DESIGN AND SYNTHESIS OF BENZODIAZEPINES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE AND INDOLE MOIETIES AS A POTENT ANTIMICROBIAL AND ANTIOXIDANT AGENTS

  Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives, namely, 2-((1H-benzo[d] imidazol-2-yl) thio)-N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl) acetamide 3a-d, N-(4-(4-(1H-indol-3-yl)-8-methyl- 1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-((5-methoxy-1H-benzo[d]imidazol-2-yl) thio) acetamide 4a-d and N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-(benzo[d]thiazol-2-ylthio) acetamide 5a-d.Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity (RSA), ferric ions (Fe3+) reducing antioxidant power (FRAP), and ferrous (Fe2+) metal ion chelating activity.Result: The structures of all the newly synthesized compounds were characterized by their infrared,1H nuclear magnetic resonance, mass spectral studies, and elemental analysis. Compounds 7a and 7b exhibited good RSA at a concentration 100 μg/ml, compounds 6d, 7a-d and 8a-c displayed good FRAP at a concentration 100 μg/ml, compounds 7b-d and 8b-d showed good Fe2+ ion metal chelating activity. Compounds 6b, 6d, 7a-d, and 8a-d exhibited good activity against all the screened bacteria and fungi.Conclusion: Some of the compounds have shown potent antimicrobial activity against all the screened bacteria and fungi, and some have exhibited very good antioxidant activity.</jats:p

DESIGN AND SYNTHESIS OF BENZODIAZEPINES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE AND INDOLE MOIETIES AS A POTENT ANTIMICROBIAL AND ANTIOXIDANT AGENTS

  Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives, namely, 2-((1H-benzo[d] imidazol-2-yl) thio)-N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl) acetamide 3a-d, N-(4-(4-(1H-indol-3-yl)-8-methyl- 1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-((5-methoxy-1H-benzo[d]imidazol-2-yl) thio) acetamide 4a-d and N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-(benzo[d]thiazol-2-ylthio) acetamide 5a-d.Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity (RSA), ferric ions (Fe3+) reducing antioxidant power (FRAP), and ferrous (Fe2+) metal ion chelating activity.Result: The structures of all the newly synthesized compounds were characterized by their infrared,1H nuclear magnetic resonance, mass spectral studies, and elemental analysis. Compounds 7a and 7b exhibited good RSA at a concentration 100 μg/ml, compounds 6d, 7a-d and 8a-c displayed good FRAP at a concentration 100 μg/ml, compounds 7b-d and 8b-d showed good Fe2+ ion metal chelating activity. Compounds 6b, 6d, 7a-d, and 8a-d exhibited good activity against all the screened bacteria and fungi.Conclusion: Some of the compounds have shown potent antimicrobial activity against all the screened bacteria and fungi, and some have exhibited very good antioxidant activity

DESIGN AND SYNTHESIS OF BENZODIAZEPINES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE AND INDOLE MOIETIES AS A POTENT ANTIMICROBIAL AND ANTIOXIDANT AGENTS

  Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives, namely, 2-((1H-benzo[d] imidazol-2-yl) thio)-N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl) acetamide 3a-d, N-(4-(4-(1H-indol-3-yl)-8-methyl- 1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-((5-methoxy-1H-benzo[d]imidazol-2-yl) thio) acetamide 4a-d and N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-(benzo[d]thiazol-2-ylthio) acetamide 5a-d.Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity (RSA), ferric ions (Fe3+) reducing antioxidant power (FRAP), and ferrous (Fe2+) metal ion chelating activity.Result: The structures of all the newly synthesized compounds were characterized by their infrared,1H nuclear magnetic resonance, mass spectral studies, and elemental analysis. Compounds 7a and 7b exhibited good RSA at a concentration 100 μg/ml, compounds 6d, 7a-d and 8a-c displayed good FRAP at a concentration 100 μg/ml, compounds 7b-d and 8b-d showed good Fe2+ ion metal chelating activity. Compounds 6b, 6d, 7a-d, and 8a-d exhibited good activity against all the screened bacteria and fungi.Conclusion: Some of the compounds have shown potent antimicrobial activity against all the screened bacteria and fungi, and some have exhibited very good antioxidant activity

Physical mapping of ribosomal DNA and genome size in diploid and polyploid North African Calligonum species (Polygonaceae)

38 p., tablas, gráf.Most Calligonum species are desert plants, characteristic of the Saharan bioclimatic region. All species karyologically analyzed until present have the basic chromosome number x = 9 and comprise diploids, triploids and tetraploids. The Tunisian flora comprises diploid Calligonum arich and C. azel, of restricted distribution, and the tetraploid C. comosum with wider distribution. Analyses of their karyotypes and polyploidisation-linked rDNA changes by orcein staining, fluorochrome banding with chromomycin A3 and fluorescent in situ hybridisation with 5S and 26S ribosomal DNA probes have been performed. We report the chromosome number for Calligonum arich (2n = 18) as well as the diploid level for C. comosum for the first time. Chromosome counts have also verified the earlier described tetraploid cytotype (2n = 36) of C. comosum. A general pattern of six GC-rich bands as well as two 35S sites and four 5S sites is described for Calligonum species at the diploid level although there is intraspecific variation regarding the site number in a second type of C. comosum, with one pair of 35S rDNA sites and two pairs of 5S rDNA sites. The tetraploid cytotype of C. comosum has undergone locus loss and genome downsizing. Genome size assessments confirmed previous data. Nonetheless, statistically significant differences were found depending on the type of tissue used for estimation. Measurements from seeds had always larger values than from leaves. The presence of cytosolic compounds in leaves, interfering with DNA staining, is discussed as a possible cause of the differences.This work was supported by the Dirección General de Investigación Científica y Técnica, government of Spain (CGL2010-22234-C02-01/BOS and CGL2010-22234-C02-02/BOS) and the Generalitat de Catalunya, government of Catalonia (‘‘Ajuts a grups de recerca consolidats’’, 2009SGR0439). SG and OH benefitted from Juan de la Cierva postdoctoral contracts of the Ministry of Economy and Competitiveness, government of Spain.Peer reviewe