Category: 70060-13-8

N-(4-(4-(2,3-Dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with Functionalized Linking Chains as High Affinity and Enantioselective D3 Receptor Antagonists was written by Newman, Amy Hauck;Grundt, Peter;Cyriac, George;Deschamps, Jeffrey R.;Taylor, Michelle;Kumar, Rakesh;Ho, David;Luedtke, Robert R.. And the article was included in Journal of Medicinal Chemistry in 2009.Application of 70060-13-8 This article mentions the following:

In the present report, the D3 receptor pharmacophore is modified in the 2,3-diCl- and 2-OCH₃-phenylpiperazine class of compounds with the goal to improve D3 receptor affinity and selectivity. This extension of structure-activity relationships (SAR) has resulted in the identification of the first enantioselective D3 antagonists (R- and S-22) to be reported, wherein enantioselectivity is more pronounced at D3 than at D2, and that a binding region on the second extracellular loop (E2) may play a role in both enantioselectivity and D3 receptor selectivity. Moreover, we have discovered some of the most D3-selective compounds reported to date that show high affinity (K_i = 1 nM) for D3 and ∼400-fold selectivity over the D2 receptor subtype. Several of these analogs showed exquisite selectivity for D3 receptors over >60 other receptors, further underscoring their value as in vivo research tools. These lead compounds also have appropriate phys. characteristics for in vivo exploration and therefore will be useful in determining how intrinsic activity at D3 receptors tested in vitro is related to behaviors in animal models of addiction and other neuropsychiatric disorders. In the experiment, the researchers used many compounds, for example, 5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8Application of 70060-13-8).

5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8) belongs to benzothiophene derivatives. Functionalized benzothiophenes are important constructs found in molecules with wide ranging biological activity and in organic materials. It is found within the chemical structures of pharmaceutical drugs such as raloxifene, zileuton, and sertaconazole, and also BTCP.Application of 70060-13-8

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Potential hypolipidemic agents. XX. Synthesis and lipid-lowering properties of annelated thiophenecarboxylic acids was written by Gronowitz, Salo;Herslof, Margareta;Svenson, Rolf;Bondesson, Goran;Magnusson, Olle;Stjernstrom, Nils E.. And the article was included in Acta Pharmaceutica Suecica in 1978.Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid This article mentions the following:

Condensed thiophenecarboxylic acids I–V (R = H, Cl, F; R¹ = H, Cl; R² = H, Cl, F, Me, R³ = H; R² = H, R³ = Cl) were prepared The V had anticholesteremic and hypolipemic activity superior that of clofibrate, whereas IV was inactive. Chlorination increased the hypolipemic activity of I through III. In the experiment, the researchers used many compounds, for example, 5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid).

5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8) belongs to benzothiophene derivatives. Benzothiophenes are valuable heterocycles that are widely used in medicines, agrochemicals, and materials science. It is found within the chemical structures of pharmaceutical drugs such as zileuton, raloxifene, and sertaconazole, and also BTCP.Quality Control of 5-Fluoro-1-benzothiophene-2-carboxylic acid

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents was written by Zhao, Liyu;Sun, Yin;Yin, Wenbo;Tian, Linfeng;Sun, Nannan;Zheng, Yang;Zhang, Chu;Zhao, Shizhen;Su, Xin;Zhao, Dongmei;Cheng, Maosheng. And the article was included in European Journal of Medicinal Chemistry in 2022.Synthetic Route of C9H5FO2S This article mentions the following:

To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives were designed and synthesized. Compounds I [R¹ = 6-F, 6-Cl, 6-Br; R² = 4-F] and [R¹ = 6-Cl, 6-Br; R² = 4-Cl] exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03-0.5μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25-2μg/mL. In addition, compounds I [R¹ = 6-Cl; R² = 4-F] and [R¹ = 6-Cl; R² = 4-Cl] showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, resp. Moreover, compounds I [R¹ = 6-Cl; R² = 4-F] and [R¹ = 6-Cl; R² = 4-Cl] showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compoundI [R¹ = 6-Cl; R² = 4-F] had suitable pharmacokinetic properties and was worthy of further study. In the experiment, the researchers used many compounds, for example, 5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8Synthetic Route of C9H5FO2S).

5-Fluoro-1-benzothiophene-2-carboxylic acid (cas: 70060-13-8) belongs to benzothiophene derivatives. Benzothiophene finds use in research as a starting material for the synthesis of larger, usually bioactive structures. It is also used in the manufacturing of dyes such as thioindigo.Synthetic Route of C9H5FO2S

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem