang, Long-Sen; Wang, Jeh-Jeng published an article.COA of Formula: C14H12N2S The title of the article was Synthesis, and biological evaluation of 2-(4-aminophenyl)benzothiazole derivatives as photosensitizing agents. And the article contained the following:

Photodynamic therapy (PDT) employing exogenous photosensitizers is currently being approved for treatment of basal cell carcinoma (BCC). 2-(4-Aminophenyl)benzothiazoles (6) consist of chromophoric structure and absorb light in the UVA (315-400 nm). These results encouraged us to design and synthesize a diversity of 2-phenylbenzothiazoles (6). Studies on the apoptotic mechanism involved in photosensitive effects induced by UVA-activated 6 in BCC cells are carried out in the present article. 6-UVA-treated cells displayed several features of apoptosis, including an increase in the sub-G1 population, a significantly increased annexin V binding, and activation of caspase-3. 6-UVA induced a decrease in mitochondrial membrane potential (Δψ mt) and ATP via enhanced ROS generation and promoted phosphorylation of extracellular signal-regulated kinase (ERK) and p38 MAPK expression. These results suggest that 6-UVA elicits photosensitive effects in mitochondria processes which involve ERK and p38 activation, and ultimately lead to BCC cell apoptosis. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).COA of Formula: C14H12N2S

The Article related to aminophenyl benzothiazole derivative preparation pdt photosensitizer, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.COA of Formula: C14H12N2S

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

On June 6, 2013, Ali-Torres, Jorge; Rimola, Albert; Rodriguez-Rodriguez, Cristina; Rodriguez-Santiago, Luis; Sodupe, Mariona published an article.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Insights on the Binding of Thioflavin Derivative Markers to Amyloid-Like Fibril Models from Quantum Chemical Calculations. And the article contained the following:

Thioflavin-T (ThT) is one of the most widely used dyes for staining and identifying amyloid fibrils, which share a common parallel in register β-sheet structure. Unfortunately, ThT is a charged mol., which limits its ability to cross the blood brain barrier and its use as an efficient dye for in vivo detection of amyloid fibrils. For this reason, several uncharged ThT derivatives have been designed and their binding properties to Aβ fibrils studied by fluorescence assays. However, there are still many unknowns on the binding mechanism and the role of noncovalent interactions on the affinity of these ligands toward β-sheet structures. The present contribution analyzes the binding of ThT (1) and neutral ThT derivatives (2-7) to a β-sheet model by means of quantum chem. B3LYP-D calculations and including solvent effects with the continuum CPCM method. Results show that, in all cases, ligand binding is mainly driven by dispersion interactions. In addition, ligands with -NH groups display hydrogen bond interactions with CO groups of the peptide strand, increasing the intrinsic affinity toward the β-sheet surface. Solvent effects notably reduce the affinity of charged ThT, as compared to neutral systems, due to its larger solvation energy. As a result, neutral derivatives display significantly higher affinities than ThT in solution, in agreement with exptl. observations. Anal. of the hydrogen bonding network of the β-sheet structure indicates that stacking interactions upon ligand binding induce a shortening of interstrand hydrogen bonding, suggesting a strengthening of the β-sheet. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to thioflavin derivative amyloid fibril model quantum chem, General Biochemistry: Proteins and Their Constituents and other aspects.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On July 31, 2006, Wu, Chunying; Cai, Lisheng; Wei, Jingjun; Pike, Victor W.; Wang, Yanming published an article.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Lipophilic analogs of thioflavin S as novel amyloid-imaging agents. And the article contained the following:

Lipophilic analogs of thioflavin S were synthesized and radiolabeled with positron or single photon emitting radionuclides. The binding affinity for Aβ was evaluated using isolated amyloid fibrils from human brain tissue. Binding specificity was assessed using fluorescent tissue staining. In vivo brain uptake was evaluated in mice. Following synthesis, neutral analogs of thioflavin S capable of radiolabeling with 11C or 125I, were found to bind isolated human Aβ with affinities in the nanomolar range. Fluorescent tissue staining showed selective binding to Aβ deposits in vitro. Biodistribution of selected compounds displayed high brain permeability at early time points. At later points, the compounds were cleared from the normal brain, indicating low non-specific binding in vivo. These studies indicated that novel amyloid imaging probes can be developed based on thioflavin S that readily entered the brain and selectively bound to Aβ deposits and neurofibrilary tangles. Potential applications of these amyloid binding agents include facilitating drug screening in animal models and use as in vivo markers of early and definitive diagnosis of AD. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to thioflavin s lipophilic analog amyloid imaging agent, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On February 1, 2010, Law, K. P. published an article.Synthetic Route of 92-36-4 The title of the article was Surface-assisted laser desorption/ionization mass spectrometry on nanostructured silicon substrates prepared by iodine-assisted etching. And the article contained the following:

Surface-assisted laser desorption/ionization (SALDI) is a matrix-free mass spectrometry (MS) approach that utilizes the unique properties of a nanostructured surface to promote desorption and ionization. However, there are still questions on what constitutes a suitable SALDI substrate for mass spectrometric application. A range of SALDI substrates prepared by anodization with an oxidizing electrolyte was investigated. The laser desorption/ionization (LDI) performance was examined on a reflectron time-of-flight (ToF) mass spectrometer. The physicochem. properties of the substrates were characterized by a number of surface anal. techniques including SEM, at. force microscopy (AFM), secondary ion mass spectrometry (SIMS), XPS and water contact angle measurement. Examination of surface cleaning technologies and methods for surface chem. modification were carried out. Correlation between the substrate physicochem. properties and the LDI performance was determined It was found that only the substrate, which had a thick nanostructured layer, was effective for LDI-MS. SALDI substrate was found to have a high surface potential. However, this unique property offered no advantage for the application of LDI-MS. Surface chem. is also an important factor in affecting the LDI performance. Plasma etching can effectively remove the surface contamination but it also increases the thickness of the oxide layer. Fluorine and hydroxyl termination is advantageous. Fluorine passivation increases the surface hydrophobicity, which confines the analyte solution droplet to a smaller area and also withdraws the electronic d. from the surface, and acidifies the surface Si-OH moieties, which is believed a major proton source. The effect of laser etching was investigated by SIMS and XPS imaging and provided new insight of the SALDI ionization mechanism. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Synthetic Route of 92-36-4

The Article related to iodine assisted etching nanostructure silicon saldi mass spectrum, Surface Chemistry and Colloids: Solid-Liquid Systems and other aspects.Synthetic Route of 92-36-4

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