13375-29-6Relevant academic research and scientific papers
Phosphodiesterase 4 inhibitors as airways smooth muscle relaxant agents: synthesis and biological activities of triazine derivatives
Leroux,Van Keulen,Daliers,Pommery,Henichart
, p. 509 - 516 (1999)
A series of triazine derivatives was synthesized. The compounds were evaluated for tracheal smooth muscle relaxant and type 4 phosphodiesterase inhibitory activities. A highly significant correlation was observed between the two effects. Two compounds exh
A process for the preparation of cyclopropyl methylamine
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Paragraph 0027-0028, (2017/03/08)
The invention relates to a method for preparing dicyclopropane methyl amine. The method comprises a step of performing catalytic hydrogenation on the dicyclopropane ketoxime and the hydrogen under the existence of a catalyst to generate the dicyclopropane methyl amine, wherein the raney nickel is taken as a catalyst in the catalytic hydrogenation and the process is performed in the water or the alkaline solution at the temperature of 30-90 DEG C. Compared with the current hydrogenation, the method has the advantages that a high-purity product with obviously increased yield can be obtained, the salt formation and dissociation process in an alcohol solvent can be avoided and the operation can be greatly simplified, besides, the costs of the solvent and the post-processing solvent can be greatly reduced, the wastewater discharge can be reduced and the process is green and environmentally friendly.
THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
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, (2015/02/02)
Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
New imidazoline/α2-adrenoceptors affecting compounds-4(5)-(2-aminoethyl)imidazoline (dihydrohistamine) derivatives. Synthesis and receptor affinity studies
Treder, Adam P.,Andruszkiewicz, Ryszard,Zgoda, W?odzimierz,Walkowiak, Aleksandra,Ford, Celeste,Hudson, Alan L.
, p. 156 - 167 (2011/03/18)
Compilation of agmatine structure and imidazoline moiety leads to a new group of imidazoline/α2-adrenoceptor ligands, 4(5)-(2-aminoethyl)imidazoline derivatives. In this study the exploration of previously unknown 4(5)-(2-aminoethyl)imidazolines including the analogues of reported imidazoline and α2-aderenoceptors ligands: clonidine, rilmenidine, idazoxan, efaroxan, antazoline, tracizoline is described. The synthesis of a variety of novel 4(5)-(2-aminoethyl)imidazolines and their I 1, I2, α2-adrenoceptors affinities are reported.
Influence of bulky substituents on histamine H3 receptor agonist/antagonist properties
Sasse, Astrid,Ligneau, Xavier,Rouleau, Agnès,Elz, Sigurd,Ganellin, C. Robin,Arrang, Jean-Michel,Schwartz, Jean-Charles,Schunack, Walter,Stark, Holger
, p. 4000 - 4010 (2007/10/03)
Novel derivatives of 3-(1H-imidazol-4-yl)propanol were designed on the basis of lead compounds belonging to the carbamate or ether series possessing (partial) agonist properties on screening assays of the histamine H3 receptor. One pair of enantiomers in the series of α-methyl-branched chiral carbamates was stereoselectively prepared in high optical yields. Enantiomeric purity was checked by Mosher amide derivatives of precursors and capillary electrophoresis of the final compounds with trimethyl-β-cyclodextrin as chiral selector, and was determined to be ≥95%. The novel compounds were investigated in various histamine H3 receptor assays in vitro and in vivo. Some compounds displayed partial agonist activity on synaptosomes of rat brain cortex, whereas others exhibited antagonist properties only. Selected compounds were investigated in [125I]iodoproxyfan binding studies on the human histamine H3 receptor and showed high affinity in the nanomolar concentration range. Under in vivo conditions after oral administration to mice, some of the compounds exhibited partial or full agonist activity in the brain at low dosages. The (S)-enantiomer of one pair of chiral carbamates (9) proved to be the eutomer; thus, the (S)-enantiomer was selected for further pharmacological studies. In a peripheral in vivo test model in rats, measuring the level of inhibition of capsaicin-induced plasma extravasation, (S)-9 again proved its high oral agonist potency with full intrinsic activity (ED50 values of 0.07-0.1 mg/kg depending on tissue).
Amberlyst-15(H+)-NaBH4-LiCl: An effective reductor for oximes and hydrazones
Baruah, Bipul,Dutta, Manu P.,Boruah, Anima,Prajapati, Dipak,Sandhu, Jagir S.
, p. 409 - 410 (2007/10/03)
A simple and mild procedure reduces oximes and hydrazones on amberlyst 15(H+) support with LiCl-NaBH4 to the corresponding amines and hydrazines respectively in high yield and purity.
New prolyl endopeptidase inhibitors: In vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives
Portevin, Bernard,Benoist, Alain,Rémond, Georges,Hervé, Yolande,Vincent, Michel,Lepagnol, Jean,De Nanteuil, Guillaume
, p. 2379 - 2391 (2007/10/03)
A series of potent and selective prolylendopeptidase (PEP) inhibitors of the α-keto heterocyclic type has been obtained by replacing the classical central proline of 1-[1-(4-phenylbutanoyl)-L-prolyl]pyrrolidine (SUAM 1221, 3) by non-natural amino acids PHI, ABO, and ABH. These 4-phenylbutanoyl side- chain-containing inhibitors exhibited potent in vitro inhibitory potencies with IC50 around 30 nM (compounds 24 and 25). Modulation of the side chain by replacement of the terminal phenyl ring by the dicyclopropyl moiety afforded derivatives 30 and 32 with improved potencies (IC50 between 10 and 20 nM). Furthermore, replacing the linear 4-phenylbutanoyl side chain by the (2-phenylcyclopropyl)carbonyl entity provided potent inhibitors with IC50 culminating at 0.9 nM on a rat cortex enzymatic preparation (compound 70). The configuration of the cyclopropyl ring had to be R,R in order to obtain not only a strong PEP inhibition in vitro but also a good activity in vivo, exemplified by inhibitor 68, which gave ID50 ip and po of 0.3 and 1 mg/kg, respectively. Finally, demonstration of the cognition-enhancing properties of compound 54 was given in the passive avoidance test using scopolamine- induced amnesia in the rat, where it dose dependently inhibited the scopolamine-induced decrease in avoidance response.
Reduction of Oximes with Sodium Borohydride in the Presence of Transition Metal Compounds
Ipaktschi, Junes
, p. 856 - 858 (2007/10/02)
The reduction of oximes with sodium borohydride in the presence of NiCl2 * 6 H2O and MoO3 was investigated.The combination of NaBH4 with NiCl2 * 6 H2O converted the unsaturated oximes through exhaustive reduction into saturated amines (Table 1).The C = C double bond remains preserved if the reduction is carried out in the presence of MoO3 (Table 2).The stereochemistry of the reduction in the presence of NiCl2 * 6 H2O is distinctivly different from that of MoO3.
