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Each analog was evaluated for its anti\u2010inflammatory ability via the suppression of nitric oxide (NO) on IFN\u2010\u03b3\/LPS\u2010activated RAW264.7 macrophage cells. The compounds were also investigated for their inhibitory capability toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), using a modification of Ellman's spectrophotometric method. The most potent NO inhibitor was found to be phenylpyrazole analog <jats:bold>4c<\/jats:bold>, followed by <jats:bold>4e<\/jats:bold>, when compared with curcumin. In contrast, pyrazole <jats:bold>3a<\/jats:bold> and pyrazoline <jats:bold>5a<\/jats:bold> were found to be the most selective and effective BChE inhibitors over AChE. The data collected from the single\u2010crystal X\u2010ray diffraction analysis of compound <jats:bold>5a<\/jats:bold> were then applied in a docking simulation to determine the potential binding interactions that were responsible for the anti\u2010BChE activity. The results obtained signify the potential of these pyrazole and pyrazoline scaffolds to be developed as therapeutic agents against inflammatory conditions and Alzheimer's disease.<\/jats:p>","DOI":"10.1002\/ardp.202000161","type":"journal-article","created":{"date-parts":[[2020,9,4]],"date-time":"2020-09-04T17:13:38Z","timestamp":1599239618000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["In silico studies, nitric oxide, and cholinesterases inhibition activities of pyrazole and pyrazoline analogs of diarylpentanoids"],"prefix":"10.1002","volume":"354","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8043-798X","authenticated-orcid":false,"given":"Siti Munirah","family":"Mohd Faudzi","sequence":"first","affiliation":[{"name":"Department of Chemistry, Faculty of Science Universiti Putra Malaysia  Serdang Selangor Malaysia"},{"name":"Laboratory of Natural Products, Institute of Bioscience Universiti Putra Malaysia  Serdang Selangor Malaysia"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0021-3092","authenticated-orcid":false,"given":"S. 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