67135-97-1Relevant academic research and scientific papers
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors
Pajouhesh, Hassan,Feng, Zhong-Ping,Ding, Yanbing,Zhang, Lingyun,Pajouhesh, Hossein,Morrison, Jerrie-Lynn,Belardetti, Francesco,Tringham, Elizabeth,Simonson, Eric,Vanderah, Todd W.,Porreca, Frank,Zamponi, Gerald W.,Mitscher, Lester A.,Snutch, Terrance P.
scheme or table, p. 1378 - 1383 (2010/07/06)
A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC50 values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.
ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 28, (2008/06/13)
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of isoxazole containing compounds are disclosed of the general formula (1) where Z is N or CHNR3 and (Ar1)2CR4 is optionally substituted benzhydryl.
Comparative Mechanistic Study of the Reaction of Benzophenone with n-BuMgBr and n-BuLi
Yamataka, Hiroshi,Miyano, Nobutaka,Hanafusa, Terukiyo
, p. 2573 - 2575 (2007/10/02)
Substituent effects on reactivity and product distribution (addition vs reduction) were determined for the reactions of benzophenones with n-BuMgBr and n-BuLi at 0 deg C.In case of the reaction with n-BuMgBr, meta and para-substituted benzophenones gave a reasonably linear Hammet plot, from which the ρ value of 1.45 was calculated, while ortho-substituted derivatives deviated downward from the correlation line.In contrast, the reaction with n-BuLi exhibit very small substituent effects on reactivity.The product distrubution is highly dependent on substituents in the n-BuMgBr reaction, whereas it is essentially independent of substituents in the n-BuLi reaction.Mechanistic differences between the reactions of these two reagents are discussed on the basis of these experimental results.
ASSYMETRIC REDUCTIONS OF KETONES USING LITHIUM ALUMINIUM HYDRIDE MODIFIED WITH N,N-DIALKYL DERIVATIVES OF (R)-(-)-2-AMINOBUTAN-1-OL
Brown, Eric,Penfornis, Annie,Bayma, Joaquim,Touet, Joeul
, p. 339 - 342 (2007/10/02)
LiAlH4 previuosly treated with 2 equivalents of (R)-(-)-2-(2-iso-indolinyl)butan-1-ol (a readily available reagent) reduced 2-chloro and 2,4-dimethyl benzophenones into the corresponding benzhydrols with 100percent enantiomeric excess.Other examples of ketone reductions are given.
