tianli，作者Heterocyclic Building Blocks-Thiazole

Laghezza, Antonio’s team published research in Bioorganic & Medicinal Chemistry in 2020 | CAS: 95-24-9

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.Safety of 6-Chlorobenzothiazol-2-ylamineThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

Laghezza, Antonio; Luisi, Grazia; Caradonna, Alessia; Di Pizio, Antonella; Piemontese, Luca; Loiodice, Fulvio; Agamennone, Mariangela; Tortorella, Paolo published an article on February 1 ,2020. The article was titled 《Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry.Safety of 6-Chlorobenzothiazol-2-ylamine The information in the text is summarized as follows:

Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor progression and invasiveness. This encouraged over the years the approach of MMP, and particularly MMP-2, targeting for anticancer treatment. Early generations of MMP inhibitors, based on aspecific zinc binding groups (ZBGs) assembled on (pseudo)peptide scaffolds, have been discontinued due to the clin. emergence of toxicity and further drawbacks, giving the way to inhibitors with alternative zinc-chelator moieties or not binding the catalytic zinc ion. In the present paper, we continue the search for new non-zinc binding MMP-2 inhibitors: exploiting previously identified compounds, a virtual screening (VS) campaign was carried out and led to the identification of a new class of ligands. The structure-activity relationship (SAR) of the benzimidazole scaffold was explored by synthesis of several analogs whose inhibition activity was tested with enzyme inhibition assays. By performing the mol. simplification approach, we disclosed different sets of single-digit micromolar inhibitors of MMP-2, with up to a ten-fold increase in inhibitory activity and ameliorated selectivity towards off-target MMP-8, compared to selected lead compound Mol. dynamics calculations conducted on complexes of MMP-2 with docked privileged structures confirmed that analyzed inhibitors avoid targeting the zinc ion and dip inside the S1′ pocket. Present results provide a further enrichment of our insights for the design of novel MMP-2 selective inhibitors. After reading the article, we found that the author used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Safety of 6-Chlorobenzothiazol-2-ylamine)

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

Saha, Rituparna’s team published research in Enzyme and Microbial Technology in 2022 | CAS: 30931-67-0

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Formula: C18H24N6O6S4

Saha, Rituparna; Mukhopadhyay, Mainak published an article on January 31 ,2022. The article was titled 《Electrochemical analysis of Catechol polymerization in presence of Trametes versicolor laccase and the mediator ABTS》, and you may find the article in Enzyme and Microbial Technology.Formula: C18H24N6O6S4 The information in the text is summarized as follows:

The phenolic compound catechol has found various applications in the industry but is often discharged untreated in industrial effluents. Catechol is highly toxic and adversely affects the environment. This has increased extensive investigation into elucidating the effects of various synthetic elements or different biocatalysts on catechol, thereby leading the way to its bioremediation. Hence, an electrochem.-based study on catechol in the presence of the enzyme laccase could provide a basic understanding of the unique characteristics exhibited by catechol, thus facilitating a distinct perspective to its subsequent treatment and removal. The present study focuses on the electrochem. characterization of catechol based on the oxidation of laccase and the redox mediator 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Catechol exhibited distinct electrochem. behavior across various concentrations The unique electroactive nature of ABTS assisted in the polymerization of catechol which was found to be concentration-dependent. Laccase produced a higher oxidation-reduction rate, thereby producing a much more stable condition for the polymerization of catechol. However, with the laccase-mediator system (LMS), the catechol polymerization rate was distinctly higher and more gradual with the enzyme utilizing the electroactive species produced by ABTS to increase the electron transfer and producing a combinatorial impact on the phenolic compound This study could rightly serve as the building block in developing future technologies like wastewater treatment and biosensors for catechol bioremediation. The experimental process involved the reaction of ABTS Diammonium(cas: 30931-67-0Formula: C18H24N6O6S4)

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

Daudu, Oluremi M.’s team published research in Journal of Apicultural Science in 2019 | CAS: 30931-67-0

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Recommanded Product: ABTS Diammonium

