Biomaterial Database

Synthesis and antischistosomal activity of a new 2-nicotinoyl dipeptide analogue of praziquantel. 1996

M H Abo-Ghalia, and A E Soliman

National Research Centre, Dokki, Cairo, Egypt.

As an approach to a structure-antischistosomal activity-relationship with possible pharmacological potentiation of the anthelmintic drug praziquantel, a new dipeptide analogue, namely, N alpha-nicotinoyl-L-aspartyl-beta-(1,2,3,6,7,11b-hexahydro-4H-pyrazino[2- 1a]isoquinoline-4-one)-L-phenylalanine methyl ester, was synthesized and antischistosomally investigated in mice infected with S. mansoni cercariae. Parallely, its simple 2-nicotinoyl analogue was synthesized and tested. Both compounds were less, but still, interestingly active (approximately 63 and approximately 66%, respectively) compared to praziquantel (approximately 90%).

UI	MeSH Term	Description	Entries
D008099	Liver	A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.	Livers
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
D005260	Female		Females
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
D012550	Schistosoma mansoni	A species of trematode blood flukes of the family Schistosomatidae. It is common in the Nile delta. The intermediate host is the planorbid snail. This parasite causes schistosomiasis mansoni and intestinal bilharziasis.	Schistosoma mansonus,mansonus, Schistosoma
D012555	Schistosomiasis mansoni	Schistosomiasis caused by Schistosoma mansoni. It is endemic in Africa, the Middle East, South America, and the Caribbean and affects mainly the bowel, spleen, and liver.	Schistosomiasis, Intestinal,Schistosoma mansoni Infection,Infection, Schistosoma mansoni,Infections, Schistosoma mansoni,Intestinal Schistosomiases,Intestinal Schistosomiasis,Schistosoma mansoni Infections,Schistosomiases, Intestinal
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
D051379	Mice	The common name for the genus Mus.	Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus