Search results for "Biological activity"
showing 10 items of 465 documents
Muskelrelaxantien, 4. Mitt. Monoacylbutyroguanamine
1986
Die Umsetzung von Butyroguanamin (1) mit den Carbonsaureanhydriden 2a−f bei 80–120° fuhrt zu den Monoacylbutyroguanaminen 3a−f, deren Struktur durch IR-, 1H-NMR- und MS-Spektren untermauert wird. Unter den hier beschriebenen Verbindungen weisen insbesondere 3e muskelrelaxierende und antidiabetische und 3a trichomonazide und antivirale Wirksamkeit auf, wahrend mit 3b−d herbizide Wirkungen beobachtet werden. Muscle Relaxants, IV: Monoacylbutyroguanamines Reaction of butyroguanamine (1) with the carboxylic acid anhydrides 2a−f at 80–120°C leads to the monoacylbutyroguanamines 3a−f, the structure of which is supported by IR, 1H-NMR, and mass spectra. Among the compounds described here, particul…
ChemInform Abstract: 1,2,3-Triazole in Heterocyclic Compounds, Endowed with Biological Activity, Through 1,3-Dipolar Cycloadditions
2014
1,3-Dipolar cycloaddition reactions can be considered a powerful synthetic tool in the building of heterocyclic rings, with applications in different fields. In this review we focus on the synthesis of biologically active compounds possessing the 1,2,3-triazole core through 1,3-dipolar cycloaddition reactions. The 1,2,3-triazole skeleton can be present as a single disubstituted ring, as a linker between two molecules, or embedded in a polyheterocycle. The cycloaddition reactions are usually catalysed by copper or ruthenium. Domino reactions can be achieved through dipolarophile anion formation, generally followed by cyclisation. The variety of attainable heterocyclic structures gives an ill…
Antimykotische Wirkstoffe, 16. Mitt. Halogenierte Cyanaminomethylenpiperidine und -piperazine
1984
Die in Gegenwart der sekundaren Amine 5a-e mit Hilfe von s-Triazin (2) als Dreikomponentenreaktion durchgefuhrte Aminomethinylierung von Cyanamid (1) liefert die korrespondierenden als Dehydro-N-Mannich-Basen aufzufassenden Cyanaminomethylenheterocyclen 6a-e. Insbesondere 6a und 6e besitzen antimykotische Wirksamkeit. Antimycotic Agents, XVI: Halogenated (Cyanaminomethylene)piperidines and -piperazines The aminomethinylation of cyanamide (1) by means of s-triazine (2), carried out as three-component reaction in the presence of the secondary amines 5a–e, yields the cyanaminomethylene heterocycles 6a–e, which are to be classed as dehydro-N-Mannich bases. Compounds 6a and 6e in particular show…
H2-Antihistaminika, 25. Mitt. Synthese und H2-antagonistische Wirkung monosubstituierter 1,2,4-Oxadiazol-3,5-diamine
1985
Es wurden die N3- bzw. N5-substituierten 1,2,4-Oxadiazol-3,5-diamine 4a-e und 5a-e dargestellt und auf Histamin-H2-antagonistische Aktivitat untersucht. H2-Antihistaminics, XXV: Synthesis and H2-Antagonistic Activity of Monosubstituted 1,2,4-Oxadiazole-3,5-diamines The N3-or N5-substituted 1,2,4-Oxadiazole-3,5-diamines 4a-e and 5a-e were prepared and tested for histamine H2-antagonistic activity.
ChemInform Abstract: Synthesis of Pyrido[2,1-a]isoquinolin-4-ones and Oxazino[2,3-a]isoquinolin-4-ones: New Inhibitors of Mitochondrial Respiratory C…
2014
Benzo[a]quinolizine is an important heterocyclic framework that can be found in numerous bioactive compounds. The general scheme for the synthesis of these compounds was based on the preparation of the appropriate dihydroisoquinolines by Bischler-Napieralski cyclization with good yields, followed by the Pemberton method to form the oxazinones or pyridones derivatives via acyl-ketene imine cyclocondensation. All the synthesized compounds were assayed in vitro for their ability to inhibit mitochondrial respiratory chain. Most of the tested compounds were able to inhibit the integrated electron transfer chain, measured as NADH oxidation, which includes complexes I, III and IV, in the low micro…
4-[5-(4-Fluorophenyl)-3-isopropylisoxazol-4-yl]pyridine
2006
In the title compound, C17H15FN2O, the exocyclic bond angles at the C atoms of the isoxazole ring bearing the pyridyl and 4-fluorophenyl substituents are 129.66 (17) and 134.58 (16)°, respectively. The structure was determined in a study of the molecular geometry of isoxazole derivatives with biological activity as MAPK inhibitors.
Synthesis and pharmacological activity of silyl isoxazolines 2
2003
Silyl isoxazolines have been synthesized by [2+3] cycloaddition reaction of nitrile oxides to vinyl- and allylsilanes. The addition of 3-pyridylnitrile oxide to 1,3-divinyl-1,1,3,3-tetraphenyldisiloxane affords 1,3-bis{5-[3-(3-pyridyl)isoxazolin-2-yl]}-1,1,3,3-tetraphenyldisiloxane; the latter exists as a mixture of trans- and cis-isomers.The bond angle of the Si–O–Si fragment in thetrans-isomer equals 180(3)° and in the cis-isomer it is 162(3)°.The pharmacological properties of 4-[3-(5-trimethylsilylisoxazolin-2-yl)]pyridinium-chloride have been studied.
Oligopeptide der β-Carbolin-3-carbonsäure - Synthese und Affinität zu Benzodiazepinrezeptoren
1987
Es wurden Oligopeptide der β-Carbolin-3-carbonsaure dargestellt und deren Affinitat zum Benzodiazepinrezeptor in Mausehirn-Membranen bestimmt. Uber Struktur-Affinitatsbeziehungen wird berichtet. Oligopeptides of β-Carboline-3-carboxylic Acid - Synthesis and Benzodiazepine Receptor Affinity Oligopeptides of β-carboline-3-carboxylic acid were prepared and tested with respect to their affinity for the benzodiazepine receptor in mouse brain membranes. Structure-affinity relationships are reported.
H2-Antihistaminika, 18. Mitt. 5,6-Alkylsubstituierte 4-Pyrimidinone mit H2-antihistaminischer Wirkung
1984
5,6-Alkylsubstituierte 2-{2-[(5-Methyl-4-imidazolyl)-methylthio]-ethylamino}-4-pyrimidinone wurden dargestellt und auf ihre H2-antihistaminische Wirksamkeit untersucht. H2-Antihistaminics, XVIII: 5,6-Alkyl-4-pyrimidones with H2-Antihistaminic Activity 5,6-Alkyl-2-{2-[(5-methyl-4-imidazolyl)methylthio]ethylamino}-4- pyrimidones were prepared and tested for their H2-antihistaminic activities.
H2-Antihistaminika, 34. Mitt. 1,3,4-Oxadiazol-2,5-diamine mit H2-antagonistischer Aktivität
1987
Es wird uber die Synthese und H2-antagonistische Wirksamkeit von mono- und disubstituierten 1,3,4-Oxadiazol-2,5-diaminen mit Piperidinomethylphenoxypropylseitenkette sowie deren methylierte Derivate berichtet. H2-Antihistaminics, XXXIV: 1,3,4-Oxadiazole-2,5-diamines with H2-Antagonistic Activity Syntheses and H2-antagonistic activities of mono- and disubstituted 1,3,4-oxadiazole-2,5-diamines with a [(piperidinomethyl)phenoxy]propyl substituent and of their methyl derivatives are reported.