Search results for "DISCOVERY"

Pyrazolo[3,4‐d]pyrimidine Derivatives as COX‐2 Selective Inhibitors: Synthesis and Molecular Modelling Studies

2009

The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin-4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5-benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5-aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a-d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological results.

Herbizide, 1. Mitt. 2-(4-Nitroanilino)pyrimidine

1982

Aus der Kondensation von 4-Nitrophenylguanidin (1) mit den β-Diketonen 2a–h gehen die 2-(4-Nitroanilino)pyrimidine 3a–h hervor. Als Aminoheterocyclus steht Verbindungstyp 3 in enger struktureller Beziehung zu 5-Acetyl-2-amino-4-methylthiazol, das herbizide Wirkungen auszuuben vermag. Herbicides, I: 2-(4-Nitroanilino)pyrimidines Condensation of 4-nitrophenylguanidine (1) with the β-diketones 2a–h yields the 2-(4-nitroanilino)pyrimidines 3a–h. Compounds of type 3 are aminoheterocycles and as such are closely related to 5-acetyl-2-amino-4-methylthiazole which exhibits herbicidal activity.

Trichomonazide Wirkstoffe, 2. Mitt. Verzweigtkettig 4,6-disubstituierte 2-Cyanaminopyrimidine

1985

Aus der Umsetzung von Dicyandiamid (1) mit den β-Diketonen 2a–b gehen die 4,6-verzweigtkettig disubstituierten 2-Cyanaminopyrimidine 3a–b hervor. Fur Strukturtyp 3 last sich aus den spektroskopischen Daten, speziell aus den 1H- und 13C-NMR-Werten, das Vorliegen eines Gleichgewichts zwischen den tautomeren 2-Cyanamino- und 2-Cyaniminopyrimidinformen ableiten. 3 zeichnet sich durch trichomonazide, antivirale und antimykotische Wirkung aus. Trichomonacidal Agents, II: 4,6-Disubstituted 2-(Cyanoamino)pyrimidines Carrying Branched Substituents The reaction of dicyandiamide (1) with the β-diketones 2a–b yields the 4,6-branched disubstituted 2-(cyanoamino)pyrimidines 3a–b. From spectroscopic evide…

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.

Chemoselective reactions of N1-methyl-2-hydroxy-3-methylamino-3-phenylpropanamide with electrophiles. Synthesis of chiral hexahydro-4-pyrimidinones a…

2002

Abstract The reactivity of (2S,3S)-N1-methyl-2-hydroxy-3-methylamino-3-phenylpropanamide 1 , containing three nucleophilic centres has been studied against dihaloalkanes and aldehydes. Hexahydro-4-pyrimidinones or oxazolidines were obtained chemoselectively. Experimental results were explained by ‘ab initio’ calculations.

Reaction of 2H-1-benzothiete with diazo compounds in the presence of rhodium(II) acetate

1995

2,3-Dihydrobenzo[b]thiophenes (7a-e) were prepared by the Rh2+ catalyzed reaction of 2H-1-benzothiete (1) and diazo compounds (3a-e). α,β-Unsaturated diazo esters (3b,e) and diazo ketones (3d,e) yielded additionally 4,5-dihydro-1-benzothiepins (11b,c) and 5H-4,1-benzoxathiepins (12d,e), respectively.

Cycloadditions in the pyrrole series

1972

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.

Triazolopyridines. Part 24: New polynitrogenated potential helicating ligands

2004

The synthesis of novel 7-{[1,2,3]triazolo[1,5-a]pyridin-3-yl}-[1,2,3]triazolo[1,5-a]pyridines 7, 2-pyridyl-[1,2,3]triazolo[1,5-a]pyrid-7-ylmethanols 11, 3-(6-substituted-2-pyridyl)-[1,2,3]triazolo[1,5-a]pyridines 12, and 7,7′-disubstituted-3,3′-[1,2,3]triazolo[1,5-a]pyridine 20, interesting polynitrogenated ligands as potential helicating compounds or luminescent sensors, from [1,2,3]triazolo[1,5-a]pyridines is described.

H2-Antihistaminika, 6. Mitt. Synthese und Wirkung N-substituierter 4-[(2-Amino-ethylmercapto)-methyl]-imidazole

1980

Es wurden die N-substituierten 4-[(2-Amino-ethylmercapto)-methyl]-imidazole 2 und 3 dargestellt und auf histaminartige Wirkung untersucht. Die Thioharnstoff- und Cyanoguanidin-Derivate von 3b zeigten keine H2-antihistaminische Wirksamkeit. H2-Antihistaminics, VI: Synthesis and Activity of N-Substituted 4-[(2-Aminoethylmercapto)methyl]imidazoles The N-substituted 4-[(2-aminoethylmercapto)methyl]imidazoles 2 and 3 were prepared and tested for their histamine-like activity. The thiourea and cyanoguanidine derivatives of 3b showed no H2-antihistaminic activity.