Tyrosine and glycine derivatives as potential prodrugs: design, synthesis, and pharmacological evaluation of amide derivatives of mefenamic acid

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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New chalcones and thiopyrimidine analogues derived from mefenamic acid: microwave-assisted synthesis, anti-HIV activity and cytotoxicity as antileukemic agents

Zeitschrift für Naturforschung B ◽

10.1515/znb-2016-0223 ◽

2017 ◽

Vol 72 (4) ◽

pp. 249-256 ◽

Cited By ~ 2

Author(s):

Hanan A. Al-Hazam ◽

Zeki A. Al-Shamkani ◽

Najim A. Al-Masoudi ◽

Bahjat A. Saeed ◽

Christophe Pannecouque

Keyword(s):

Mefenamic Acid ◽

Leukemia Cells ◽

Basic Medium ◽

Microwave Assisted Synthesis ◽

Schmidt Reaction ◽

Microwave Assisted ◽

Amide Derivatives ◽

Derivatives Of ◽

Anti Hiv ◽

Hiv 1

AbstractThe development of new HIV non-nucleoside reverse transcriptase inhibitors offers the possibility of generating structures of increased potency. To this end, coupling of mefenamic acid (4) with 4-amino-acetophenone (6) in the presence of dicyclohexylcarbodiimide and dimethylaminopyridine (DMAP) reagents afforded 4-(acetyphenyl)-2-((2,3-dimethylphenyl)amino)benzamide (7). Analogously, treatment of mefenamyl chloride (5) prepared from 4 with 6 under microwave irradiation (MWI) afforded 7. A new series of substituted chalconyl-incorporated amide derivatives of mefenamic acid 8–13 were synthesized from condensation of 7 with various substituted benzaldehydes via the Claisen–Schmidt reaction. Treatment of 8 and 11 with thiourea in a basic medium afforded the thiopyrimidine analogues 14 and 15, respectively. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 11 showed cytotoxicity values of 2.17 and 2.06 μm, respectively, against mock-infected MT-4 cells (C type adult T leukemia cells), which considered to be promising antileukemic agents.

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