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3-羟基和3-甲氧基-2-苯乙烯基色酮的抗鼻病毒活性的合成与评价

Synthesis and evaluation of antirhinovirus activity of 3-hydroxy and 3-methoxy 2-styrylchromones.

作者信息

Desideri Nicoletta, Mastromarino Paola, Conti Cinzia

机构信息

Dipartimento di Studi Farmaceutici, Università La Sapienza di Roma, Rome, Italy.

出版信息

Antivir Chem Chemother. 2003 Jul;14(4):195-203. doi: 10.1177/095632020301400404.

Abstract

Recently, we identified 2-styrylchromones as a new class of antirhinovirus flavonoids with moderate activity against both rhinovirus groups A and B. In order to improve the antiviral effect of the first series of tested 2-styrylchromones, a hydroxy or methoxy group was introduced in position 3 of the chromone ring. Cytotoxicity and antiviral activity of the new synthesized compounds were evaluated in HeLa cell cultures infected with rhinoviruses 1B and 14, selected as representative serotypes for viral groups B and A of human rhinoviruses (HRVs), respectively. These antiviral results compared to those obtained for 3-unsubstituted 2-styrylchromones indicate the greater potency of 3-hydroxy and 3-methoxy derivatives against both serotypes.

摘要

最近,我们鉴定出2-苯乙烯基色酮是一类新型抗鼻病毒类黄酮,对A组和B组鼻病毒均具有中等活性。为了提高首批测试的2-苯乙烯基色酮的抗病毒效果,在色酮环的3位引入了羟基或甲氧基。在感染鼻病毒1B和14的HeLa细胞培养物中评估了新合成化合物的细胞毒性和抗病毒活性,这两种病毒分别被选为人鼻病毒(HRV)B组和A组的代表性血清型。与3-未取代的2-苯乙烯基色酮所获得的抗病毒结果相比,这些结果表明3-羟基和3-甲氧基衍生物对两种血清型均具有更强的效力。

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