《Bee Pollen Extracts as Potential Antioxidants and Inhibitors of α-Amylase and α-Glucosidase Enzymes In Vitro Assessment》 was published in Journal of Apicultural Science in 2019. These research results belong to Daudu, Oluremi M.. Recommanded Product: ABTS Diammonium The article mentions the following:

The study was conducted to determine the antioxidant and anti-diabetic properties of bee pollen. The phenol content of extracts was 1.43, 2.04, 2.10 and 1.79 mg gallic acid g-1, resp. Total flavonoid content was 0.78, 1.39, 0.86 and 0.79 mg gallic acid g-1 resp. Bee pollen extracts have the potential to scavenge free radicals and lower blood glucose due to the presence of phenols and flavonoids. The aqueous-ethanol extract had the lowest IC50 for HRS and TAC, 0.53mg/mL and 0.25mg/mL resp., which depicts that this extract alleviates the destructive effect of hydroxyl radicals. Methanol extract had the lowest IC50 (0.21 mg/mL) for DPPH inhibition, hence it was able to scavenge the DPPH radicals. Ethanol extract had the lowest IC50 (0.04 mg/mL) for 2, 2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) inhibition, hence it can protect living cells from ABTS cations. The aqueous-ethanol extract displayed higher inhibition of α-amylase (4.51 mg/mL) while the aqueous extract exhibited a higher inhibition of α-glucosidase (0.60 mg/mL), which slows down the breakdown of disaccharides and reduces sugar buildup in the bloodstream. Bee pollen has potential antioxidative and antidiabetic activity. The results came from multiple reactions, including the reaction of ABTS Diammonium(cas: 30931-67-0Recommanded Product: ABTS Diammonium)

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

Komanova, E’s team published research in Journal of Chromatography in 1971 | 10574-69-3

Journal of Chromatography published new progress about Linear free energy relationship. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

Komanova, E.; Knoppova, V.; Koman, V.; Malinova, A. published the artcile< Gas chromatography of isothiocyanates and 3-substituted rhodanines>, SDS of cas: 10574-69-3, the main research area is retention time isothiocyanates; gas chromatog rhodanines.

Retention times in the gas chromatog. separation of 3-substituted alkyl- or arylrhodanines were 5.9 min higher than for the corresponding isothiocyanates, indicating a successful separation of a mixture of these compounds by gas-liquid chromatog. For example, the retention time observed for 4-ethoxyphenyl isothiocyanate was 18.03 min while that of 4-(ethoxyphenyl)-3-rhodanine (I) was 24.02 min. A plot of Hammett constants vs. retention times for 4-substituted isothiocyanates and 3-substituted rhodanines was not linear. Electron-releasing substituents shifted their retention times to lower values while electron-withdrawing substituents had the opposite effect.

Journal of Chromatography published new progress about Linear free energy relationship. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, SDS of cas: 10574-69-3.

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

Inouye, Satoshi’s team published research in Protein Expression and Purification in 2020-07-31 | 2591-17-5

Protein Expression and Purification published new progress about Absorption. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

Inouye, Satoshi; Sahara-Miura, Yuiko; Nakamura, Mitsuhiro; Hosoya, Takamitsu published the artcile< Expression, purification, and characterization of recombinant apoPholasin>, Category: thiazole, the main research area is apoPholasin glutathione transferase coelenterazine reactive oxygen species oxidation; Coelenteramide; Coelenteramine; Dehydrocoelenterazine; Photoproteins; Reactive oxygen.

Pholasin is a reactive oxygen-sensitive photoprotein that consists of an apoprotein (apoPholasin) and an unknown chromophore. The preferred human codon-optimized apoPholasin gene was transiently expressed in mammalian cells and apoPholasin was detected using an anti-recombinant apoPholasin antibody. For the first time, we found that apoPholasin secreted into the culture medium could catalyze the oxidation of coelenterazine (CTZ, a luciferin) to produce continuous luminescence. The fusion protein of apoPholasin and glutathione S-transferase (GST-apoPholasin) was successfully expressed as a soluble form in bacterial cells using the cold induction system. The purified GST-apoPholasin also had luminescence activity with CTZ, showing the bioluminescence emission peak at 461 nm, and the resultant product showed purple blue fluorescence under 365 nm light. Unexpectedly, the main oxidation product of CTZ was identified as coelenteramine (CTM), not coelenteramide (CTMD).

