Design, synthesis, structure-activity relationship and mechanism of action studies of a series of 4-chloro-1-phthalazinyl hydrazones as a potent agent against Leishmania braziliensis

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• 作者：Angel H. Romero^a ; ^{angel.romero12@ucv.ve} ; Rafael Medina^b ; Anamarí ; a Alcala^c ; Yael Garcí ; a-Marchan^c ; Jorge Nú ; &ntilde ; ez-Duran^c ; Jacques Lea&ntilde ; ez^c ; Ali Mijoba^c ; Carlos Ciangherotti^d ; Xenó ; n Serrano-Martí ; n^c ; Simó ; n E. Ló ; pez^a ; ^{slopez@usb.ve}
• 关键词：Leishmania braziliensis ; Antileishmanial activity ; Superoxide dismutase ; Promastigotes ; Phthalazine ; Nitroheterocycle
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：606-620
• 全文大小：1346 K
• 卷排序：127

文摘

New phthalazine analogues were designed, synthesized and evaluated against L. braziliensis. Nitroheterocyclic moiety plays an important role in the antileishmanial activity of these phthalazines. The compound 3l exhibited a significant antileishmanial response, without affecting viability of the macrophage cells. The SOD and DHFR inhibition assays and oxidative stress experiments were also conducted.