Synthesis and Octopaminergic Agonist Activity of 2-(Substituted benzylamino)-2-thiazolines
2-(Substituted benzylamino)-2-thiazolines (SBAT) were synthesized by a hydrochloric acid-catalyzed cyclization of the corresponding thioureas, using a reaction of 2-methylthio-2-thiazoline with substituted benzylamines or by alkylating 2-amino-2-thiazoline. 2-(Alkylthio)-2-thiazolines were obtained by alkylating 2-mercaptothiazoline.Most of the SBAT compounds activated adenylate cyclase in homogenates of cockroach ventral nerve cords; the effect of introducing substituents at the phenyl of the SBAT compounds on octopaminergic agonist activity was not significant. 2--2-thiazolines and 2-(alkylthio)-2-thiazolines were not significant octopaminergic agonists.Washing removed nearly all of the activity of one of the SBAT compounds, suggesting that the SBAT compounds bound reversibly to the octopaminergic receptor.
Hirashima, Akinori,Yoshii, Yutaka,Eto, Morifusa
p. 1062 - 1065
(2007/10/02)
Synthesis of new 'benzyl'-thiourea derivatives and their cyclic analogues with diuretic and saluretic activity
A series of new 'benzyl'-thiourea derivatives 2 and their cyclic analogues 3 were synthesized and tested for diuretic activity. The structure-activity relationships - being also computed - are discussed. Some selected compounds were studied in detail for
Reiter,Toldy,Schafer,et al.
p. 41 - 53
(2007/10/02)
2-Aminothiazoline derivatives. Relationships between structure and antiinflammatory activity
Pharmacological studies of 2-aminothiazoline amide and amine derivatives show these compounds to be actively anti-inflammatory. The structure determination by spectroscopic methods and X-ray diffraction indicates a relation between the structure and the activity of these compounds.
Viallet,Boucherle,Cohen-Addad
p. 553 - 559
(2007/10/05)
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