Protein Expression and Purification published new progress about Absorption. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

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

Hasgur, Suheyla’s team published research in Cytotherapy in 2021-05-31 | 2591-17-5

Cytotherapy published new progress about Adhesion G protein-coupled receptor E1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Safety of (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Hasgur, Suheyla; Desbourdes, Laura; Relation, Theresa; Overholt, Kathleen M.; Stanek, Joseph R.; Guess, Adam J.; Yu, Minjun; Patel, Pratik; Roback, Linda; Dominici, Massimo; Otsuru, Satoru; Horwitz, Edwin M. published the artcile< Splenic macrophage phagocytosis of intravenously infused mesenchymal stromal cells attenuates tumor localization>, Safety of (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is mesenchymal stromal cell splenic macrophage phagocytosis tumor localization; cancer cell therapy; lentiviral transduction; mesenchymal stromal cells (MSCs); phagocytosis; splenic macrophage; stem cell transplantation; tumor homing.

Mesenchymal stromal cells (MSCs) possess remarkable tumor tropism, making them ideal vehicles to deliver tumor-targeted therapeutic agents; however, their value in clin. medicine has yet to be realized. A barrier to clin. utilization is that only a small fraction of infused MSCs ultimately localize to the tumor. In an effort to overcome this obstacle, we sought to enhance MSC trafficking by focusing on the factors that govern MSC arrival within the tumor microenvironment. Our findings show that MSC chemoattraction is only present in select tumors, including osteosarcoma, and that the chemotactic potency among similar tumors varies substantially. Using an osteosarcoma xenograft model, we show that human MSCs traffic to the tumor within several hours of infusion. After arrival, MSCs are observed to localize in clusters near blood vessels and MSC-associated bioluminescence signal intensity is increased, suggesting that the seeded cells expand after engraftment. However, our studies reveal that a significant portion of MSCs are eliminated en route by splenic macrophage phagocytosis, effectively limiting the number of cells available for tumor engraftment. To increase MSC survival, we transiently depleted macrophages with liposomal clodronate, which resulted in increased tumor localization without substantial reduction in tumor-associated macrophages. Our data suggest that transient macrophage depletion will significantly increase the number of MSCs in the spleen and thus improve MSC localization within a tumor, theor. increasing the ED of an anti-cancer agent. This strategy may subsequently improve the clin. efficacy of MSCs as vehicles for the tumor-directed delivery of therapeutic agents.

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

Plouvier, Bertrand’s team published research in Heterocycles in 1991-04-01 | 72054-60-5

Heterocycles published new progress about 72054-60-5. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Application of C7H10N2O2S.

Plouvier, Bertrand; Bailly, Christian; Houssin, Raymond; Henichart, Jean Pierre published the artcile< Synthesis of two new thiazole-containing oligopeptides as potential DNA minor groove binding analogs of netropsin>, Application of C7H10N2O2S, the main research area is netrospin thiazole analog DNA binding.

On the basis of previous studies on synthetic models related to the antibiotic agents netropsin and distamycin A, the design and synthesis of two potential DNA minor groove ligands I and II are described. I and II were prepared by liquid-phase peptide synthesis from the key compounds Et 2-amino-5-methylthiazole-4-carboxylate and Et 2-aminothiazole-5-carboxylate, resp.

Heterocycles published new progress about 72054-60-5. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Application of C7H10N2O2S.

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

Hayashi, Kumiko’s team published research in Biophysical Journal in 2021-05-04 | 2222768-84-3

Biophysical Journal published new progress about Alzheimer disease. 2222768-84-3 belongs to class thiazole, and the molecular formula is C22H23F2N3O2S, Application In Synthesis of 2222768-84-3.

Hayashi, Kumiko; Miyamoto, Miki G.; Niwa, Shinsuke published the artcile< Effects of dynein inhibitor on the number of motor proteins transporting synaptic cargos>, Application In Synthesis of 2222768-84-3, the main research area is dynein inhibitor motor protein synaptic cargo.

Synaptic cargo transport by kinesin and dynein in hippocampal neurons was investigated by noninvasively measuring the transport force based on nonequilibrium statistical mechanics. Although direct phys. measurements such as force measurement using optical tweezers are difficult in an intracellular environment, the noninvasive estimations enabled enumerating force-producing units (FPUs) carrying a cargo comprising the motor proteins generating force. The number of FPUs served as a barometer for stable and long-distance transport by multiple motors, which was then used to quantify the extent of damage to axonal transport by dynarrestin, a dynein inhibitor. We found that dynarrestin decreased the FPU for retrograde transport more than for anterograde transport. This result indicates the applicability of the noninvasive force measurements. In the future, these measurements may be used to quantify damage to axonal transport resulting from neuronal diseases, including Alzheimer’s, Parkinson’s, and Huntington’s diseases.

Biophysical Journal published new progress about Alzheimer disease. 2222768-84-3 belongs to class thiazole, and the molecular formula is C22H23F2N3O2S, Application In Synthesis of 2222768-84-3.

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

Sun, Hua’s team published research in Chemistry – An Asian Journal in 2022-02-01 | 1003-32-3

Chemistry – An Asian Journal published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Quality Control of 1003-32-3.

Sun, Hua; Mu, Zifeng; Yang, Canglei; Zhang, Kai; Ji, Xingyu; Zhang, Tianshu; Ding, Huanda; Wang, Shifan; Dong, Liming; Zhang, Jing; Zhang, Qichun published the artcile< Facile Azabenz-Annulations through UV-induced Photocyclization: A Promising Method for Perylenediimide-Based Organic Semiconductors>, Quality Control of 1003-32-3, the main research area is bis azabenz annulated perylenediimide preparation optical electrochem semiconducting property; azabenz-annulations; perylenediimides; photocyclization; semiconductors; ultraviolet-induced.

Herein, four bis-azabenz-annulated PDIs (bis-AzaBPDIs) I (Ar = Ph, thiophen-2-yl, 2-cyanothiophen-5-yl, thiazol-5-yl) are concisely synthesized in high yields through UV-induced photocyclization, where the reaction processes including aldimine condensation, cyclization, and oxidative re-aromatization are investigated. The optical characterizations and theor. simulation reveal that the unique properties of the four bis-AzaBPDIs are comparable to their parent PDI. Organic field effect transistors with compounds I (Ar = thiophen-2-yl, 2-cyanothiophen-5-yl, thiazol-5-yl) as active layers indicated that all compounds showed unipolar electron transport properties with the mobilities of 1.1×10-3, 5.8×10-4, and 8.5×10-6 cm2 V-1 s-1, resp. These results suggest the great potential of bis-AzaBPDIs as organic semiconductors. The easy preparation approach reported in this work would renew research interest in developing bis-AzaBPDI-based optoelectronic mols.

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

Takakura, Hideo’s team published research in Molecules in 2021 | 2591-17-5

Molecules published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Takakura, Hideo published the artcile< Molecular design of D-luciferin-based bioluminescence and 1,2-dioxetane-based chemiluminescence substrates for altered output wavelength and detecting various molecules>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is review luciferin bioluminescence chemiluminescence substrate imaging reagent mol design; bioluminescence; chemiluminescence; design strategy; imaging; molecular probes; near infrared.

A review. Optical imaging including fluorescence and luminescence is the most popular method for the in vivo imaging in mice. Luminescence imaging is considered to be superior to fluorescence imaging due to the lack of both autofluorescence and the scattering of excitation light. To date, various luciferin analogs and bioluminescence probes have been developed for deep tissue and mol. imaging. Recently, chemiluminescence probes have been developed based on a 1,2- dioxetane scaffold. In this , the accumulated findings of numerous studies and the design strategies of bioluminescence and chemiluminescence imaging reagents are summarized.

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