09/29/21 News Discovery of Ethyl 2-aminobenzo[d]thiazole-6-carboxylate

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Novel methotrexate (MTX) derivatives bearing dihydro-2H-1,4- benzothiazine or dihydro-2H-1,4-benzoxazine were synthesized and tested for in vitro antiproliferative activities against human synovial cells (hSC) and human peripheral blood mononuclear cells (hPBMC) obtained from patients with rheumatoid arthritis and healthy volunteers, respectively. In vivo antiarthritic activities of these derivatives were also evaluated in a rat adjuvant arthritis model. N-[[4-[(2,4-Diaminopteridin-6-yl)methyl]-3,4- dihydro-2H-1,4-benzothiazin-7-yl]carbonyl]-L-glutamic acid (3c) exhibited more potent antiproliferative activities in hSC and hPBMC than MTX in vitro. Antiproliferative activities of N-[[4-[(2,4-diaminopteridin-6-yl)methyl]- 3,4-dihydro-2H-1,4-benzoxazin-7-yl]carbonyl]-L-homoglutamic acid (3b) and N- [[4-[(2,4-diaminopteridin-6-yl)methyl]-3,4-dihydro-2H-1,4-benzothiazin-7- yl]carbonyl]-L-homoglutamic acid (3d) (MX-68) were comparable to that of MTX in these in vitro assays. Compounds 3b,d (MX-68) significantly suppressed progression of the adjuvant arthritis in a dose-dependent manner ranging from 0.5 to 2.5 mg/kg (po). In addition, 3d (MX-68) completely suppressed this progression at the dose of 2.5 mg/kg (po). Importantly, 3d (MX-68) having benzothiazine and homoglutamate, as expected, did not undergo polyglutamation, a process which may be responsible for the associated side effects of MTX. These results suggest that 3d (MX-68) is a potent and safe candidate antirheumatic agent, absent of the side effects of MTX.

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Reference:
Thiazole | C3H10658NS – PubChem,
Thiazole | chemical compound | Britannica

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The syntheses of a series of 2-acetamido-6-alkoxycarbonylbenzthiazoles (12-17), 2-alkoxycarbonylamino-6-alkoxycarbonylbenzthiazoles (18-27), 2-alkoxycarbonylamino-6-benzoylbenzthiazoles (29,30), and 2,2′-dicarbalkoxyamino-6,6′-dibenzthiazolyl oxides, sulphides and sulphones (38-43) have been carried out as structural congeners of tioxidazole (2) and related anthelmintics (3 and 4).All the benzthiazoles have been evaluated for their anthelmintic activity against Ancylostoma ceylanicum in hamsters, Hymenolepis nana in mice and Litomosoides carinii in cotton rats.Compound 15 showes more than 85percent clearance of hookworms (A. ceylanicum) at an oral dose of 250 mg/kg, while compound 24 eliminates nearly 90percent of the microfilariae in blood and also kills 50percent of the adult filarial worms at an intraperitonial dose of 30 mg/kg * 5 from the cotton rats infected with Litomosoides carinii.

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Reference:
Thiazole | C3H10635NS – PubChem,
Thiazole | chemical compound | Britannica

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.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, Application In Synthesis of Ethyl 2-aminobenzo[d]thiazole-6-carboxylate

In the current study aimed to investigate a number of heterocyclic compounds 4-amino benzoate (procaine) (A1), where the ester was synthesized by esterification of 4-amino benzoic acid with ethanol. Then, this compound was treated with potassium thiocyanate, followed by oxidative cyclization of the produced thiourea with bromine solution to afford ethyl-2-aminobenzothiazole-6-carboxylate (A2). The produced compound was further treated with some substituted benzaldehyde yielding the Schiff bases (A3a-d). Compound (A2) was also treated with acetic anhydride giving the corresponding N-(ethyl-2-amino benzo thiazolyl-6-carboxylate acetamide (A4). Compound (A4) was allowed to react with hydrazine hydrate afforded 2- benzothiazolyl-6- hydrazido acetamide (A5),which was then condensed with substituted aromatic aldehydes affording 6-[(arylidine hydrazino)-carbonyl]-2-acetamidobenzothiazole as a final product (A6a-d). All the synthesized compounds were characterized by the Infrared (FT-IR) technology. Some of the studied samples were checked by either their elemental analysis, (CHNS), 1H-NMR method, and biological evaluations antibacterial activities for some of the synthesized imides were evaluated against four types of bacteria and in addition to systematic identification of some actives functional groups in these compounds.

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Reference:
Thiazole | C3H10663NS – PubChem,
Thiazole | chemical compound | Britannica

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate, molecular formula is C10H10N2O2S. In a Patent,once mentioned of 50850-93-6, Application In Synthesis of Ethyl 2-aminobenzo[d]thiazole-6-carboxylate

The present invention provides a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis

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Reference:
Thiazole | C3H10641NS – PubChem,
Thiazole | chemical compound | Britannica

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Formula: C10H10N2O2S, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 50850-93-6, in my other articles.

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 50850-93-6, Name is Ethyl 2-aminobenzo[d]thiazole-6-carboxylate, molecular formula is C10H10N2O2S. In a Patent,once mentioned of 50850-93-6, Formula: C10H10N2O2S

no abstract published

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Formula: C10H10N2O2S, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 50850-93-6, in my other articles.

Reference:
Thiazole | C3H10659NS – PubChem,
Thiazole | chemical compound | Britannica

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 50850-93-6, C10H10N2O2S. A document type is Patent, introducing its new discovery., Quality Control of: Ethyl 2-aminobenzo[d]thiazole-6-carboxylate

Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.

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Reference:
Thiazole | C3H10656NS – PubChem,
Thiazole | chemical compound | Britannica

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.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, COA of Formula: C10H10N2O2S

Two series of analogues of riluzole, a blocker of excitatory amino acid mediated neurotransmission, have been synthesized: monosubstituted 2- benzothiazolamines and 3-substituted derivatives. Of all the compounds prepared in the first series, only 2-benzothiazolamines bearing alkyl, polyfluoroalkyl, or polyfluoroalkoxy substituents in the 6-position showed potent anticonvulsant activity against administration of glutamic acid in rats. The most active compounds displaying in vivo ‘antiglutamate’ activity were the 6-OCF3 (riluzole), 6-OCF2CF3, 6-CF3, and 6-CF2CF3 substituted derivatives with ED50 values between 2.5 and 3.2 mg/kg i.p. Among the second series of variously substituted benzothiazolines, compounds as active as riluzole or up to 3 times more potent were identified in two series: benzothiazolines bearing a beta-dialkylaminoethyl moiety and compounds with an alkylthioalkyl chain and their corresponding sulfoxides and sulfones. The most potent derivatives were 2-imino-3-(2-methylthio)- and 2-imino-3-(2- methylsulfinyl)-ethyl-6-trifluoromethoxybenzothiazolines (61 and 64, ED50 = 1.0 and 1.1 mg/kg i.p., respectively). In addition, intraperitoneal administration of some of the best benzothiazolines protected mice from mortality produced by hypobaric hypoxia.

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Reference:
Thiazole | C3H10628NS – PubChem,
Thiazole | chemical compound | Britannica

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Novel methotrexate (MTX) derivatives bearing dihydro-2H-1,4- benzothiazine or dihydro-2H-1,4-benzoxazine were synthesized and tested for in vitro antiproliferative activities against human synovial cells (hSC) and human peripheral blood mononuclear cells (hPBMC) obtained from patients with rheumatoid arthritis and healthy volunteers, respectively. In vivo antiarthritic activities of these derivatives were also evaluated in a rat adjuvant arthritis model. N-[[4-[(2,4-Diaminopteridin-6-yl)methyl]-3,4- dihydro-2H-1,4-benzothiazin-7-yl]carbonyl]-L-glutamic acid (3c) exhibited more potent antiproliferative activities in hSC and hPBMC than MTX in vitro. Antiproliferative activities of N-[[4-[(2,4-diaminopteridin-6-yl)methyl]- 3,4-dihydro-2H-1,4-benzoxazin-7-yl]carbonyl]-L-homoglutamic acid (3b) and N- [[4-[(2,4-diaminopteridin-6-yl)methyl]-3,4-dihydro-2H-1,4-benzothiazin-7- yl]carbonyl]-L-homoglutamic acid (3d) (MX-68) were comparable to that of MTX in these in vitro assays. Compounds 3b,d (MX-68) significantly suppressed progression of the adjuvant arthritis in a dose-dependent manner ranging from 0.5 to 2.5 mg/kg (po). In addition, 3d (MX-68) completely suppressed this progression at the dose of 2.5 mg/kg (po). Importantly, 3d (MX-68) having benzothiazine and homoglutamate, as expected, did not undergo polyglutamation, a process which may be responsible for the associated side effects of MTX. These results suggest that 3d (MX-68) is a potent and safe candidate antirheumatic agent, absent of the side effects of MTX.

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Reference:
Thiazole | C3H10658NS – PubChem,
Thiazole | chemical compound | Britannica

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Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38alpha MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by the replacement of the central oxazole or imidazole ring with an aminopyrazole system. The proposed binding mode of this new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies of a representative inhibitor (6a) bound to the p38alpha enzyme.

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Thiazole | C3H10654NS – PubChem,
Thiazole | chemical compound | Britannica

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By using ambient air as the oxidant and malic acid as the promoter, a practical method for the preparation of 2-aminobenzothiazoles through visible-light-initiated cascade reaction of aromatic amines and KSCN in eco-friendly bis(methoxypropy)ether under metal-, hazardous additive-, photocatalyst-free conditions was established.

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Reference£º
Thiazole | C3H10671NS – PubChem,
Thiazole | chemical compound | Britannica