Author: tianli

《Identification of 1,3-thiazole-5-carboxylic Acid Derivatives as Inhibitors of Protein Kinase CK2》 was written by Protopopov, Mykola V.; Volynets, Galyna P.; Starosyla, Sergiy A.; Vdovin, Vasyl S.; Lukashov, Sergiy S.; Bilokin, Yaroslav V.; Bdzhola, Volodymyr G.; Yarmoluk, Sergiy M.. Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid And the article was included in Current Enzyme Inhibition on August 31 ,2018. The article conveys some information:

Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive mol. target for the development of small-mol. inhibitors which can be important compounds for pharmaceutical application. The main aim of this research is to identify novel chem. class of CK2 inhibitors with good lead-like properties. In order to find novel CK2 inhibitors, virtual screening experiments were performed using Autodock software. Best-scored compounds were tested in vitro using P32 radioactive kinase assay. Small-mol. inhibitors of protein kinase CK2 were identified among the derivatives of 1,3-thiazole-5-carboxylic acid. The most active compound inhibited CK2 with IC50 value of 0.4 μM. Ligand efficiency for studied derivatives of 1,3-thiazole-5-carboxylic acid was in the range from 0.45 to 0.56 kcal/mol/non-hydrogen atom. Considering the fact that the lower limit for ligand efficiency parameter is 0.3, the identified CK2 inhibitors among the derivatives of 1,3-thiazole-5-carboxylic acid are excellent candidates for further lead optimization. The results came from multiple reactions, including the reaction of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid

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

《One-step photostructuring of multiple hydrogel arrays for compartmentalized enzyme reactions in microfluidic devices》 was published in Reaction Chemistry & Engineering in 2019. These research results belong to Obst, Franziska; Simon, David; Mehner, Philipp J.; Neubauer, Jens W.; Beck, Anthony; Stroyuk, Oleksandr; Richter, Andreas; Voit, Brigitte; Appelhans, Dietmar. Product Details of 30931-67-0 The article mentions the following:

We present a technique for the simultaneous photostructuring of hydrogels on the μm scale with different compositions on one substrate. The existing methods (e.g. spin-coating of the hydrogel precursor and application of simple molds or spacers) have less potential to integrate spatially separated functional hydrogel dots as needed for the fabrication of complex polydimethylsiloxane (PDMS) on-glass microfluidic chips. Here, we report a method for the fast production of precisely placed hydrogel structures with adjustable height (= 80μm) and width (= 500μm) on glass substrates utilizing black polyoxymethylene molds. The integration of several chambers for different hydrogel precursor solutions in one mold allows the simultaneous photopolymerization of hydrogels with different compositions To visualize the difference in composition of the hydrogel dots and to demonstrate the precision in structuring, various quantum dots were added to the hydrogel precursor solutions and phys. entrapped during the photopolymerization To show the high potential of our photostructuring method, a microfluidic double-chamber reactor was designed and the variability in the performance of tri-enzymic cascade reactions with optionally spatially separated or non-separated enzymes β-galactosidase, glucose oxidase, and horseradish peroxidase was visualized.ABTS Diammonium(cas: 30931-67-0Product Details of 30931-67-0) was used in this study.

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Product Details of 30931-67-0

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

In 2022,Organic & Biomolecular Chemistry included an article by Choudhary, Shivani; Gayyur; Ghosh, Nayan. Formula: C7H5ClN2S. The article was titled 《Cu(II)-catalyzed [4 + 1] and [4 + 3] annulation reactions: a modular approach to N-aryl/alkyl substituted 2,5-diamidopyrroles and diazepines》. The information in the text is summarized as follows:

A one-pot copper-catalyzed [4 + 1] annulation reaction of primary amines with ynamide-derived buta-1,3-diynes for the synthesis of 2,5-diamido bearing N-aryl/alkyl pyrroles in up to excellent yields has been showcased. A broad range of primary amines having highly reactive functional groups are well tolerated. Notably, sterically demanding aniline and primary aliphatic amines are excellent amine sources. Furthermore, the current protocol may yield structurally unique diazepine derivatives The scale-up reaction and fruitful chem. elaboration of pyrrole motifs highlight the importance of this reaction. In the experiment, the researchers used many compounds, for example, 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Formula: C7H5ClN2S)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Formula: C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

The author of 《Layer by layer supported laccase on lignin nanoparticles catalyzes the selective oxidation of alcohols to aldehydes》 were Piccinino, Davide; Capecchi, Eliana; Botta, Lorenzo; Bollella, Paolo; Antiochia, Riccarda; Crucianelli, Marcello; Saladino, Raffaele. And the article was published in Catalysis Science & Technology in 2019. Name: ABTS Diammonium The author mentioned the following in the article:

Lignin has been used as an electrochem. active nanostructured support for the immobilization of laccase from Trametes versicolor by encapsulation, phys. adsorption, and layer by layer (LbL) technologies, including the glutaraldehyde and bovine derum albumin procedure. The activity parameters and kinetic properties of novel catalysts have been evaluated. Cyclic voltammetry and amperometric measurements confirmed the electrochem. behavior of the immobilized enzyme, which showed pseudo direct electron transfer (pseudo-DET) and mediated electron transfer (MET) mechanisms. The novel catalysts converted alcs. to the corresponding aldehydes with high selectivity in the presence of low mol. weight redox mediators, retaining the activity for more runs. In addition to this study using ABTS Diammonium, there are many other studies that have used ABTS Diammonium(cas: 30931-67-0Name: ABTS Diammonium) was used in this study.

