RESUMEN
This review article deals with the structure activity relationship (SAR) for a variety of palladacycles in biomedical applications. Moreover, the types of antibacterial, antifungal, antimycobacterial and antiprotozoal (antiamoebic and antitrypanosomal) activities will vary considerably from one country to another. Therefore, all efforts will be required to face such a vast diversity of problems. This study gives an up to date overview of the antibacterial, antifungal, antimycobacterial and antiprotozoal chemistry of the palladium group elements with an emphasis on the new strategies used in the development of new antibacterial agents. Methodologies for application of bulky aromatic or aliphatic nitrogen ligands, chiral organic moieties, chelates containing other donor atoms than nitrogen, and biologically active ligands in the design of agents analogous to palladacycles are presented. Therefore, the use of palladacycles in medicinal chemistry is interesting as potential application in the biological properties with less toxic drugs compounds..
Asunto(s)
Antiinfecciosos/química , Complejos de Coordinación/química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Quelantes/química , Complejos de Coordinación/farmacología , Diseño de Fármacos , Hongos/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Mycobacteriaceae/efectos de los fármacos , Paladio/química , Trypanosoma/efectos de los fármacosRESUMEN
Two novel series of pyrimidine derivatives have been prepared, namely; 3,6-disubstituted perhydropyrimidine-2,4-diones 8a-l as well as 3,6-disubstituted 2-thioxo-perhydropyrimidine-4-ones 9a-k. The anticancer as well antimicrobial activities of these compounds and their open-chain counterparts have been determined.
Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Pirimidinonas/síntesis química , Pirimidinonas/farmacología , Tionas/síntesis química , Tionas/farmacología , Antibacterianos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Indicadores y Reactivos , Pruebas de Sensibilidad Microbiana , Relación Estructura-Actividad , Células Tumorales CultivadasRESUMEN
Five main classes of novel pyrimidine derivatives have been synthesized; namely 6-substituted phenyl-5-cyano-3-methyl-2-phenacylhydrazino-3,4-dihydropyrimidin-4-ones 4a-e; 6-substituted phenyl-2-arylidene hydra-zino-5-cyano-3-methyl-3,4-dihydropyrimidin-4-ones 5a-i; 6-substituted phenyl-2-acylhydrazino-5-cyano-3-methyl-3,4-dihydropyrimidin-4-ones 7a-d, 8a-e and 9a-c; three novel series of 1,2,4-triazolo[4,3-a] pyrimidones 10a,b, 11a-d and 12a-d and 6-substituted phenyl-7-cyano-9-methyl-3-phenyl or 4-chlorophenyl-4,9-dihydropyrimido[2,1-c][1,2,4] triazin-8-ones 13a-c. Besides, the azide compound 2-azido-5-cyano-3-methyl-6-phenyl-3,4-dihydropyrimidin-4-one 6 was also synthesized. The prepared compounds were tested for antimicrobial and anticancer activity. Compounds 4b and 4d showed promising activity against Escherichia coli. Compounds 3c, 5c, 5e, 5g and 7b were active in the three cell line antitumor one dose primary assay and were evaluated in the 60 human tumor full panel cell line invitro screening. Compound 5c showed promising activity against all types of leukemia especially leukemia K-562 and leukemia SR with GI50 = 1.61 and 2.63 mmol/l respectively.