833480-90-3Relevant articles and documents
Dantrolene analogues revisited: General synthesis and specific functions capable of discriminating two kinds of Ca2+ release from sarcoplasmic reticulum of mouse skeletal muscle
Hosoya, Takamitsu,Aoyama, Hiroshi,Ikemoto, Takaaki,Kihara, Yasutaka,Hiramatsu, Toshiyuki,Endo, Makoto,Suzuki, Masaaki
, p. 663 - 673 (2003)
The general synthesis of dantrolene analogues with various substituents on its phenyl ring has been developed via palladium-catalyzed cross-coupling reactions, the Stille or Suzuki reaction, as the key step. The effects of synthesized analogues have been evaluated by two kinds of Ca2+ release modes from sarcoplasmic reticulum (SR) of mouse skeletal muscle fibers based on: (1) the measurement of twitch contraction caused by the physiological Ca2+ release (PCR) of intact skeletal muscle and (2) the rate of Ca2+-induced Ca2+ release (CICR) in saponin-treated skinned muscle fibers. Although dantrolene, a lead compound, inhibits both twitch contraction and CICR, some structurally modified analogues exhibit one or the other of these effects. The methoxy congener, GIF-0185, potently inhibits the twitch contraction without affecting the CICR, while GIF-0166 and GIF-0248, the ortho-nitro regioisomer and ortho, ortho-dinitro substituted analogues, respectively, doubly potentiate the CICR exclusively.
Mechanochemistry for "no solvent, no base" preparation of hydantoin-based active pharmaceutical ingredients: Nitrofurantoin and dantrolene
Colacino, Evelina,Porcheddu, Andrea,Halasz, Ivan,Charnay, Clarence,Delogu, Francesco,Guerra, Ruben,Fullenwarth, Julien
supporting information, p. 2973 - 2977 (2018/07/13)
The eco-compatible, base- and waste-free, energy-efficient, low-environmental-impact, gram-scale, mechanochemical preparation of marketed drugs such as nitrofurantoin (Furantin), dantrolene (Dantrium) and their structurally related derivatives is herein reported. Not a drop of organic solvent was used for the entire process and high yields of pure compounds were obtained without post-reaction work-up. Hydrazones were stable in the presence of water and gaseous HCl, formed as by-products during the synthesis. Comparative mechanochemical experiments were performed using diverse milling devices and jar materials, the active pharmaceutical ingredients were analyzed by PXRD and green metrics are calculated.
PACKAGING BAG FOR PLASTER AND PACKAGED PLASTER
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, (2008/06/13)
Packaged patch (10) according to the invention comprises patch (2) situated in space (4) inside patch package (3) composed of laminated packaging material (1), and its edges are sealed. Laminated packaging material (1) comprises hygroscopic material layer (13) made of LDPE containing 20-40 wt% of an inorganic filler, situated between moisture-permeable material layer (14) made of LDPE and having a moisture permeability of 40-120 g/m2/day and a screen material layer which blocks penetration of moisture, etc. and is composed of HDPE layer (12) and aluminum foil (11). The saturation hygroscopicity of laminated packaging material (1) is 2-30 g/m2under atmosphere conditions with a temperature of 25°C and a relative humidity of 75%. This construction sufficiently reduces the effect of moisture on a drug in patch (2) and allows patch (2) to be held in a stable state for prolonged periods, while also improving the economy and handleability of patch package (3).
Solid phase synthesis of 1-aminohydantoin libraries
Wilson, Lawrence J.,Li, Min,Portlock, David E.
, p. 5135 - 5138 (2007/10/03)
The solid support synthesis of a series of I-aminohydantoins based on a diverse set of hydrazino amino acid, aldehydes, and amines is described. The method involves the construction of resin attached hydrazino acid precursors, followed by subsequent derivatization, and then cyclizative cleavage off the resin. Overall yields vary per example between 15 and 60%, and the samples are suitable for biological evaluations without further purification.
