Search results for "3-Amino-1"
showing 10 items of 12 documents
Ethanol Modulates Corticotropin Releasing Hormone Release From the Rat Hypothalamus: Does Acetaldehyde Play a Role?
2010
BACKGROUND AND METHODS Ethanol (EtOH) activates hypothalamic-pituitary-adrenal (HPA) axis, resulting in adrenocorticotropin hormone, glucocorticoid release, and in modifications of the response of the axis to other stressors. The initial site of EtOH action within the HPA system seems to be the hypothalamus. Thus, to determine the mechanisms responsible for these effects, we investigated: (i) whether EtOH was able to release corticotrophic releasing hormone (CRH) from incubated hypothalamic explants; (ii) whether acetaldehyde (ACD), its first metabolite formed in the brain by catalase activity, might play a role in EtOH activity. To this aim, rat hypothalamic explants were incubated with: (…
Reaction of 3-Amino-1,2,4-Triazole with Diethyl Phosphite and Triethyl Orthoformate: Acid-Base Properties and Antiosteoporotic Activities of the Prod…
2017
The reaction of diethyl phosphite with triethyl orthoformate and a primary amine followed by hydrolysis is presented, and the reaction was suitable for the preparation of (aminomethylene)bisphosphonates. 3-Amino-1,2,4-triazole was chosen as an interesting substrate for this reaction because it possesses multiple groups that can serve as the amino component in the reaction-namely, the side-chain and triazole amines. This substrate readily forms 1,2,4-triazolyl-3-yl-aminomethylenebisphosphonic acid (compound 1) as a major product, along with N-ethylated bisphosphonates as side products. The in vitro antiproliferative effects of the synthesized aminomethylenebisphosphonic acids against J774E m…
Discovery of the 3-Amino-1,2,4-triazine-Based Library as Selective PDK1 Inhibitors with Therapeutic Potential in Highly Aggressive Pancreatic Ductal …
2023
Pyruvate dehydrogenase kinases (PDKs) are serine/threonine kinases, that are directly involved in altered cancer cell metabolism, resulting in cancer aggressiveness and resistance. Dichloroacetic acid (DCA) is the first PDK inhibitor that has entered phase II clinical; however, several side effects associated with weak anticancer activity and excessive drug dose (100 mg/kg) have led to its limitation in clinical application. Building upon a molecular hybridization approach, a small library of 3-amino-1,2,4-triazine derivatives has been designed, synthesized, and characterized for their PDK inhibitory activity using in silico, in vitro, and in vivo assays. Biochemical screenings showed that …
CCDC 1005287: Experimental Crystal Structure Determination
2014
Related Article: Michael Giese, Markus Albrecht, Arto Valkonen, Kari Rissanen|2015|Chemical Science|6|354|doi:10.1039/C4SC02762K
CCDC 902349: Experimental Crystal Structure Determination
2013
Related Article: A.L.Mindich, N.A.Bokach, M.L.Kuznetsov, M.Haukka, A.P.Zhdanov, K.Yu.Zhizhin, S.A.Miltsov, N.T.Kuznetsov, V.Yu.Kukushkin|2012|ChemPlusChem|77|1075|doi:10.1002/cplu.201200257
CCDC 631805: Experimental Crystal Structure Determination
2008
Related Article: A.Kusakiewicz-Dawid, E.Masiukiewicz, B.Rzeszotarska, I.Dybala, A.E.Koziol, M.A.Broda|2007|Chem.Pharm.Bull.|55|747|doi:10.1248/cpb.55.747
CCDC 268080: Experimental Crystal Structure Determination
2005
Related Article: E.Goreshnik, D.Schollmeyer, M.Mys'kiv|2005|Acta Crystallogr.,Sect.C:Cryst.Struct.Commun.|61|m127|doi:10.1107/S0108270105000806
CCDC 620768: Experimental Crystal Structure Determination
2006
Related Article: A.E.Koziol, T.Lis, E.Kolodziejczyk, A.Kusakiewicz-Dawid, B.Rzeszotarska|2006|Acta Crystallogr.,Sect.E:Struct.Rep.Online|62|o3664|doi:10.1107/S1600536806029515
CCDC 277295: Experimental Crystal Structure Determination
2006
Related Article: H.Sopo, J.Sviili, A.Valkonen, R.Sillanpaa|2006|Polyhedron|25|1223|doi:10.1016/j.poly.2005.08.044
Susceptibility of Methyl 3-Amino-1H-pyrazole-5-carboxylate to Acylation
2009
Abstract In the search for a new method of synthesis of hybrid peptides with aminopyrazole carboxylic acid, we tried to force selective acylation at the aromatic amino group instead of at the ring nitrogen atom with fairly gentle acylating agents. The acylating agents used were acid anhydrides: acetic anhydride, tert-butyl pyrocarbonate, and 2-(2-methoxyethoxy)ethoxyacetic acid/dicyclohexylcarbodiimide. We succceded in acylation at this amino group with almost none at the ring nitrogen atom. Sometimes, however, acylation in small quantities at the ring nitrogen atom was observed as a by-product. To remove this by-product, imidazole was used. Thus, we were able to obtain the hybrid peptides …