Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: Synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis was written by Khan, Imtiaz;Ibrar, Aliya;Zaib, Sumera;Ahmad, Sarfraz;Furtmann, Norbert;Hameed, Shahid;Simpson, Jim;Bajorath, Jurgen;Iqbal, Jamshed. And the article was included in Bioorganic & Medicinal Chemistry in 2014.Product Details of 1877-75-4 This article mentions the following:
In an effort to identify novel cholinesterase candidates for the treatment of Alzheimer’s disease (AD), a diverse array of potentially bioactive compounds including triazolothiadiazoles and triazolothiadiazines was obtained in good yields through the cyclocondensation reaction of 4-amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol with various substituted aryl/heteroaryl/aryloxy acids and phenacyl bromides, resp. The structures of the newly prepared compounds were confirmed by IR, 1H and 13C NMR spectroscopy and, in case of 4a, by single crystal X-ray diffraction anal. The purity of the synthesized compounds was ascertained by elemental anal. The newly synthesized conjugated heterocycles were screened for cholinesterase inhibitory activity against elec. eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinesterase (hBChE). Among the evaluated hybrids, several compounds were identified as potent inhibitors. Two triazolothiadiazoles were most active with an IC50 value of 3.09 ± 0.154 and 11.3 ± 0.267 μM, resp., against acetylcholinesterase, whereas three compounds were most potent against butyrylcholinesterase, with an IC50 of 0.585 ± 0.154, 0.781 ± 0.213, and 1.09 ± 0.156 μM, resp., compared to neostigmine and donepezil as standard drugs. The synthesized heteroaromatic compounds were also tested for their cytotoxic potential against lung carcinoma (H157) and vero cell lines. One compound exhibited highest antiproliferative activity against H157 cell lines, with IC50 value of 0.96 ± 0.43 μM at 1 mM concentration as compared to vincristine (IC50 = 1.03 ± 0.04 μM), standard drug used in this study. In the experiment, the researchers used many compounds, for example, 2-(4-Methoxyphenoxy)acetic acid (cas: 1877-75-4Product Details of 1877-75-4).
2-(4-Methoxyphenoxy)acetic acid (cas: 1877-75-4) belongs to ethers. Of all the functional groups, ethers are the least reactive ones. Ether bonds are quite stable towards bases, oxidizing agents and reducing agents. Electron-deficient reagents are also stabilized by ethers. For example, borane (BH3) is a useful reagent for making alcohols. Pure borane exists as its dimer, diborane (B2H6), a toxic gas that is inconvenient and hazardous to use. Borane forms stable complexes with ethers, however, and it is often supplied and used as its liquid complex with tetrahydrofuran (THF).Product Details of 1877-75-4
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem