Piperazine N-substituted naphthyridines, pyridothienopyrimidines and pyridothienotriazines: new antiprotozoals active against Philasterides dicentrarchi.
New antiprotozoals active against Philasterides dicentrarchi, the causative agent of scuticociliatosis in farmed turbot and Black Sea bass-bream, have been synthesised and tested. The most active compounds posses a piperazine ring, generally N-bonded to the heterocycle, and are the 1,8-naphthyridines, 2f and 5o, the pyridothienopyrimidine (7), and the pyridothienotriazines, 8, 9, 12d, 12f, 12h, 12m and 12k. Pyridothienotriazine (12k) presents the same activity (Lethal Dose, LD=0.8/1.5 mg L(-1)) as the well-known antiparasitics niclosamide and oxyclozanide.
Quintela
José M
JM
Departamento de Qui;mica Fundamental e Industrial, Facultad de Ciencias, Universidad de La Coruña, 15071, La Coruña, Spain.
Peinador
Carlos
C
González
Liliana
L
Iglesias
Raúl
R
Paramá
Anabel
A
Alvarez
Francisca
F
Sanmartín
Manuel L
ML
Riguera
Ricardo
R
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001492:Bass / Q000469:parasitology; D016770:Ciliophora Infections / Q000469:parasitology*; D003470:Culture Media; D005393:Fish Diseases / Q000469:parasitology*; D005412:Flatfishes / Q000469:parasitology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D016802:Oligohymenophorea / Q000187:drug effects*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D003470:Culture Media; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D009287:Naphthyridines; D011743:Pyrimidines