Synthesis, molecular docking and enzyme inhibitory approaches of some new chalcone-engrafted pyrazoles as potential antialzheimer, antidiabetic and antioxidant agents was written by Islam, Mohammad Shahidul;Al-Majid, Abdullah Mohammed;Sholkamy, Essam Nageh;Yousuf, Sammer;Ayaz, Muhammad;Nawaz, Asif;Wadood, Abdul;Rehman, Ashfaq Ur;Verma, Ved Prakash;Bari, Ahmed;Haukka, Matti;Soliman, Saied M.;Barakat, Assem. And the article was included in Journal of Molecular Structure in 2022.SDS of cas: 827-01-0 This article mentions the following:
A series of pyrazole-based chalcones I (R = Ph, 3-MeC6H4, 2-benzothienyl, 3-indolyl, 5-chloro-3-methyl-1-phenylpyrazol-4-yl, etc.) was designed and constructed in two steps from readily available acetylacetone, phenylhydrazine and DMF-DMA as starting materials. The synthesized chalcone analogs were screened for in vitro anti-acetylcholinesterase potential, antidiabetic potential against 伪-glucosidase and 伪-amylase, and antioxidant potentials against DPPH free radicals. The compounds I (R = ferrocenyl, Ph, 1-naphthyl, 3-BrC6H4, 3-O2NC6H4) showed strongest acetylcholine esterase inhibition (AChEI) with IC50 values of 5 卤 1.16渭g/mL, 8 卤 0.14渭g/mL, 8 卤 0.57渭g/mL, 10 卤 1.73渭g/mL and 10 卤 0.60渭g/mL, resp. The highest inhibition against 伪-glucosidase was demonstrated by compounds I (R = 4-ClC6H4, 3-O2NC6H4, 3-FC6H4, 4-MeOC6H4, 3-MeC6H4, Ph) with IC50 values of 4 卤 0.14, 6 卤 0.43, 8 卤 0.43, 10 卤 0.11, 11 卤 0.28 and 12 卤 0.57渭g/mL, resp., whereas, the compounds I (R = 5-bromo-3-indolyl, benzothiophen-2-yl, 1-methyl-3-indolyl, 5-chloro-3-indolyl, 5-chloro-3-methyl-1-phenylpyrazol-4-yl) showed prominent 伪-amylase inhibition with IC50 values of 20 卤 1.15渭g/mL, 30 卤 0.60渭g/mL, 40 卤 0.72渭g/mL, 40 卤 0.50渭g/mL, and 60 卤 2.19渭g/mL, resp.. The highest anti-oxidant potential against DPPH free radicals was demonstrated by compounds I (R = 1-methyl-3-indolyl, 3-indolyl, 5-chloro-3-indolyl) with IC50 values of 160 卤 5.77, 260 卤 4.63, and 360 卤 4.04渭g/mL, resp. Mol. docking was used to study their interaction with the active site of enzymes. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0SDS of cas: 827-01-0).
5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). SDS of cas: 827-01-0
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Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles