文献类型：期刊文献

英文题名：Pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety as potential antiviral agents

作者：Wang Y.-Y. Xu F.-Z. Zhu Y.-Y. Song B. Luo D. Yu G. Chen S. Xue W. Wu J.

机构：[1]State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang, 550025, China;[2]School of Chemical Engineering, Guizhou Institute of Technology, Guiyang, 550001, China

第一机构：State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang, 550025, China

通信机构：State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang, 550025, China

年份：2018

卷号：28

期号：17

起止页码：2979-2984

外文期刊名：Bioorganic and Medicinal Chemistry Letters

收录：Scopus(收录号：2-s2.0-85049465355)

语种：英文

外文关键词：AMTNEOOXRXWRCM-YAXRCOADSA-N; Antiviral activity; AWRYWUXZPWEGMZ-REZTVBANSA-N; BPOQQDJRWDOIEB-UHFFFAOYSA-N; CBJAOOXXTPSOLT-VIZOYTHASA-N; FAWORDBUPCDJHF-VIZOYTHASA-N; HFJRRPIHLFGLBQ-UBKPWBPPSA-N; HWQWEWGQLIQLOZ-REZTVBANSA-N; IAJUSFPXNMPMFP-SYZQJQIISA-N; JENMSLPZSGMTJB-REZTVBANSA-N; JKKQWVVDGMTXPR-OMCISZLKSA-N; KLRPLYVCPQRLRB-PJQLUOCWSA-N; KRUDYPVNOBPVEA-UBKPWBPPSA-N; MAONEPGLKKOQLN-MKMNVTDBSA-N; Molecular docking; NMBRCUQFFSCKOJ-FRKPEAEDSA-N; NVBQIDGJIOLBFT-GIDUJCDVSA-N; OLKSNIVQMRCSJZ-UBKPWBPPSA-N; OMCOLYYBELREHP-LHHJGKSTSA-N; OQRMFCDBRZMINH-MKMNVTDBSA-N; ORFLBOXAUYGODB-GIDUJCDVSA-N; PJPULIXXEOCLQG-OMCISZLKSA-N; PMZCIEIUZYAOGL-UHFFFAOYSA-N; PWWLLXGBICCGEI-FZSIALSZSA-N; Pyrazolo[3,4-d]pyrimidine; QAMUGIJEYLOARY-LZYBPNLTSA-N; QDVKGTBCFZTXDG-FRKPEAEDSA-N; QRKJTDALEQWBTK-VGOFMYFVSA-N; RDJSZXARXGALQP-REZTVBANSA-N; RNUASPIEZKHLLA-LHHJGKSTSA-N; RNYZJFGNVRJBRF-FRKPEAEDSA-N; RWHKMCAUWHIOCS-WUXMJOGZSA-N; RWWXQODYOPFBQM-GIDUJCDVSA-N; RZOLJYUWCDHIGH-OMCISZLKSA-N; Schiff base; TVKDNILWGVYQAU-UHFFFAOYSA-N; VXTJXLMBWKNDLK-VIZOYTHASA-N; WCIAWDONFWQAGP-UHFFFAOYSA-N; XAKGEQLFVUBVML-WUXMJOGZSA-N; XNVSNJUMLJWFMO-OMCISZLKSA-N; XTTVXBKEJVEKBS-MKMNVTDBSA-N; ZVADRITWHMRBQP-CXUHLZMHSA-N

摘要：A series of pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base moiety were synthesized, characterised, and evaluated for their activity against tobacco mosaic virus (TMV). Biological assays indicated that several of the derivatives exhibited significant activity against TMV. In particularly, compounds 5y and 5aa displayed excellent inactivating activity against TMV, with half maximal effective concentration (EC50) values of 70.3 and 53.65 μg/mL, respectively, which were much better than that of ribavirin (150.45 μg/mL), and 5aa was superior to ningnanmycin (EC50 = 55.35 μg/mL). Interactions of compounds 5y and 5aa with TMV coat protein (TMV-CP) were investigated using microscale thermophoresis and molecular docking. Compounds 5y and 5aa displayed strong binding capability to TMV-CP with dissociation constant (Kd) values of 22.6 and 9.8 μM, respectively. These findings indicate that pyrazolo[3,4-d]pyrimidine derivatives containing a Schiff base may be potential antiviral agents. ? 2018 Elsevier Ltd