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Name: ABTS Diammonium

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

In 2015,Liu, Gang; Abraham, Sunny; Liu, Xing; Xu, Shimin; Rooks, Allison M.; Nepomuceno, Ron; Dao, Alan; Brigham, Daniel; Gitnick, Dana; Insko, Darren E.; Gardner, Michael F.; Zarrinkar, Patrick P.; Christopher, Ron; Belli, Barbara; Armstrong, Robert C.; Holladay, Mark W. published 《Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Synthetic Route of C3H3BrN2S The information in the text is summarized as follows:

Based on a putative binding mode of quizartinib, a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clin. development, the authors have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focusing on maximizing in vivo efficacy and minimizing CYP3A4 time-dependent inhibition resulted in a highly efficacious compound I in tumor xenograft model for further preclin. development. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Synthetic Route of C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Synthetic Route of C3H3BrN2S

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

Category: thiazoleOn May 11, 2020 ,《Label-free colorimetric detection of acid phosphatase and screening of its inhibitors based on biomimetic oxidase activity of MnO2 nanosheets》 appeared in ACS Biomaterials Science & Engineering. The author of the article were Wang, Jing; Lu, Qiaoyun; Weng, Chenyuan; Li, Xiaoyun; Yan, Xiaoqiang; Yang, Wei; Li, Bingzhi; Zhou, Xuemin. The article conveys some information:

In this research, we attempted to develop a sensitive colorimetric sensing strategy for the detection of acid phosphatase (ACP) based on MnO2 nanosheets and explored its applications in screening and evaluating inhibitors of ACP. The MnO2 nanosheets exhibit intrinsic biomimetic oxidase activity, which can catalyze the oxidation of the colorless 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonate) diammonium salt (ABTS) into green oxidized ABTS (oxABTS). Upon the introduction of ACP, L-ascorbic acid-2-phosphate can be dephosphorylated to ascorbic acid, which arouses the disintegration of MnO2 nanosheets into Mn2+ ions. This disintegration weakens the enzyme mimicking activity of the MnO2 nanosheets, leading to the impediment of the oxidation of ABTS. Conversely, in the absence of ACP, the ABTS is rapidly oxidized by MnO2, leading to a significant colorimetric signal change. The absorbance difference at 420 nm displayed a linear relationship with the concentration of ACP ranging from 0.075 to 0.45 mU·mL-1, generating a detection limit of 0.046 mU·mL-1. In the inhibition assays, this sensing platform provided simple detection for parathion-Me (PM), a representative inhibitor of ACP. The facile evaluation of the inhibitory effect of PM, including its IC50 toward ACP, was also realized. The experimental part of the paper was very detailed, including the reaction process of ABTS Diammonium(cas: 30931-67-0Category: thiazole)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Category: thiazole

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

Computed Properties of C7H5ClN2SOn May 31, 2020, Acar Cevik, Ulviye; Osmaniye, Derya; Saglik, Beguem N.; Levent, Serkan; Cavusoglu, Betuel K.; Karaduman, Abdullah B.; Oekay, Uemide D.; Ozkay, Yusuf; Kaplancikli, Zafer A.; Turan, Guelhan published an article in Journal of Heterocyclic Chemistry. The article was 《Synthesis of new benzothiazole derivatives bearing thiadiazole as monoamine oxidase inhibitors》. The article mentions the following:

In this study, a novel series of benzothiazole-thiadiazole I (R1 = Et, methoxyethyl, n-Pr, n-Bu; R2 = H, Cl, NO2) was synthesized. These compounds I were evaluated as inhibitors for types A and B MAO enzymes. Compounds I [(A), R1 = methoxyethyl, R2 = NO2; R1 = n-Bu, R2 = NO2, (B)] were the most active derivatives in the series with IC50 values of 0.107 ± 0.003 and 0.128 ± 0.004, resp. Furthermore, compounds (A) and (B) were investigated for their cytotoxicity and found as non-cytotoxic. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Computed Properties of C7H5ClN2S)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Computed Properties of C7H5ClN2SThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

Recommanded Product: 6-Chlorobenzothiazol-2-ylamineOn March 12, 2020, Zaldivar-Diez, Josefa; Li, Lingling; Garcia, Ana M.; Zhao, Wen-Ning; Medina-Menendez, Cristina; Haggarty, Stephen. J.; Gil, Carmen; Morales, Aixa V.; Martinez, Ana published an article in Journal of Medicinal Chemistry. The article was 《Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate》. The article mentions the following:

Leucine rich repeat kinase 2 (LRRK2) is an enigmatic enzyme and a relevant target for Parkinson’s disease (PD). However, despite the significant amount of research done in the past decade, the precise function of LRRK2 remains largely unknown. Moreover, the therapeutic potential of its inhibitors is in its infancy with the first clin. trial having just started. In the present work, the mol. mechanism of LRRK2 in the control of neurogenesis or gliogenesis was investigated. We designed and synthesized novel benzothiazole-based LRRK2 inhibitors and showed that they can modulate the Wnt/β-catenin signaling pathway. Furthermore, compounds I and II were able to promote neural progenitors proliferation and drive their differentiation toward neuronal and oligodendrocytic cell fates. These results suggest potential new avenues for the application of LRRK2 inhibitors in demyelinating diseases in which oligodendrocyte cell-death is one of the pathol. features. In the part of experimental materials, we found many familiar compounds, such as 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 6-Chlorobenzothiazol-2-ylamine)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Recommanded Product: 6-Chlorobenzothiazol-2-ylamineThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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