89197-63-7

Upstream product

• 89197-62-6 5-fluorobenzofuran-2-carboxylic acid 
• 135634-27-4 (5-fluoro-2,3-dihydro-benzofuran-2-yl)-methanol 
• 13997-72-3 1-allyl-2-hydroxy-5-fluorobenzene 
• 13990-72-2 1-allyloxy-4-fluorobenzene 
• 371-41-5 4-Fluorophenol 
• 93849-31-1 ethyl 5-fluoro-1H-benzofuran-2-carboxylate 
• 347-54-6 5-fluoro-2-hydroxybenzaldehyde 

Relevant academic research and scientific papers

ANTHELMINTIC COMPOUNDS AND COMPOSITIONS AND METHOD OF USING THEREOF

The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

α-Adrenoreceptor Reagents. 2. Effects of Modification of the 1,4-Benzodioxan Ring System on α-Adrenoreceptor Activity

Modification of the 1,4-benzodioxan ring present in RX 781094 (1) has not previously been considered.This paper describes a number of analogues of this ring system, including compounds in which one of the oxygen atoms has been replaced by a methylene group and also those in which the ring size has been changed to give, for example, furan and thiophene derivatives.The dihydroxybenzofuranylimidazoline compound 7 is the only analogue possesing presynaptic antagonist potency and selectivity comparable to that of 1.In view of this result, a number of derivatives was prepared to determine the structure-activity relationships within this series.Many derivatives, as well as the parent compound 7, were found to possess presynaptic α2-adrenoreceptor antagonist and postsynaptic α1-adrenoreceptor partial agonist properties.Two of the selective presynaptic antagonists,13 and 14, possess greater potency and selectivity than that possessed by 1.The 5-chloro derivative 25 is twice as potent as 1 after oral administration but only about half as potent when given intravenously.

Imidazoline derivatives as presynaptic α2 -adrenoreceptor antagonists

Imidazoline derivatives of the formula STR1 wherein R1 is hydrogen or alkyl C1-6 ; R2 is hydrogen, methyl, chloro, bromo or fluoro; R3 is hydrogen, methyl, hydroxy, methoxy, fluoro, chloro or bromo; and their non-toxic salts. Processes for their preparation and pharmaceutical compositions thereof. The compounds exhibit presynaptic α2 -adrenoreceptor antagonist activity.