Sep 2021 News Brief introduction of Ethyl 2-(2-aminothiazol-4-yl)acetate

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[A] of the dihydrofolate reductase inhibitory activity has the effect, due to the choice of therapeutic drug resistant bacteria and fungal infections can extend the width of a new compound, or a salt thereof, and the novel compound, or a salt thereof containing an antibacterial agent, more effective dihydrofolate reductase inhibitors there. (I) represented by the following formula [a], a compound having a 2, 4 – Diaminopyrimidine, or a salt thereof, said compound, or a salt thereof as an active ingredient of antibacterial agents. [1 A][Drawing] no (by machine translation)

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Reference:
Thiazole | C3H10845NS – PubChem,
Thiazole | chemical compound | Britannica

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Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: STR1 in which R1, R4 and R5 ae various organic radicals, R2 is alkoxycarbonyl, Y is Cl, Br or –O–SO2 –R5, and X is a conventional cephalosporin substituent. Many of the intermediates are new, especially in pure Z-form.

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Reference:
Thiazole | C3H10773NS – PubChem,
Thiazole | chemical compound | Britannica

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C18H21ClN2O3S, monoclinic, P21/c, a = 12.582(4) A, b = 14.790(5) A, c = 21.406(8) A, beta = 92.572(13), V = 3979(2) A3, Z = 8, Rgt(F) = 0.0464, wRref(F2) = 0.1298, T = 298(2) K.

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Reference:
Thiazole | C3H10800NS – PubChem,
Thiazole | chemical compound | Britannica

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Dual-target-directed agents simultaneously inhibiting glycogen phosphorylase (GP) and activating glucokinase (GK) could decelerate the inflow of glucose from glycogenolysis and accelerate the outflow of glucose in the liver, therefore allow for a better control over hyperglycaemia in a synergetic manner. A series of hybrid compounds were designed by structure-assisted and ligand-based strategies. In vitro bioassays found two novel compounds (1j, 6g) worthy of further optimization on balance of dual action to GP and GK. In addition, for single-target activity, two compounds exhibited more potent GP inhibitory activity and four compounds showed better GK activation than their corresponding references.

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Reference:
Thiazole | C3H10777NS – PubChem,
Thiazole | chemical compound | Britannica

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A thiazole-based novel dipeptide module has been synthesized, which exhibited selective Cu(II) recognition in water in the presence of other competing divalent transition metal ions at micromolar concentrations. This is the first example of an entirely synthetic peptide based chemosensor for Cu(II). (C) 2000 Elsevier Science Ltd.

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Reference:
Thiazole | C3H10814NS – PubChem,
Thiazole | chemical compound | Britannica

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The conformations and hydrogen bonding in the thiophene and thiazole title compounds, [Fe(C5H5)(C20H14NO 3S)], (I), and [Fe(C5H5)(C19H 17N2O3S)], (II), are discussed. The sequence (C5H4)-(C6H4)-(CONH)-(C 4H2S)-(CO2Me) of rings and moieties in (I) is close to being planar; all consecutive interplanar angles are less than 10. An intramolecular N-H…O=Cester hydrogen bond [graph set S(6), N…O = 2.768 (2) A and N – H…O = 134 (2)] effects the molecular planarity, and aggregation occurs via hydrogen-bonded chains formed from intermolecular Car – H…O=Cester/amide interactions along [010], with C…O distances ranging from 3.401 (3) to 3.577 (2) A. The thiazole system in (II) crystallizes with two molecules in the asymmetric unit; these differ in the conformation along their long molecular axes; for example, the interplanar angle between the phenylene (C 6H4) and thiazole (C3NS) rings is 8.1 (2) in one molecule and 27.66 (14) in the other. Intermolecular N-H…O=Cester hydrogen bonds [N…O = 2.972 (4) and 2.971 (3) A], each augmented by a Cphenylene – H…O=C ester interaction [3.184 (5) and 3.395 (4) A], form motifs with graph set R21(7) and generate chains along [100]. The amide C=O groups do not participate in hydrogen bonding. Compound (II) is the first reported ferrocenyl-containing thiazole structure.

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Reference:
Thiazole | C3H10736NS – PubChem,
Thiazole | chemical compound | Britannica

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Mirabegron is a muscle relaxing drug for the treatment of overactive bladder. The existing synthetic methods for mirabegron produced intermediate product 4-(2-(phenethylamino)ethyl)aniline, which complicated the final product purification process. In this study, we designed a new synthetic route for mirabegron with low cost starting materials and a production of mirabegron at a 99.6% purity and a 61% overall yield. Particularly, this new synthetic route did not produce side product 4-(2-(phenethylamino)ethyl)aniline, which significantly simplified the product purification process.

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Reference:
Thiazole | C3H10758NS – PubChem,
Thiazole | chemical compound | Britannica

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Four series of ferulic acid derivatives were designed, synthesized, and evaluated for their neuraminidase (NA) inhibitory activities against influenza virus H1N1 in vitro. The pharmacological results showed that the majority of the target compounds exhibited moderate influenza NA inhibitory activity, which was also better than that of ferulic acid. The two most potent compounds were 1m and 4a with IC50 values of 12.77 ± 0.47 and 12.96 ± 1.34 mug/ml, respectively. On the basis of the biological results, a preliminary structure?activity relationship (SAR) was derived and discussed. Besides, molecular docking was performed to study the possible interactions of compounds 1p, 2d, 3b, and 4a with the active site of NA. It was found that the 4-OH-3-OMe group and the amide group (CON) of ferulic acid amide derivatives were two key pharmacophores for NA inhibitory activity. It is meaningful to further modify the natural product ferulic acid to improve its influenza NA inhibitory activity.

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Reference:
Thiazole | C3H10776NS – PubChem,
Thiazole | chemical compound | Britannica

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The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

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Reference:
Thiazole | C3H10711NS – PubChem,
Thiazole | chemical compound | Britannica

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The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.

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Reference:
Thiazole | C3H10727NS – PubChem,
Thiazole | chemical compound | Britannica