Formula: C8H8O2. In 2019.0 BIOORG CHEM published article about ALZHEIMERS-DISEASE; DONEPEZIL; TACRINE; HYBRIDS; DESIGN; E2020 in [Kuzu, Burak; Tan, Meltem; Menges, Nurettin] Van Yuzuncu Yil Univ, Pharmaceut Chem Sect, TR-65080 Van, Turkey; [Kuzu, Burak; Tan, Meltem; Menges, Nurettin] YYU TEKNOKENT, SAFF Chem Reagent R&D Lab, TR-65080 Van, Turkey; [Taslimi, Parham; Gulcin, Ilhami] Ataturk Univ, Dept Chem, TR-25240 Erzurum, Turkey; [Taspinar, Mehmet] Van Yuzuncu Yil Univ, Dept Med Biol, TR-65080 Van, Turkey in 2019.0, Cited 32.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.
Mono- or di-substituted imidazole derivatives were synthesized using a one-pot, two-step strategy. All imidazole derivatives were tested for AChE and BChE inhibition and showed nanomolar activity similar to that of the test compound donepezil and higher than that of tacrine. Structure activity relationship studies, docking studies to on X-ray crystal structure of AChE with PDB code 1B41, and adsorption, distribution, metabolism, and excretion (ADME) predictions were performed. The synthesized core skeleton was bound to important regions of the active site of AChE such as the peripheral anionic site (PAS), oxyanion hole (OH), and anionic subsite (AS). Selectivity of the reported test compounds was calculated and enzyme kinetic studies revealed that they behave as competitive inhibitors, while two of the test compounds showed noncompetitive inhibitory behavior. ADME predictions revealed that the synthesized molecules might pass through the blood brain barrier and intestinal epithelial barrier and circulate freely in the blood stream without binding to human serum albumin. While the toxicity of one compound on the WS1 (skin fibroblast) cell line was 1790 mu M, its toxicity on the SH-SY5Y (neuroblastoma) cell line was 950 mu M.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles