Category: 50850-93-6

Electric Literature of 50850-93-6, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate, molecular formula is C10H10N2O2S. In a Article£¬once mentioned of 50850-93-6

Starting from the structure of thioperamide, a known H3-antagonist, a new series of compounds with a benzothiazole nucleus instead of the cyclohexylcarbothioamide moiety was synthesized. Various substituents, selected by experimental design, were introduced in position 6 of the benzothiazole nucleus, in order to change its physico-chemical characteristics. The lipophilicity of the synthesized compounds was measured by means of RP-HPLC, and their H3-receptor affinity was evaluated by competitive binding assays on rat cortex synaptosomes, with the labelled ligand N(alpha)-[3H]methylhistamine. A QSAR analysis was performed on the experimental data, using also substituent constants taken from the literature. The newly synthesized compounds showed lower H3-affinities than thioperamide; quantitative structure-activity relationships, described by models obtained with PLS and MRA techniques, were observed among benzothiazole derivatives. According to these relationships, any attempt to improve the potency of these compounds should involve the substitution of the benzothiazole moiety with less bulky and/or more flexible structures, which should also be less lipophilic and allow better electronic interactions with the binding site. 1-(Benzothiazol-2-yl)-4-[(1H)-imidazol-4-yl]piperidine represents a limit structure for H3-activity, since it seems impossible to improve its affinity by means of substitution in the studied position of the benzothiazole nucleus, as shown by predictions performed by a PLS model.

Starting from the structure of thioperamide, a known H3-antagonist, a new series of compounds with a benzothiazole nucleus instead of the cyclohexylcarbothioamide moiety was synthesized. Various substituents, selected by experimental design, were introduced in position 6 of the benzothiazole nucleus, in order to change its physico-chemical characteristics. The lipophilicity of the synthesized compounds was measured by means of RP-HPLC, and their H3-receptor affinity was evaluated by competitive binding assays on rat cortex synaptosomes, with the labelled ligand N(alpha)-[3H]methylhistamine. A QSAR analysis was performed on the experimental data, using also substituent constants taken from the literature. The newly synthesized compounds showed lower H3-affinities than thioperamide; quantitative structure-activity relationships, described by models obtained with PLS and MRA techniques, were observed among benzothiazole derivatives. According to these relationships, any attempt to improve the potency of these compounds should involve the substitution of the benzothiazole moiety with less bulky and/or more flexible structures, which should also be less lipophilic and allow better electronic interactions with the binding site. 1-(Benzothiazol-2-yl)-4-[(1H)-imidazol-4-yl]piperidine represents a limit structure for H3-activity, since it seems impossible to improve its affinity by means of substitution in the studied position of the benzothiazole nucleus, as shown by predictions performed by a PLS model.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 50850-93-6 is helpful to your research., Electric Literature of 50850-93-6

Reference£º
Thiazole | C3H10651NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,molecular formula is C10H10N2O2S, is a conventional compound. this article was the specific content is as follows.category: thiazole

Three series of novel 4-benzothiazole amino quinazolines Dasatinib derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro cytotoxic activity by the MTT-based assay against 6 human cancer cell lines. Compared with the parental Dasatinib, most of the new compounds, especially 2, 4, 6-trimethylaniline series (3), demonstrated significant inhibitory activities against six cell lines. Furthermore, the target compounds were screened for Src and Abl kinase inhibitory activity. Among them, 1a, 1f and 3a-3f are more potential dual Src/Abl kinase inhibitors. Thus they may be promising lead compounds to be developed as an alternative for current Dasatinib therapy or for Imatinib-resistant patients, potentially via simultaneously blocking multiple RTK signaling pathways.

Three series of novel 4-benzothiazole amino quinazolines Dasatinib derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro cytotoxic activity by the MTT-based assay against 6 human cancer cell lines. Compared with the parental Dasatinib, most of the new compounds, especially 2, 4, 6-trimethylaniline series (3), demonstrated significant inhibitory activities against six cell lines. Furthermore, the target compounds were screened for Src and Abl kinase inhibitory activity. Among them, 1a, 1f and 3a-3f are more potential dual Src/Abl kinase inhibitors. Thus they may be promising lead compounds to be developed as an alternative for current Dasatinib therapy or for Imatinib-resistant patients, potentially via simultaneously blocking multiple RTK signaling pathways.

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Thiazole | C3H10632NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,molecular formula is C10H10N2O2S, is a conventional compound. this article was the specific content is as follows.HPLC of Formula: C10H10N2O2S

Novel non-nucleoside tricyclic platelet ADP receptor (P2Y12) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.

Novel non-nucleoside tricyclic platelet ADP receptor (P2Y12) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.

Do you like my blog? If you like, you can also browse other articles about this kind. HPLC of Formula: C10H10N2O2S. Thanks for taking the time to read the blog about 50850-93-6

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Thiazole | C3H10657NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,molecular formula is C10H10N2O2S, is a conventional compound. this article was the specific content is as follows.50850-93-6

Novel non-nucleoside tricyclic platelet ADP receptor (P2Y12) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.

Novel non-nucleoside tricyclic platelet ADP receptor (P2Y12) antagonists have been discovered that bind reversibly and with high affinity to the platelet receptor. Condensation of various 2-aminobenzothiazoles with chlorosulfonylacetyl chloride affords these novel tricyclic heterocycles, which are novel and unpredicted products of this reaction.

Do you like my blog? If you like, you can also browse other articles about this kind. 50850-93-6. Thanks for taking the time to read the blog about 50850-93-6

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Thiazole | C3H10657NS – PubChem,
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50850-93-6,Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,as a common compound, the synthetic route is as follows.

50850-93-6, Step 1: To a solution of tert-butyl nitrite (4.5 mL, 37.5 mmol) and copper(II) bromide (6.0 g, 27 mmol) in CH3CN(100 mL) at rt was added a mixture of ethyl 2-aminobenzo[d]thiazole-6-carboxylate (5.0 g, 22.5 mmol) in CH3CN (50mL). The reaction suspension was stirred at rt for 1 h. The resulting reaction mixture was quenched with 300 mL of 1 NHCl aqueous solution and extracted with CH2Cl2 (3×200 mL). The combined organic layers were dried over MgSO4,and concentrated under reduced pressure. The crude product was purified on a silica gel column using a mixture ofCH2Cl2-hexanes (4:1, v/v) as eluent to give ethyl 2-bromobenzo[d]thiazole-6-carboxylate as a white solid (6.2 g, 96%).1H NMR (300 MHz, CDCl3) delta 8.54 (d, J= 1.1 Hz, 1H), 8.16 (dd, J= 1.5, 8.7 Hz, 1H), 8.02 (d, J = 8.7 Hz, 1H), 4.43 (q, J=7.2 Hz, 2H), 1.43 (t, J= 7.2 Hz, 3H). LCMS (ESI) m/z 288, 286 (M+H)+.

As the paragraph descriping shows that 50850-93-6 is playing an increasingly important role.

Reference£º
Patent; Ambit Biosciences Corporation; HADD, Michael J.; HOCKER, Michael D.; HOLLADAY, Mark W.; LIU, Gang; ROWBOTTOM, Martin W.; XU, Shimin; (299 pag.)EP2766359; (2016); B1;,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.50850-93-6,Ethyl 2-aminobenzo[d]thiazole-6-carboxylate,as a common compound, the synthetic route is as follows.

Commercially available ester 1 (1.0g, 4.5mmol) was dissolved in anhydrous THF and the RB flask was cooled to 0C. Then LiAlH4 was added slowly and the flask was stirred at 0C for additional 10min. The flask was then stirred at room temperature for 24h. The reaction was then cooled, quenched with methanol, NH4Cl Rochelle’s salt and diluted with ethyl acetate (10ml). The organic layer was separated and the aqueous layer was extracted with additional ethyl acetate (3¡Á10ml). The organic layers were combined, dried over Na2SO4 and concentrated under vacuo on a rotary evaporator to obtain a yellow solid. The crude product was purified via gradient silica gel column chromatography using a mixture of CH2Cl2 and methanol (100:1 to 5:1) to obtain the desired alcohol as yellow solid 2 (420mg, 52%). (0009) 1H NMR (500MHz, CDCl3): delta 7.57 (d, J=0.9Hz, 1H), 7.35-7.46 (m, 1H), 7.25 (dd, J=8.2, 1.8Hz, 1H), 6.45 (br s, 1H), 4.53 (s, 2H), 4.0 (br s, 1H). (0010) 13C NMR (125MHz, CDCl3): delta 167.6, 150.5, 134.9, 130.6, 125.1, 119.4, 117.7, 64.2,., 50850-93-6

The synthetic route of 50850-93-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Dutta, Aloke K.; Santra, Soumava; Harutyunyan; Das, Banibrata; Lisieski, Michael J.; Xu, Liping; Antonio, Tamara; Reith, Maarten E.A.; Perrine, Shane A.; European Journal of Pharmacology; vol. 862; (2019);,
Thiazole | C3H3NS – PubChem
Thiazole | chemical compound | Britannica