On September 30, 2020, Szczukowski, Lukasz; Redzicka, Aleksandra; Wiatrak, Benita; Krzyzak, Edward; Marciniak, Aleksandra; Gebczak, Katarzyna; Gebarowski, Tomasz; Swiatek, Piotr published an article.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Design, synthesis, biological evaluation and in silico studies of novel pyrrolo[3,4-d]pyridazinone derivatives with promising anti-inflammatory and antioxidant activity. And the article contained the following:
Novel Mannich base analogs of pyrrolo[3,4-d]pyridazinone I (R1 = n-Bu, Ph; X = N, O, C; R2 = Ph, 4-MeC6H4, 2-pyridyl, etc.; R3 = OH) are designed and synthesized as potential anti-inflammatory agents. The title compounds are obtained via convenient one-pot synthesis with good yields. The aim of this study is to evaluate the inhibitory activity of the new derivatives against both cyclooxygenase isoforms COX1 and COX2 as well as their cytotoxicity. The results clearly indicate that the tested compounds are not toxic, all show better affinity towards isoform COX-2, and some of them act as selective COX-2 inhibitors. Moreover, every examined compounds I demonstrates better inhibitory activity towards COX-2 and a superior COX-2/COX-1 selectivity ratio compared to the reference drug meloxicam. Mol. docking studies confirm that all compounds preferably bind COX-2 and all of them bind to the active site of cyclooxygenase in a way very similar to meloxicam. Subsequently, synthesized Mannich bases are evaluated for potential antioxidant activity. Most of the investigated derivatives reduce induced oxidative and nitrosative stress. Moreover, some compounds protect chromatin from oxidative stress and decrease the number of DNA strand breaks caused by intracellular growth of free radicals. Finally, a study of the binding mechanism between compounds I and bovine serum albumin (BSA) was carried out and all examined derivatives interact with BSA, which suggests their potential long half-life in vivo. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol
The Article related to pyrrolopyridazinone preparation antiinflammatory antioxidant drug toxicity mol docking sar, 1,3,4-oxadiazole-2-thione, anti-inflammatory agents, antioxidants, cyclooxygenase inhibitors, mannich bases, molecular docking, pyridazinone and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem