- 6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 37; 37-38
(2008/12/08)
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- Unusual rearrangement of spiro β-lactams to 1,4-diazabicyclo[4,4,0] decanes and 1,4-diazabicyclo[4,3,0]nonanes. Synthesis of conformationally restricted σ-receptor ligands
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Synthesis of 1,4-diazabicyclo[4,4,0]decanes and 1,4-diazabicyclo[4,3,0] nonanes was achieved by using 4-formyl spiro β-lactams as easily available starting materials. Furthermore, the application of this protocol to the preparation of conformationally res
- Macías, Alberto,Alonso, Eduardo,Del Pozo, Carlos,González, Javier
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p. 4657 - 4660
(2007/10/03)
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- Studies in Potential Filaricides: Part XIII - Synthesis of 1,4-Diazabicyclononanes, 1,4-Diazabicyclodecanes and 1,4-Diazabicycloundecanes as diethylcarbamazine Analogs
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1,4-Diazabicyclononanes (13 - 20), 1,4-diazabicyclodecanes (21 - 28), 1,4-diazabicycloundecanes (29 - 34), 1,4-diazabicyclononan-5-ones (37 - 41) and 1,4-diazabicyclodecan-5-ones (42 - 44) having alkyl and acyl substituents at 4-position have been synthesized and evaluated for their filaricidal activity against Litomasoides carinii infection in cotton rats.Except 4-diethylcarbamoyl-1,4-diazabicyclononane (13), which exhibits significant activity, being about 3/5th as active as the standard diethylcarbamazine (DEC), none of the other compounds shows any activity against adult worms.The results have been rationalised in terms of critical bulk around the N-1 of the piperazine ring of DEC.From this work and earlier published results it appears that both axial and equatorial N-CH3 bonds in DEC are acceptable for activity.
- Shukla, U. K.,Khanna, J. M.,Sharma, Satyavan,Anand, Nitya,Chatterjee, R. K.,Sen, A. B.
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p. 664 - 668
(2007/10/02)
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