A facile synthesis of 2-aryl-4,5-di(2-thienyl)imidazoles under microwave irradiation and their antimicrobial activities.

In this study, some 2-aryl-4,5-dithienylimidazoles were synthesized by reacting di-(2-thienyl)ethandione and a suitable aromatic aldehyde in the presence of ammonium acetate in acetic acid. Either the classical reflux method or microwave irradiation method were applied as alternative reaction conditions. The antimicrobial activities of the compounds obtained were investigated in vitro and appreciable activities were obtained.

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

New 4-(aroyloxyalkanoyl)-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one s (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.

Synthesis and antimicrobial activities of some 3-arylamino-5-[2-(substituted 1-imidazolyl)ethyl]-1,2,4-triazole derivatives.

In this study, some 3-arylamino-5-[2-(substituted imidazol-1-yl or benzimidazol-1-yl)ethyl]-1,2,4-triazole derivatives were synthesised by reacting 3-(substituted imidazol-1-yl)propionyl hydrazides, with S-methyl-N'-arylisothiouronium iodide salts. Their structures were elucidated by IR, 1H-NMR and mass spectroscopic data and elemental analyses results. Antimicrobial activities of the compounds were observed against Staphylococcus aureus NRRL B-767, Micrococcus luteus NRRL B-4375, Escherichia coli B, Pseudomonas aeroginosa NRRL B-23 and the fungi Candida albicans and Candida glabrata by using the tube dilution technique. Remarkable activity was obtained.

Synthesis of some 3-arylamino-5-aryloxymethyl[1,2,4]triazole derivatives and their antimicrobial activity.

In this study, some 3-arylamino-5-aryloxymethyl[1,2,4]triazole derivatives were synthesized by reacting S-methyl-N'-arylisothiouronium iodide and 2-(aryloxy)alkanoic acid hydrazide. The structural elucidation of the compounds was performed by IR, 1H-NMR and MS spectroscopic data and elemental analyses results. Antibacterial and antifungal activities of the compounds were examined.

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.

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.

Some 3-hydrazono-2-indolinones and N-Mannich bases as potential anticonvulsants.

In this study a new series of 3-aryloxy/arylthioxyacetylhydrazono-2-indolinones obtained by condensation of isatin with aryloxy/arythioxyacetylhydrazines were treated with morpholine and formaldehyde to yield 1-morpholinomethyl-3-aryloxy/arylthioxyacetylhydrazono-2- indolinones. Structures of all the compounds were assigned on the basis of spectral data (UV, IR, 1H-NMR, EIMS) and elemental analyses. Anticonvulsant evaluation of the compounds revealed varying degrees of activity against pentylenentetrazole induced seizures.

[Synthesis of certain derivatives of 5-methoxy-3-[(benzazole-2-yl) thioacetylamino]-2,3-dihydrobenzofuran and research on their antihypertensive activities]. / Synthèse de quelques dérivés de méthoxy-5 [(benzazole-2-yl)thioacétylamino]-3 dihydro-2,3 benzofuranne et recherche d'activité antihypertensive.

In this study, some 5-methoxy-3-[(benzazole-2-yl)thioacetylamino]-2, 3-dihydrobenzofuran derivatives were synthesized and their structures were elucidated by IR, NMR and microanalyses. The antihypertensive activities of the compounds obtained were investigated.

Synthesis of some pyrido- and pyrazino-benzimidazole derivatives and their antifungal activity.

Some 2-aryl-4-hydroxypyrido[1,2-a]benzimidazole and 1-substituted 3-arylpyrazino-[1,2-a]benzimidazole derivatives were synthesized using 1-(2-arylethan-2-on)-2-acylbenzimidazole derivatives as starting materials. Antifungal activities of the compounds obtained were examined in vitro.

Synthesis of some 2-[(benzazole-2-yl)thoiacetyl]phenol derivatives and preliminary investigation on their vasodilatory activity.

Some 2-[(benzazol-2-yl)thioacetyl]phenol derivatives were synthesized and their structures were elucidated by IR, NMR and microanalyses. The vasodilatory activity of the obtained compounds was investigated.

[Synthesis of certain derivatives of methoxy-5-[(benzazole-2-yl)thioacetylamino]-3-dihydro-2,3-benzofuran and research on their antihypertensive activity]. / Synthèse de certains derivès de methoxy-5 [(benzazole-2-yl) thioacetylamino]-3 dihydro-2,3 benzofurane et recherche d'activité antihypertensive.

In this study, some 5-methoxy-3-[benzazole-2-yl)thioacetylamino]-2,3-dihydrobenzofuran derivatives were synthesized and their structures were elucidated by IR, NMR and microanalyses. The antihypertensive activities of the compounds obtained were investigated.

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.

Some nitroimidazole derivatives as possible antibacterial agents.

In this study, six 1-[2(benzazol-2-yl)thioethyl]-2-methyl-5- nitroimidazole derivatives were synthesized. Antibacterial activities of the compounds obtained were examined and it was found that they are effective against aerobe bacteria.

Synthesis of some new hydrazide-hydrazones, thiosemicarbazides, thiadiazoles, triazoles and their derivatives as possible antimicrobials.

The title compounds were prepared by reacting [(4,5-diphenyl-1H-imidazol-2-yl)thio]acetic acid hydrazides 6 and 7 with aromatic aldehydes to give the corresponding hydrazones 6a-m and 7a-d or with isothiocyanates to afford the corresponding thiosemicarbazides 8a-c and 9. 8a-c and 9 were cyclized into triazoline-5-thiones 10a-c and 11 in the presence of sodium hydroxide or into 1,3,4-thiadiazoles 14a-c and 15 in the presence of sulfuric acid. On the other hand, 10c and 11 were also reacted with alkyl halides to obtain their thioether derivatives, 12a,b and 13. All the synthesized compounds were characterized by their elementary analysis and by using UV, IR, NMR and mass spectrometry. 6b, c, f, h-k, m, 7, 7d, 8c, 9, 10c, 11, 12a-b, 13, 14 and 15 were tested for antimicrobial activity, but no significant activity was observed.