RESUMEN
Some new pyrazolo[3,4-d]pyrimidine derivatives have been prepared and tested for their antiviral and DNA-binding activities. Compounds 4, 5, and 6 showed high binding affinity to DNA at concentrations of 19, 27, and 28 micrograms/ml, respectively. On the other hand, compounds 6 and 10 reduced the number of viral plaques of Herpes simplex type-1 (HSV-1) by 66 and 41%, respectively. The detailed synthesis and spectroscopic and biological data are reported.
Asunto(s)
Antivirales/síntesis química , Antivirales/farmacología , ADN/metabolismo , Pirazoles/farmacología , Pirimidinas/farmacología , Animales , Antineoplásicos/síntesis química , Antineoplásicos/metabolismo , Antineoplásicos/farmacología , Antivirales/metabolismo , Afidicolina/farmacología , División Celular/efectos de los fármacos , Chlorocebus aethiops , Herpesvirus Humano 1/efectos de los fármacos , Pirazoles/síntesis química , Pirazoles/metabolismo , Pirimidinas/síntesis química , Pirimidinas/metabolismo , Células VeroRESUMEN
A series of 5-methyl-3-phenyl thiazolo[5,4-e][1,2,4]triazolo[1,5-c] pyrimidin-2-thiones and 5-methyl-3-phenyl thiazolo[5,4-e]pyrimidino[3,4-b][1,2,4]triazin-2-thiones were prepared as potential antimicrobial and antitumor agents. Some of the tested compounds showed promising activity. The detailed synthesis, spectroscopic and biological data are reported.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Pirimidinas/síntesis química , Tiazoles/síntesis química , ADN de Neoplasias/efectos de los fármacos , ADN de Neoplasias/metabolismo , Pruebas de Sensibilidad Microbiana , Pirimidinas/farmacología , Tiazoles/farmacologíaRESUMEN
A series of 5-imino-2-methyl-4-(4'-substituted phenacyl)-1,3, 4-thiadiazole derivatives 3-5 have been synthesized and further used to prepare a series of 2-methyl-6-(4'-substituted phenyl)imidazo[2, 1-b]-1,3,4-thiadiazoles 6-8 and 5-substituted-2-methyl-6-(4'-substituted phenyl) imidazo[2, 1-b]-1,3, 4-thiadiazoles 9-18. All of newly prepared imidazothiadiazole compounds were screened for their cardiotonic activity in isolated guinea pig atria. The detailed synthesis, spectroscopic and biological data are reported.
Asunto(s)
Cardiotónicos/síntesis química , Imidazoles/síntesis química , Tiadiazoles/síntesis química , Animales , Cardiotónicos/farmacología , Cobayas , Atrios Cardíacos/efectos de los fármacos , Imidazoles/farmacología , Técnicas In Vitro , Contracción Miocárdica/efectos de los fármacos , Tiadiazoles/farmacologíaRESUMEN
A number of quinazoline derivatives containing basic amine substituents at position 4, as well as new derivatives of triazolo[4,3-alpha]quinoxalines carrying basic amine or carboxylic acid moieties have been synthesized. A tetracyclic imidazotriazoloquinoxaline compound is also reported. Two of the new products (2b and 7b) exhibited good antiinflammatory activity in rats, although inferior to that of indomethacin.
