The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT7 receptor antagonists

Abstract A unique series of amide-scutellarin derivatives were designed and synthesized in order to develop the function of scutellarin further. The antiproliferative activity of all target compounds against two human leukaemia cell lines were evaluated. Among them, compounds 6g and 7c displayed the most antitumor activities against HL-60 and THP-1. Moreover, all compounds were also assayed for their neuroprotective activity against hydrogen peroxide (H2O2)-induced PC-12 cell injury, and the majority of the compounds had moderate to good neuroprotective properties. These findings confirmed that these target compounds could be used as anti-leukaemia and neuroprotective candicates in the future.

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Amide derivatives of Gallic acid: Design, synthesis and evaluation of inhibitory activities against in vitro α-synuclein aggregation

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2020.115596 ◽

2020 ◽

Vol 28 (15) ◽

pp. 115596

Author(s):

Li Chen ◽

Guo-Long Huang ◽

Ming-Huan Lü ◽

Yun-Xiao Zhang ◽

Ji Xu ◽

...

Keyword(s):

Gallic Acid ◽

Design Synthesis ◽

Amide Derivatives ◽

Inhibitory Activities ◽

Derivatives Of

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Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2004.01.033 ◽

2004 ◽

Vol 14 (7) ◽

pp. 1791-1794 ◽

Cited By ~ 3

Author(s):

Anandan Palani ◽

Sundeep Dugar ◽

John W. Clader ◽

William J. Greenlee ◽

Vilma Ruperto ◽

...

Keyword(s):

Receptor Antagonists ◽

Amide Derivatives ◽

Derivatives Of

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Design, synthesis, and biological evaluation of amide derivatives of imidazo[2,1-b][1,3,4]thiadiazole as anticancer agents

Synthetic Communications ◽

10.1080/00397911.2020.1797814 ◽

2020 ◽

Vol 50 (21) ◽

pp. 3221-3233

Author(s):

Gattu Sridhar ◽

Sadanandam Palle ◽

Jyothi Vantikommu ◽

Kiran Gangarapu

Keyword(s):

Anticancer Agents ◽

Biological Evaluation ◽

Design Synthesis ◽

Amide Derivatives ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

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A new class of 5-HT1A receptor antagonists with procognitive and antidepressant properties

Future Medicinal Chemistry ◽

10.4155/fmc-2020-0363 ◽

2021 ◽

Author(s):

Agnieszka Jankowska ◽

Grzegorz Satała ◽

Artur Świerczek ◽

Krzysztof Pociecha ◽

Anna Partyka ◽

...

Keyword(s):

Antidepressant Drugs ◽

Antidepressant Activity ◽

Functional Profile ◽

Receptor Antagonists ◽

Receptor Affinity ◽

New Class ◽

Amide Derivatives ◽

Derivatives Of

Aims: 5-HT1A receptor antagonists constitute a potential group of drugs in the treatment of CNS diseases. The aim of this study was to search for new procognitive and antidepressant drugs among amide derivatives of aminoalkanoic acids with 5-HT1A receptor antagonistic properties. Materials & methods: Thirty-three amides were designed and evaluated in silico for their drug-likeness. The synthesized compounds were tested in vitro for their 5-HT1A receptor affinity and functional profile. Moreover, their selectivity over 5-HT7, 5-HT2A and D2 receptors and ability to inhibit phosphodiesterases were evaluated. Results: A selected 5-HT1A receptor antagonist 20 ( Ki = 35 nM, Kb = 4.9 nM) showed procognitive and antidepressant activity in vivo. Conclusion: Novel 5-HT1A receptor antagonists were discovered and shown as potential psychotropic drugs.

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