Month: February 2023

Synthesis and study of novel benzothiazole derivatives with potential nonlinear optical properties was written by Sigmundova, Ivica;Zahradnik, Pavol;Loos, Dusan. And the article was included in Collection of Czechoslovak Chemical Communications in 2007.COA of Formula: C8H6N2O2S This article mentions the following:

The synthesis of new benzothiazole push-pull systems as candidates for NLO-phores is described. Spectral (UV/VIS and solvatochromic) and theor. studies (electronic properties based on semiempirical AM1 and PM3 methods) of the prepared compounds were carried out. The structure and physico-chem. parameters affecting the push-pull character and intramol. charge transfer (ICT) of the studied compounds have been investigated and compounds with enhanced hyperpolarizability β have been predicted. The benzothiazolium salts were found to be much more effective NLO-phores in comparison with the corresponding neutral benzothiazoles. The 4-NPh₂ group is the most effective donor. The extension of conjugated bridge improves the studied NLO characteristics. An addnl. acceptor group bonded to the heterocycle causes a red shift of λ_max but does not increase hyperpolarizability. In the experiment, the researchers used many compounds, for example, 2-Methyl-6-nitrobenzothiazole (cas: 2941-63-1COA of Formula: C8H6N2O2S).

2-Methyl-6-nitrobenzothiazole (cas: 2941-63-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.COA of Formula: C8H6N2O2S

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

Integrative multi-biomarker approach on caged rainbow trout: A biomonitoring tool for wastewater treatment plant effluents toxicity assessment was written by Beghin, Mahaut;Paris-Palacios, Severine;Mandiki, Syaghalirwa N. M.;Schmitz, Melodie;Palluel, Olivier;Gillet, Erin;Bonnard, Isabelle;Nott, Katherine;Robert, Christelle;Porcher, Jean-Marc;Ronkart, Sebastien;Kestemont, Patrick. And the article was included in Science of the Total Environment in 2022.Reference of 14769-73-4 This article mentions the following:

The complex mixtures of contaminants released in wastewater treatment plant (WWTP) effluents are a major source of pollution for aquatic ecosystems. The present work aimed to assess the environmental risk posed by WWTP effluents by applying a multi-biomarker approach on caged rainbow trout (Oncorhynchus mykiss) juveniles. Fish were caged upstream and downstream of a WWTP for 21 days. To evaluate fish health, biomarkers representing immune, reproductive, nervous, detoxification, and antioxidant functions were assayed. Biomarker responses were then synthesized using an Integrated Biomarker Response (IBR) index. The IBR highlighted similar response patterns for the upstream and downstream sites. Caged juvenile females showed increased activities of innate immune parameters (lysozyme and complement), histol. lesions and reduced glycogen content in the hepatic tissue, and higher muscle cholinergic metabolism However, the intensity of the observed effects was more severe downstream of the WWTP. The present results suggest that the constitutive pollution level of the Meuse River measured upstream from the studied WWTP can have deleterious effects on fish health condition, which are exacerbated by the exposure to WWTP effluents. Our results infer that the application of IBR index is a promising tool to apply with active biomonitoring approaches as it provides comprehensive information about the biol. effects caused by point source pollution such as WWTP, but also by the constitutive pollutions levels encountered in the receiving environment. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4Reference of 14769-73-4).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Reference of 14769-73-4

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

Pulmonary Delivery of Levamisole Nanoparticles as an Immunomodulator Affecting Th and a Potential ADAM10 Inhibitor to Ameliorate Severe Allergic Asthma was written by Fang, Liping;Nikfarjam, Nasser;Gharagozlou, Mohammad;Huang, Tao;Song, Yu;Islambulchilar, Ziba;Esmaeilzadeh, Abdolreza;Jafari, Davood;Athari, Seyyed Shamsadin. And the article was included in ACS Biomaterials Science & Engineering in 2022.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole This article mentions the following:

Asthma is a common chronic lung disease without absolute treatment, and hypersensitivity reactions and type 2 immune responses are responsible for asthma pathophysiol. ADAM10 as a metalloproteinase transmembrane protein is critical for development of Th2 responses, and levamisole as an anthelmintic drug has immunomodulatory effects, which not only regulates ADAM10 activity but also can suppress the bone marrow and neutrophil production Therefore, in the present study, nanoparticles were used as a levamisole delivery system to reduce bone marrow suppression, and the immunomodulatory and ADAM10 inhibitory effects of levamisole were studied in allergic asthma. Asthmatic mice were treated with PLGA-levamisole nanoparticles. Then, AHR, BALF, and blood cell counts, levels of the IgG1 subclass, total and OVA-specific IgE, IL2, IL-4, IL-5, IL-10, IL-13, IL-17, IL-25, IL-33, INF-γ, and TNF-α, gene expression of FoxP3, T-bet, RORγt, PU.1, GATA3, FcεRII, CysLT1R, eotaxin, and ADAM10, and lung histopathol. were evaluated. PLGA-LMHCl with considered characteristics could control airway hyper-responsiveness, eosinophils in the BALF, levels of Igs, Th2-, Th9-, and Th17-derived cytokines and pivotal genes, eosinophilic inflammation, hyperplasia of the goblet cell, and hyperprodn. of mucus and could increase Th1- and Treg-derived cytokines and also pivotal genes. It could also modulate the ADAM10 activity and had no effect on the number of neutrophils in the bloodstream. The novel safe nanodrug had no side effect on the bone marrow to produce neutrophils and could control the allegro-immuno-inflammatory response of asthma. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole

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

A Double-Clicking Bis-Azide Fluorogenic Dye for Bioorthogonal Self-Labeling Peptide Tags was written by Demeter, Orsolya;Fodor, Eszter A.;Kallay, Mihaly;Mezo, Gabor;Nemeth, Krisztina;Szabo, Pal T.;Kele, Peter. And the article was included in Chemistry – A European Journal in 2016.Application of 2942-06-5 This article mentions the following:

Herein, the authors give the very first example for the development of a fluorogenic mol. probe that combines the two-point binding specificity of biarsenical-based dyes with the robustness of bioorthogonal click-chem. This proof-of-principle study reports on the synthesis and fluorogenic characterization of a new, double-quenched, bis-azide fluorogenic probe suitable for bioorthogonal two-point tagging of small peptide tags by double strain-promoted azide-alkyne cycloaddition The presented probe exhibits remarkable increase in fluorescence intensity when reacted with bis-cyclooctynylated peptide sequences, which could also serve as possible self-labeling small peptide tag motifs. In the experiment, the researchers used many compounds, for example, 6-Nitrobenzothiazole (cas: 2942-06-5Application of 2942-06-5).

6-Nitrobenzothiazole (cas: 2942-06-5) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Application of 2942-06-5

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

The interaction of chlorinated 6-spiroepoxypenicillins with Bacillus cereus β-lactamase I: irreversible inhibition and turnover was written by Bycroft, Barrie W.;Gledhill, Linden;Shute, Richard E.;Williams, Paul. And the article was included in Journal of the Chemical Society, Chemical Communications in 1988.COA of Formula: C4H7NS This article mentions the following:

Two chlorinated 6-spiroepoxypenicillin anilides were irreversible inhibitors of β-lactamase I (penicillinase) of B. cereus, but they were also turned over by this enzyme to yield the same hydrolysis product, whose structure was determined to be an unusual 6-substituted-1,4-dihydrothiazine-3-carboxylate, α-ketoamide; a possible pathway for the turnover and inhibitory processes associated with these interactions is presented. In the experiment, the researchers used many compounds, for example, 2-Methyl-4,5-dihydrothiazole (cas: 2346-00-1COA of Formula: C4H7NS).

2-Methyl-4,5-dihydrothiazole (cas: 2346-00-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.COA of Formula: C4H7NS

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

Design and discovery of novel thiazole derivatives as potential MMP inhibitors to protect against acute lung injury in sepsis rats via attenuation of inflammation and apoptotic oxidative stress was written by Ge, Lingqing;Hu, Qiaozhen;Shi, Mengrao;Yang, Huiyun;Zhu, Guoji. And the article was included in RSC Advances in 2017.Product Details of 2103-99-3 This article mentions the following:

Acute lung injury (ALI) is considered to be an inflammatory syndrome of the airway system that is initiated by failure of the respiratory system. In this study, we evaluated the possible benefits of some novel thiazole derivatives against ALI. These derivatives were synthesized and evaluated for the inhibition of MMP-8 and MMP-2. Most of the tested compounds had better inhibitory activity for MMP-8 than for MMP-2, with compound 26 being the most potent analog among the tested series. Thus, compound 26 was further investigated to determine its beneficial effects in an ALI model of rats with sepsis. In vivo results suggested that compound 26 significantly reduced the protein concentration together with a decline in enhanced leukocytes compared with those in ALI induced by cecal ligation and puncture. The effect of compound 26 on myeloperoxidase activity was also quantified, which was found to be significantly reduced at the maximum tested dose of 20 mg kg^-1. The protective effect of compound 26 against ALI was also established to occur via the significant modulation of various biomarkers; for example, the malondialdehyde level was found to be reduced, while there were increased levels of superoxide dismutase and glutathione. Thus, it is proposed that compound 26 exerts a protective effect against ALI via modulation of the antioxidant status. Furthermore, the compounds tested caused significant attenuation of the levels of tumor necrosis factor-α, interleukin-1β, and interleukin-6, and protected the lung through the modulation of systemic inflammatory mediators in septic rats. In conclusion, we identified a novel series of thiazoles, which potentially exert protective effects against ALI via the inhibition of numerous pathways. In the experiment, the researchers used many compounds, for example, 4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3Product Details of 2103-99-3).

4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Product Details of 2103-99-3

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

Volatile compounds and odor preferences of ground beef added with garlic and red wine, and irradiated with charcoal pack was written by Lee, Kyung Haeng;Yun, Hyejeong;Lee, Ju Woon;Ahn, Dong Uk;Lee, Eun Joo;Jo, Cheorun. And the article was included in Radiation Physics and Chemistry in 2012.Reference of 15679-19-3 This article mentions the following:

Irradiation is the most efficient non-thermal technol. for improving hygienic quality and extending the shelf-life of food products. One of the adverse effects of food irradiation, however, is off-flavor production, which significantly affects the sensory preferences for certain foods. In this study, garlic (5%, weight/weight) and red wine (1:1, weight/weight) were added to ground beef to increase the radiation sensitivity of pathogens and improve meat odor/flavor. Samples were irradiated at 0 or 5 kGy in the presence of charcoal pack. SPME-GC-MS anal. was performed to measure the changes in the volatile compounds and sensory characteristics of the samples. The amount of total volatile compounds produced from ground beef was greater when the sample was irradiated. When garlic and red wine were added to the ground beef, the amount of volatile compounds significantly increased, and the amount of volatile compounds increased even further after irradiation However, when the samples were irradiated with charcoal pack, the amount of volatile compounds decreased significantly. Sensory evaluation indicated that charcoal pack significantly increased the odor preferences for both irradiated and non-irradiated ground beef added with garlic. These results indicated that addition of charcoal pack to ground beef could reduce off-odor problems induced by irradiation, and this effect was consistent even when certain additives such as garlic and red wine were added. In the experiment, the researchers used many compounds, for example, 2-Ethoxythiazole (cas: 15679-19-3Reference of 15679-19-3).

2-Ethoxythiazole (cas: 15679-19-3) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 15679-19-3

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

Agonist-directed trafficking of porcine α_2A-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates G_s was written by Brink, Christiaan B.;Wade, Susan M.;Neubig, Richard R.. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 2000.Electric Literature of C10H17Cl2N3S This article mentions the following:

In this study, we investigated the hypothesis of agonist-directed trafficking of receptor signaling for the α_2A-adrenergic receptor (α_2A-AR). α_2A-ARs couple to both G_s and G_i to stimulate or inhibit adenylyl cyclase activity. Chinese hamster ovary-K1 cell lines expressing the porcine α_2A-AR at high (α_2A-H) and low (α_2A-L) levels were used to estimate the relative efficacies (R.e.s) of a series of agonists for the G_s and G_i pathways. G_s-mediated responses were measured after pertussis toxin treatment to inactivate G_i in α_2A-H, whereas G_i responses were measured in α_2A-L, where G_s responses were absent. The full agonist UK-14,304 showed a large receptor reserve for G_i responses in α_2A-H but little receptor reserve for G_s responses in α_2A-H or for G_i responses in α_2A-L. With the exception of l-isoproterenol (ISO), all agonists showed similar R.e.s. at the α_2A-AR for G_s and G_i responses, with rank orders of R.e.s as follows: l-epinephrine = l-norepinephrine = UK-14,304 > p-aminoclonidine ≥ BHT-920 ≥ BHT-933 > clonidine = p-iodoclonidine ≥ xylazine ≥ guanabenz. Interestingly, ISO had the highest efficacy at the α_2A-AR for activating G_s vs. G_i (9-fold higher); however, it had low potency for both. By several criteria, the ISO response was mediated by the α_2A-AR, supporting the hypothesis of agonist-directed trafficking of receptor signaling or agonist-specific G protein selectivity. In contrast, the apparent G_i pathway selectivity of oxymetazoline appears to be mediated by an endogenous serotonergic receptor. It is intriguing that a classic β-AR agonist that activates G_s through β₂-ARs also appears to produce a G_s-selective conformation of the G_i-coupled α_2A-AR. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Electric Literature of C10H17Cl2N3S).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C10H17Cl2N3S

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

Novel high/low solubility classification methods for new molecular entities was written by Dave, Rutwij A.;Morris, Marilyn E.. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2016.Related Products of 16595-80-5 This article mentions the following:

This research describes a rapid solubility classification approach that could be used in the discovery and development of new mol. entities. Compounds (N = 635) were divided into two groups based on information available in the literature: high solubility (BDDCS/BCS 1/3) and low solubility (BDDCS/BCS 2/4). We established decision rules for determining solubility classes using measured log solubility in molar units (MLogS_M) or measured solubility (MSol) in mg/mL units. ROC curve anal. was applied to determine statistically significant threshold values of MSol and MLogS_M. Results indicated that NMEs with MLogS_M > -3.05 or MSol > 0.30 mg/mL will have ≥85% probability of being highly soluble and new mol. entities with MLogS_M ≤ -3.05 or MSol ≤ 0.30 mg/mL will have ≥85% probability of being poorly soluble When comparing solubility classification using the threshold values of MLogS_M or MSol with BDDCS, we were able to correctly classify 85% of compounds We also evaluated solubility classification of an independent set of 108 orally administered drugs using MSol (0.3 mg/mL) and our method correctly classified 81% and 95% of compounds into high and low solubility classes, resp. The high/low solubility classification using MLogS_M or MSol is novel and independent of traditionally used dose number criteria. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride (cas: 16595-80-5Related Products of 16595-80-5).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride (cas: 16595-80-5) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Related Products of 16595-80-5

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

Suppression of glioblastoma by a drug cocktail reprogramming tumor cells into neuronal like cells was written by Gao, Longfei;Huang, Shichao;Zhang, Hong;Hua, Wei;Xin, Shunmei;Cheng, Lin;Guan, Wuqiang;Yu, Yongchun;Mao, Ying;Pei, Gang. And the article was included in Scientific Reports in 2019.Category: thiazole This article mentions the following:

Glioblastoma (GBM) is the most common and aggressive malignant tumor in adult brain. Even with the current standard therapy including surgical resection followed by postoperative radiotherapy and chemotherapy with temozolomide (Temo), GBM patients still have a poor median survival. Reprogramming of tumor cells into non-malignant cells might be a promising therapeutic strategy for malignant tumors, including GBM. Based on previous studies using small mols. to reprogram astrocytes into neuronal cells, here we further identified a FTT cocktail of three commonly used drugs (Fasudil, Tranilast, and Temo) to reprogram patient-derived GBM cells, either cultured in serum containing or serum-free medium, into neuronal like cells. FTT-treated GBM cells displayed a neuronal like morphol., expressed neuronal genes, exhibited neuronal electrophysiol. properties, and showed attenuated malignancy. More importantly, FTT cocktail more significantly suppressed tumor growth and prolonged survival in GBM patient derived xenograft than Temo alone. Our study provided preclin. evidence that the neuronal reprogramming drug cocktail might be a promising strategy to improve the existing treatment for GBM. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Category: thiazole).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

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