Tag: 200-300

On May 1, 2017, Xu, Jiayi; Lin, Songnian; Myers, Robert W.; Trujillo, Maria E.; Pachanski, Michele J.; Malkani, Sunita; Chen, Hsuan-shen; Chen, Zhesheng; Campbell, Brian; Eiermann, George J.; Elowe, Nadine; Farrer, Brian T.; Feng, Wen; Fu, Qinghong; Kats-Kagan, Roman; Kavana, Michael; McMasters, Daniel R.; Mitra, Kaushik; Tong, Xinchun; Xu, Libo; Zhang, Fengqi; Zhang, Rui; Addona, George H.; Berger, Joel P.; Zhang, Bei; Parmee, Emma R. published an article.Recommanded Product: 859522-19-3 The title of the article was Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. And the article contained the following:

Systemically acting glucokinase activators (GKA) have been demonstrated in clin. trials to effectively lower blood glucose in patients with type II diabetes. However, mechanism-based hypoglycemia is a major adverse effect that limits the therapeutic potential of these agents. The authors hypothesized that the predominant mechanism leading to hypoglycemia is GKA-induced excessive insulin secretion from pancreatic β-cells at (sub-)euglycemic levels. The authors further hypothesized that restricting GK activation to hepatocytes would maintain glucose-lowering efficacy while significantly reducing hypoglycemic risk. Here the authors report the discovery of a novel series of carboxylic acid substituted GKAs based on pyridine-2-carboxamide. These GKAs exhibit preferential distribution to the liver vs. the pancreas in mice. SAR studies led to the identification of a potent and orally active hepatoselective GKA, compound I. GKA I demonstrated robust glucose lowering efficacy in high fat diet-fed mice at doses ≥10 mpk, with ≥70-fold liver:pancreas distribution, minimal effects on plasma insulin levels, and significantly reduced risk of hypoglycemia. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Recommanded Product: 859522-19-3

The Article related to glucokinase activator antidiabetic diabetes, diabetes, glucokinase, glucokinase activator (gka), glucose homeostasis, glucose metabolism, hepatoselective, hepatospecific, hexokinase iv, liver preferring, pyridine-2-carboxamide, type ii diabetes mellitus and other aspects.Recommanded Product: 859522-19-3

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

Prasanna, Gutta Lakshmi; Bharat, Y.; Sreenivasulu, Reddymasu; Rao, Mandava Venkata Basaveswara published an article in 2018, the title of the article was Synthesis and antibacterial activity of benzothiazole analogues.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole And the article contains the following content:

A series of novel benzothiazole fused derivatives I [R = Me, Cl, Br, I; R1 = Me, OMe] was designed, synthesized and screened for their antibacterial activity against Escherichia coli (MTCC 40) (Gram-neg.) and Staphylococcus aureus (MTCC 96)(Gram-pos.) bacteria. Among them, derivative I [R = Cl; R1 = Me] showed highest antibacterial activity against Gram-pos. and Gram-neg. bacteria. 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 benzothiazole preparation antibacterial, benzothiazolyl benzenamine preparation diketone potassium bisulfate catalyst paal knorr, thiobenzanilide preparation, benzanilide preparation, nitrobenzoyl chloride aniline reactant benzanilide preparation and other aspects.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On July 17, 2008, Murray, Anthony; Lau, Jesper; Vedsoe, Per; Christiansen, Lise Brown published a patent.Application of 859522-19-3 The title of the patent was Preparation of ureidothiazolylthioalkanoates as glucokinase activators. And the patent contained the following:

Title compounds were prepared for treatment of diabetes, impaired glucose tolerance, obesity, hyperglycemia, syndrome X, and dyslipidemia (no data). Thus, [2-(2-chlorobenzyloxy)ethyl]-(trans-4-methylcyclohexyl)amine TFA salt (preparation given), Et 3-(2-aminothiazol-5-ylthio)-2,2-dimethylpropionate (preparation given), carbonyldiimidazole, and DMAP were stirred together in THF for 18 h; EtOH and aqueous NaOH were added followed by heating at 75° for 5 h to give 53% 3-[2-[3-[2-(2-chlorobenzyloxy)ethyl]-3-(trans-4-methylcyclohexyl)ureido]thiazol-5-ylthio]-2,2-dimethylpropionic acid. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Application of 859522-19-3

The Article related to ureidothiazolylthioalkanoate preparation glucokinase activator, diabetes obesity hyperglycemia syndrome x treatment thiazolylthioalkanoate ureido preparation, methylcyclohexylureidothiazolylsulfanylalkanoate preparation antidiabetic and other aspects.Application of 859522-19-3

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

On April 30, 2004, Moloney, Gerard P.; Garavelas, Agatha; Martin, Graeme R.; Maxwell, Miles; Glen, Robert C. published an article.Category: thiazole The title of the article was Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor. And the article contained the following:

The synthesis and vascular 5-HT1B receptor activity of a novel series of substituted 3-amido phenylpiperazine and 4-(4-methyl-1-piperazinyl)-1-benzo[b]thiophene derivatives is described. Modifications to the amido linked sidechains of the 3-amidophenyl piperazine derivatives and to the 2-side-chain of the 1-benzo[b]thiophene derivatives have been explored. Several compounds were identified which exhibited affinity at the vascular 5-HT1B receptor of pKB > 7.0. From the 3-amidophenyl-piperazine series, N-[5-(4-chlorophenyl)-2-thiazolyl]-3-(4-methyl-1-piperazinyl)benzamide (I) and from the benzo[b]thiophene-4-piperazine series N-(2-ethylphenyl)-4-(4-methyl-1-piperazinyl)benzo[b]thiophene-2-carboxamide (II) were identified as a highly potent, silent (as judged by the inability of angiotensin II to unmask 5-HT1B receptor mediated agonist activity in the rabbit femoral artery) and competitive vascular 5-HT1B receptor antagonist. The affinity of compounds from these two series of compounds for the vascular 5-HT1B receptor is discussed as well as a proposed mode of binding to the receptor pharmacophore. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Category: thiazole

The Article related to 5-ht antagonists (type 5-ht1b), 5-ht1b receptors role: bsu (biological study, unclassified), biol (biological study) (antagonists), molecular modeling, pharmacophores, structure-activity relationship, serotoninergic antagonist and other aspects.Category: thiazole

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

Sagnou, Marina; Tzanopoulou, Stamatia; Raptopoulou, Catherine P.; Psycharis, Vassilis; Braband, Henrik; Alberto, Roger; Pirmettis, Ioannis C.; Papadopoulos, Minas; Pelecanou, Maria published an article in 2012, the title of the article was A Phenylbenzothiazole Conjugate with the Tricarbonyl fac-[M(I)(CO)3]+ (M = Re, 99Tc, 99mTc) Core for Imaging of β-Amyloid Plaques.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole And the article contains the following content:

The 2-(4′-aminophenyl)-6-methylbenzothiazole that is known to display affinity and specificity toward the amyloid plaques of Alzheimer’s disease (AD) has been joined to the tricarbonyl [M(CO)3NNO] chelate (M = Re, 99Tc, and 99mTc) through a five-carbon linker chain to generate the neutral complex (1) (namely, Re-1 for M = Re; 99Tc-1 for M = 99Tc; and 99mTc-1 for M = 99mTc) with the aim of developing a single-photon emission computed tomog. (SPECT) radiodiagnostic agent for AD. Re-1 was characterized by spectroscopic methods and x-ray crystallog., whereas the detailed NMR spectroscopic anal. of 99Tc-1 demonstrated its structural similarity to Re-1. Complexes Re-1 and 99Tc-1 display selective binding affinity for amyloid plaques as evidenced by fluorescence spectroscopy, whereas the biodistribution data of 99mTc-1 characterized by relatively low brain uptake, fast clearance from brain and blood, and in vivo stability are considered encouraging for further elaboration on the structural features of 1 in the direction of increased brain uptake. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to radiolabeled benzothiazole chelate conjugate spect imaging amyloid alzheimers, crystal structure rhenium benzothiazolyl phenylaminocarbonylbutyl pyridinylmethyl aminoacetate tricarbonyl complex, mol structure rhenium benzothiazolyl phenylaminocarbonylbutyl pyridinylmethyl aminoacetate tricarbonyl complex and other aspects.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

The author of 《1-Phenyl-N-(benzothiazol-2-yl)methanimine derivatives as Middle East respiratory syndrome coronavirus inhibitors》 were Hu, Min-Qi; Li, Heng; Lin, Ying; Zhang, Ying; Tang, Jie; Zuo, Jian-Ping; Yu, Li-Fang; Tong, Xian-Kun; Tang, Wei; Yang, Fan. And the article was published in RSC Advances in 2020. Synthetic Route of C7H3BrFNS The author mentioned the following in the article:

Middle East respiratory syndrome coronavirus (MERS-CoV) poses a serious threat to human health, and currently there are no effective or specific therapies available to treat it. Herein a series of 1-phenyl-N-(benzothiazol-2-yl)methanimine derivatives with inhibitory activity against MERS-CoV are described. The compound 4f with a 50% inhibition concentration value of 0.09 μM is a promising inhibitor that warrants further evaluation, towards the development of potential anti-MERS-CoV drugs. After reading the article, we found that the author used 2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7Synthetic Route of C7H3BrFNS)

2-Bromo-6-fluorobenzothiazole(cas: 152937-04-7) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Synthetic Route of C7H3BrFNSTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.

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

Zhang, Qian; Liu, Xiaobo; Gan, Wenhui; Wu, Jinjin; Zhou, Hualan; Yang, Zunhua; Zhang, Yiling; Liao, Min; Yuan, Ping; Xu, Shan; Zheng, Pengwu; Zhu, Wufu published an article in ACS Omega. The title of the article was 《Discovery of Triazolo-pyridazine/-pyrimidine Derivatives Bearing Aromatic (Heterocycle)-Coupled Azole Units as Class II c-Met Inhibitors》.Application of 144060-98-0 The author mentioned the following in the article:

Two series of novel triazolo-pyridazine/-pyrimidine derivatives were designed, synthesized, and evaluated for their inhibitory activity against c-Met kinase, as well as three c-Met overexpressed cancer cell lines (A549, MCF-7, and HeLa) and one normal human hepatocytes cell line LO2 in vitro. The most promising compound I exhibited significant cytotoxicity against A549, MCF-7, and HeLa cell lines with IC50 values of 1.06 +/- 0.16, 1.23 +/- 0.18, and 2.73 +/- 0.33μM, resp. Moreover, the inhibitory activity of compound I against c-Met kinase (IC50 = 0.090μM) was equal to that of Foretinib (IC50 = 0.019μM). The result of the acridine orange single staining test demonstrated that compound I could remarkably induce apoptosis of A549 cells. The results of apoptosis and cycle distribution of cells showed that compound I could induce late apoptosis of A549 cells and stimulate A549 cells arresting in the G0/G1 phase. Structure-activity relationships (SARs), pharmacol. results, and docking studies indicated that the introduction of 5-methylthiazole fragment to the five-atom moiety was beneficial for the activity. So far, the existing data indicated that I may become a potential class II c-Met inhibitor. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Application of 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Application of 144060-98-0

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

Li, Guoliang; He, Yundong; Zhou, Wenbo; Wang, Peng; Zhang, Yong; Tong, Weiguang; Wu, Haigang; Liu, Mingyao; Ye, Xiyun; Chen, Yihua published an article on February 1 ,2014. The article was titled 《Identification, synthesis and photo-protection evaluation of arylthiazole derivatives as a novel series of sunscreens》, and you may find the article in Heterocycles.Recommanded Product: 144060-98-0 The information in the text is summarized as follows:

