QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2-BENZAMIDO-5-NITROTHIAZOLE MOLLUSCICIDAL DERIVATIVES

Citation
P. Vignoles et al., QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS OF 2-BENZAMIDO-5-NITROTHIAZOLE MOLLUSCICIDAL DERIVATIVES, Quantitative structure-activity relationships, 13(4), 1994, pp. 426-432
Citations number
18
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
09318771
Volume
13
Issue
4
Year of publication
1994
Pages
426 - 432
Database
ISI
SICI code
0931-8771(1994)13:4<426:QSO2>2.0.ZU;2-N
Abstract
The pharmacologic action of 2-benzamido-5-nitrothiazole and eleven der ivatives was studied in Lymnaea peregra ovata Muller, Gammarus pulex p ulex L., and Euglena gracilis Klebs. The toxicity parameters (50 % let hal concentration, 50 % inhibitory concentration) were correlated with the physicochemical parameters of the compounds (lipophilicity, stabi lity). The toxicity of the molecule was related to its lipophilicity a nd stability. By combining these parameters it was possible to establi sh specific equations for each species studied. Linear equations of th e overall parameters of the molecule were obtained with L.p. ovata and E. gracilis, whereas second-degree relationships were found with G. p . pulex. Using these pharmacokinetics models, it is possible to predic t the pharmacologic action of these compounds knowing only the physico chemical parameters of each molecule.