- PIPERAZIN DERIVATIVES AND THEIR USE IN CONTROLLING PESTS
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The use of a compound of formula (I) wherein Y is a single bond, C=O, C=S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Ra, R1 , R2 , R4 and R8 are specified organic groups; n and p are independently 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
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Page/Page column 96-97
(2010/02/14)
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- Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4- fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors
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A series of novel diamine, amine-amide, and piperazinone analogues of N- [2-(bisarylmethoxy)-ethyl]-N'-(phenylpropyl)piperazines, GBR 12909 and 12935, were synthesized and evaluated as inhibitors of presynaptic monoamine neurotransmitter transporters. The primary objective of the study was to determine the structural requirements for selectivity of ligand binding and potency for neurotransmitter reuptake inhibition. In general, the target compounds retained transporter affinity; however, structural variations produced significant effects on reuptake inhibition and transporter selectivity. For example, analogues prepared by replacing the piperazine ring in the GBR structure with an N,N'-dimethylpropyldiamine moiety displayed enhanced selectivity for binding and reuptake inhibition at the norepinephrine (NE) transporter site (e.g. 4 and 5). Congeners in which the amide nitrogen atom was attached to the aralkyl moiety of the GBR molecule showed moderate affinity (K(i) = 51-61 nM) and selectivity for the dopamine transporter (DAT) site. In contrast, introduction of a carbonyl group adjacent to either nitrogen atom of the piperazine ring (e.g. 25 and 27) was not well tolerated. From the compounds prepared, analogue 16 was selected for further evaluation. With this congener, locomotor activity induced by cocaine at a dose of 20 mg/kg was attenuated with an-AD50 (dose attenuating cocaine-induced stimulation by 50%) of 60.0 ± 3.6 mg/kg.
- Choi, Sung-Woon,Elmaleh, David R.,Hanson, Robert N.,Fischman, Alan J.
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p. 3647 - 3656
(2007/10/03)
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