A series of arylthiazole derivatives I [R3 = C6H5, C6H5CH2, C6H5CH2CH2], II [R1 = C6H5, 4-BrC6H4, 3-H3COC6H4, 2-H3COC6H4], III [n= 1, 2, 3, 5; R = H, n-Pr, n-Bu, Et; R2 = OMe, OEt] and IV [R1 = H, CF3, OMe, Cl; R2 = H, Cl; R3 = H, Cl] was designed and synthesized. Addnl., phenylfuran derivative V [X = O; Y = C; R = H], phenylthiophene derivative V [X = S; Y = C; R = H], phenyloxazole derivative V [X = O; Y = N; R = Me], N-(Ethoxycarbonylmethyl)-2-phenyl-4-thiazolecarboxamide and N-(Ethoxycarbonylmethyl)-3-phenyl-5-methyl-4-isooxazolecarboxamide were also prepared All the synthesized compounds were evaluated for their photo-protective effect against UVB exposure induced cellular damage in keratinocytes cell (HaCaT) and their structure-activity relationship (SAR) was discussed. Among the tested compounds, compound III [n = 1; R = Et; R2 = OEt] significantly protected the dorsal skin of BALB/c-nu mice against UVB-induced decrustation in vivo. The in vitro and in vivo data for these arylthiazole derivatives suggest further studies for their potential use as photo-protection agents as well as sunscreen candidates. After reading the article, we found that the author used 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Recommanded Product: 144060-98-0)

4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Recommanded Product: 144060-98-0

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

Arora, Amandeep; Teegardin, Kip A.; Weaver, Jimmie D. published their research in Organic Letters on August 7 ,2015. The article was titled 《Reductive Alkylation of 2-Bromoazoles via Photoinduced Electron Transfer: A Versatile Strategy to Csp2-Csp3 Coupled Products》.Reference of 2-Bromo-4-chlorobenzo[d]thiazole The article contains the following contents:

Access to Csp2-Csp3-coupled products is a challenging goal at the forefront of catalysis. The photocatalytic reductive coupling of aryl bromides with unactivated alkenes is introduced as a convenient method that circumvents any need for synthesis of sp3-hybridized coupling partners. The reaction takes place via photoinduced electron transfer from a tertiary amine to an aryl bromide that fragments to provide an aryl radical and subsequently reacts with an alkene to form a C-C bond. Conveniently, the amine also serves as the final reductant. The method is operationally simple, functional group tolerant, and takes place with selectivities that will allow it to be used in the context of complex mol. synthesis. The experimental process involved the reaction of 2-Bromo-4-chlorobenzo[d]thiazole(cas: 3622-40-0Reference of 2-Bromo-4-chlorobenzo[d]thiazole)

2-Bromo-4-chlorobenzo[d]thiazole(cas: 3622-40-0) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Reference of 2-Bromo-4-chlorobenzo[d]thiazoleTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.

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

In 1989,Dyes and Pigments included an article by Rangnekar, D. W.; Chaudhari, M. B.. Computed Properties of C11H13N3OS. The article was titled 《Synthesis of disperse azo dyes from 2-amino-4- and 6-N,N-dialkylaminobenzothiazoles and their application》. The information in the text is summarized as follows:

2-Amino-6-(dialkylamino)benzothiazole and 2-amino-4-(dialkylamino)-6-thiocyanatobenzothiazoles were prepared by condensation of 4-(dialkylamino)anilines and 2-(dialkylamino)anilines, resp., with NH4SCN and bromine in HOAc. These amines were diazotized and coupled with substituted N,N-dialkylanilines to give 2-[substituted-4-(dialkylamino)phenylazo]-6-(dialkylamino)benzothiazole dyes (I; NR1R2 = NEt2, morpholino, piperidino; R3 = Me, Et, 2-hydroxyethyl; R4 = Me, 2-cyanoethyl; X = H, OMe; Y = H, AcNH) and 2-[substituted-4-(dialkylamino)phenylazo]-6-thiocyanato-4-(dialkylamino)benzothiazole dyes (II; NR1R2, R3, R4, X, Y as for I). I and II were applied to polyester and polyamide fibers and their dyeing properties assessed. In the experiment, the researchers used 6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2Computed Properties of C11H13N3OS)

6-Morpholinobenzo[d]thiazol-2-amine(cas: 94641-22-2) 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 C11H13N3OSTheir presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.

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