Research Paper on Based on a 1,3-Disubstituted 1H-yrazolo[3,4-d], Zika Virus Inhibitors Scaffold for pyrimidine-amines

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Title: Based on a 1,3-Disubstituted 1H-yrazolo[3,4-d], Zika Virus Inhibitors Scaffold for pyrimidine-amines

Abstract: By investigating a different substitution pattern of their central scaffold, we further investigated the previously reported 7H-pyrrolo[2,3-d]pyrimidines and discovered compound 5 with low micromolar antiviral activity. We have utilized a 1H-pyrazolo[3,4-d]pyrimidine scaffold and conducted structure-activity relationship studies on its periphery rings A and B in order to get around the difficulties in synthesizing compound 5 in the first place. For improved antiviral activity, an electron-withdrawing group is preferred at the para position of ring A even though ring B is less susceptible to structural changes. Overall, we have generated anti-ZIKV compounds like 6 and 13, which have low micromolar antiviral activity and relatively low cytotoxicity, in addition to discovering an alternative substitution pattern centered on a 1H-pyrazolo[3,4-d]pyrimidine scaffold. These substances represent novel chemotypes that will be improved further in our ongoing search for anti-ZIKV agents.

Keywords: Zika virus; flavivirus; antiviral agents; Zika virus inhibitors

Paper Quality: SCOPUS / Web of Science Level Research Paper

Subject: Chemistry

Writer Experience: 20+ Years

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