Synthesis and antibacterial activities of some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives

In this study, some 1-[2-(substituted pyrrol-1-yl)ethyl]-2-methyl-5-nitroimidazole derivatives were synthesized by reacting 2-(2-methyl-5-nitro-1H-imidazolyl)ethylamine dihydrochloride, which was prepared using metronidazole, with some 1,4-dicarbonyl compounds. The structure elucidation of the compounds was performed by IR, H-1-NMR and mass spectroscopic data and elemental analysis results. Antimicrobial activities of the compounds were examined and notable activity was obtained. (C) Elsevier, Paris

Spectroscopic determination of acid dissociation constants of some biologically active 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives

WOS: 000179368500015The acid dissociation constants, pK(a), of twelve biologically active 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives were determined using spectroscopic techniques. Elucidation of the structure-reactivity relationships was attempted from structural considerations based on the acid dissociation constants

Some 1-substituted 3-aryl-1,4-dihydro-1,2,4-triazino[4,3-a]- benzimidazoles and their vasodilatory activities

In this study, some 1-substituted 3-aryl-1,4-dihydro-1,2,4- triazino[4,3-a]benzimidazole derivatives were synthesized, their structures were elucidated, and their vasodilatory activities were examined. It was found that the compounds under investigation showed appreciable vasodilatory activity

A theoretical approach to acidity-basicity behaviour of some biologically active 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives

Symposium on Role of Chemistry in the Evolution of Molecular Medicine -- JUN 27-29, 2003 -- UNIV SZEGED, SZEGED, HUNGARYWOS: 000188928800067The acid dissociation constants, pK(a) values, of 12 biologically active 6-[p- or p- and m-substituted] phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives were computed using semi-empirical methods. Correlations between the experimental and computed acid dissociations constants were found to be satisfactory

Quinazolinones, XVII1): Synthesis and Pharmacological Activities of Some Antipyryloxoalkylthioquinazolinones

PubMed: 2288484Chinazolinone, 17. Mitt.1): Synthese und pharmakologische Wirksamkeit einiger Antipyryloxoalkylthiochinazolinone Copyright © 1990 WILEY-VCH Verlag GmbH & Co. KGaA, Weinhei

Synthesis and vasodilatory activity of some thiazolo-triazole derivative

In this study, some thiazolo[3,2-b]-1,2,4-triazole derivatives were synthesized. Their vasodilatory activities were examined in vitro. All examined compounds showed appreciable activity

Synthesis of some 1-(2-arylvinyl)-3-arylpyrazino[1,2-a]benzimidazole derivatives and their antimicrobial activities

Some 1-(2-arylvinyl)-3-arylhyrazino[1,2-a] benzimidazole derivatives were synthesized, their structures were elucidated, and their antibacterial and antifungal activities were examined. None of the compounds proved to be sufficiently active

Synthesis and preliminary evaluation of new 5-pyrazolinone derivatives as analgesic agents

New 4-(aroyloxyalkanoyl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-ones (5) were cyclized to 4-(2-aryl-5-unsubstituted/substituted oxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-ones (6) employing the Davidson procedure. Preliminary evaluation of analgesic activity revealed that the effect of 4-(2-phenyl-5-ethyloxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-chlorophenyl)-5-ethyloxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazoline-5-one on acetic acid induced writhing was superior to that of antypyrine and aminopyrine. 4-[2-(4-Chlorophenyl)-5-methyloxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-methoxyphenyl)-5-ethyloxazol-4-yl]-2,3- dimethyl-1-phenyl-3-pyrazolin-5-one were more potent than aminopyrine, whereas 4-(2-phenyl-5-methyloxazol-4-yl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one and 4-[2-(4-methoxyphenyl)-5-methyl-oxazol-4-yl]-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one were not as active (modified Koster's Test; 0.19-0.21 mmol.kg(-1)). None of the selected entries showed inhibition of formaldehyde-induced paw oedema. (C) 2000 Editions scientifiques et medicales Elsevier SAS

Synthesis and vasodilatory activity of some thiazolo-triazole derivative

PubMed: 8343214In this study, some thiazolo[3,2-b]-1,2,4-triazole derivatives were synthesized. Their vasodilatory activities were examined in vitro. All examined compounds showed appreciable activity