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Synthesis and SAR studies of praziquantel derivatives with activity against Schistosoma japonicum. 2013

Wen-Long Wang, and Li-Jun Song, and Xia Chen, and Xu-Ren Yin, and Wen-Hua Fan, and Gu-Ping Wang, and Chuan-Xin Yu, and Bainian Feng
School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China.

The synthesis and structure-activity relationship (SAR) studies of praziquantel derivatives with activity against adult Schistosoma japonicum are described. Several of them showed better worm killing activity than praziquantel and could serve as leads for further optimization.

UI MeSH Term Description Entries
D011223 Praziquantel An anthelmintic used in most schistosome and many cestode infestations. Biltricide,Cesol,Cisticid,Cysticide,Droncit,Drontsit,EMBAY 8440,Prasiquantel,Praziquantel, (+-)-Isomer,Praziquantel, (R)-Isomer,Praziquantel, (S)-Isomer,Pyquiton,Traziquantel
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012549 Schistosoma japonicum A species of trematode blood flukes belonging to the family Schistosomatidae whose distribution is confined to areas of the ASIA, EASTERN. The intermediate host is a snail. It occurs in man and other mammals. Schistosoma japonicums,japonicum, Schistosoma
D012552 Schistosomiasis Infection with flukes (trematodes) of the genus SCHISTOSOMA. Three species produce the most frequent clinical diseases: SCHISTOSOMA HAEMATOBIUM (endemic in Africa and the Middle East), SCHISTOSOMA MANSONI (in Egypt, northern and southern Africa, some West Indies islands, northern 2/3 of South America), and SCHISTOSOMA JAPONICUM (in Japan, China, the Philippines, Celebes, Thailand, Laos). S. mansoni is often seen in Puerto Ricans living in the United States. Bilharziasis,Katayama Fever,Schistoma Infection,Bilharziases,Fever, Katayama,Infection, Schistoma,Infections, Schistoma,Schistoma Infections,Schistosomiases
D012556 Schistosomicides Agents that act systemically to kill adult schistosomes. Antischistosomal Agent,Antischistosomal Agents,Schistosomicide,Agent, Antischistosomal,Agents, Antischistosomal
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular

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