3898-07-5Relevant academic research and scientific papers
Aminoguanidine hydrazone derivatives as non-peptide NPFF1 receptor antagonists reverse opioid induced hyperalgesia
Hammoud, Hassan,Elhabazi, Khadija,Quillet, Rapha?lle,Bertin, Isabelle,Utard, Valérie,Laboureyras, Emilie,Bourguignon, Jean-Jacques,Bihel, Frederic,Simonnet, Guy,Simonin, Frederic,Schmitt, Martine
, (2018/05/15)
Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's). Binding experiments and functional assays highlighted AGH 1n and its rigidified analog 2-amino-dihydropyrimidine 22e for in vivo experiments. As earlier shown with the prototypical dipeptide antagonist RF9, both 1n and 22e reduced significantly the long lasting fentanyl-induced hyperalgesia in rodents. Altogether these data indicate that AGH rigidification maintains nanomolar affinities for both NPFF receptors, while improving antagonist character towards NPFF1R.
A NO donor type he Augmentin derivatives, preparation method and application (by machine translation)
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, (2017/08/31)
The invention provides a having the general formula (I) as shown in the structural formula of the compound, the compound has better NO release of the active, with better prospect of application, can be used for anti-inflammatory, anti-thrombotic, anti-platelet activity, reducing cholesterol and triglyceride levels and/or improve the high density lipoprotein levels, treatment of peripheral ischemia, diabetic vascular complications in or atherosclerosis. The invention also provides a method for preparing said compound. (by machine translation)
Synthesis and Biological Activity of Some New 1-Aryl-2-S-methyl-5-(2-pyridyl/2-furfuryl)isodithiobiurets
Shridhar, D. R.,Gandhi, S. S.,Rao, K. Srinivasa,Rastogi, K.
, p. 716 - 717 (2007/10/02)
A number of 1-aryl-2-S-methyl-5-(2-pyridyl/2-furfuryl)isodithiobiurets (II and III) have been synthesized by the condensation of various N-aryl-S-methylisothioureas (V) with 2-pyridyl- and 2-furfurylisothiocyanates and tested for anthelmintic, antiamoebic, antitrichomonal, antileishmanial and antimicrobial activities.
Synthesis & Pharmacological Evaluation of Ethyl 3-Substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates
Gupta, K. A.,Saxena, Anil K.,Jain, Padam C.
, p. 228 - 233 (2007/10/02)
A number of ethyl 3-substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates (V) have been prepared by the reaction of amidines (III) with diethyl ethoxymethylenemalonate.In order to confirm the structure (V), ethyl 3-(2'-methylphenyl)-2-methylmercapto-4(3H)pyrimidone-5-carboxylate (103) has been transformed into the earlier synthesised 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone (115) by decarboxylation of 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone-5-carboxylic acid (114), obtained by the alkaline hydrolysis of 103.Someof these compounds have shown antiinflammatory, diuretic and antipassive cutaneous anaphylaxis activities.
2-Imidazolines. IV (1). 1-Aryl-2-alkylthio-4,5-diamino-4,5-dihydroimidazoles. Synthesis and Properties
Meola, Stefania,Rivera, Elisabetta,Stradi, Riccardo,Gioia, Bruno
, p. 1041 - 1044 (2007/10/02)
1,2-Diimmonium salts (1) react with S-substituted isothioureas (3) yielding 2-alkylthio-4,5-diamino-4,5-dihydroimidazoles (4), which under mild pyrolytic conditions afforded 2-alkylthio-5-aminoimidazoles (7).Imidazolines (4) and imidazoles (7) were easily
