Neuroprotective and Antioxidant Effects of Novel Benzofuran-2-Carboxamide Derivatives

Cho, Jungsook; Park, Chowee; Lee, Youngmun; Kim, Sunyoung; Bose, Shambhunath; Choi, Minho; Kumar, Arepalli Sateesh; Jung, Jae-Kyung; Lee, Heesoon

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자료유형: 학술저널

저자정보: Cho, Jungsook (College of Pharmacy, Dongguk University-Seoul) Park, Chowee (College of Pharmacy, Dongguk University-Seoul) Lee, Youngmun (College of Pharmacy, Dongguk University-Seoul) Kim, Sunyoung (College of Pharmacy, Dongguk University-Seoul) Bose, Shambhunath (College of Pharmacy, Dongguk University-Seoul) Choi, Minho (Collegy of Pharmacy, Chungbuk National University) Kumar, Arepalli Sateesh (Collegy of Pharmacy, Chungbuk National University) Jung, Jae-Kyung (Collegy of Pharmacy, Chungbuk National University) Lee, Heesoon (Collegy of Pharmacy, Chungbuk National University)

저널정보: 한국응용약물학회 Biomolecules & Therapeutics(구 응용약물학회지) Biomolecules & therapeutics 제23권 제3호

발행연도: 2015.1

수록면: 275 - 282 (8page)

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In the present study, we synthesized a series of novel 7-methoxy-N-(substituted phenyl)benzofuran-2-carboxamide derivatives in moderate to good yields and evaluated their neuroprotective and antioxidant activities using primary cultured rat cortical neuronal cells and in vitro cell-free bioassays. Based on our primary screening data with eighteen synthesized derivatives, nine compounds (1a, 1c, 1f, 1i, 1j, 1l, 1p, 1q and 1r) exhibiting considerable protection against the NMDA-induced excitotoxic neuronal cell damage at the concentration of $100{\mu}M$ were selected for further evaluation. Among the selected derivatives, compound 1f (with $-CH_3$ substitution at R2 position) exhibited the most potent and efficacious neuroprotective action against the NMDA-induced excitotoxicity. Its neuroprotective effect was almost comparable to that of memantine, a well-known NMDA antagonist, at $30{\mu}M$ concentration. In addition to 1f, compound 1j (with -OH substitution at R3 position) also showed marked anti-excitotoxic effects at both 100 and $300{\mu}M$ concentrations. These findings suggest that $-CH_3$ substitution at R2 position and, to a lesser degree, -OH substitution at R3 position may be important for exhibiting neuroprotective action against excitotoxic damage. Compound 1j was also found to scavenge 1,1-diphenyl-2-picrylhydrazyl radicals and inhibit in vitro lipid peroxidation in rat brain homogenate in moderate and appreciable degrees. Taken together, our structure-activity relationship studies suggest that the compound with $-CH_3$ substitution at R2 and -OH substitution at R3 positions of the benzofuran moiety might serve as the lead exhibiting potent anti-excitotoxic, ROS scavenging, and antioxidant activities. Further synthesis and evaluation will be necessary to confirm this possibility.

#Neuroprotection #Excitotoxicity #Reactive oxygen species #Antioxidant activity #Benzofuran-2-carboxamide derivatives

참고문헌 (25)

참고문헌 신청

Cho, J. / 2000 / Inhibition of excitotoxic neuronal death by methanol extract of Acori graminei rhizoma in cultured rat cortical neurons / J. Ethnopharmacol 73:31~37

Cho, J. / 2001 / NMDA recepter-mediated neuroprotection by essential oils from the rhizomes of Acorus gramineus / Life Sci 68:1567~1573

Cho, J. / 2004 / Wogonin inhibits excitotoxic and oxidative neuronal damage in primary cultured rat cortical cells / Eur. J. Pharmacol 485:105~110

Cho, J. / 2005 / Neuroprotective and antioxidant effects of the ethyl acetate fraction prepared from Tussilago farfara L / Biol. Pharm. Bull 28:455~460

Choi, D. W. / 1992 / Excitotoxic cell death / J. Neurobiol 23:1261~1276

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