Square wave adsorptive stripping voltammetric (SQWASV) method has been utilized to confirm and elucidate the possible complexation reaction between pantoprazole sodium and cobalt as a transition metal in Britton- Robinson buffer (pH=7.0). The current signal due to the oxidation process was a function of the amount of pantoprazole sodium, pH of the medium, cobalt concentration and accumulation time at the electrode surface. The oxidation peak current has varied linearly with the concentration over the range of 0.1–9.0 nM. The limit of detection was found to be 0.04 nM. The validity of the method was successfully applied for the determination of pantoprazole sodium in pharmaceutical formulations with a pharmacokinetic study in rabbit plasma. The simplicity, rapidity, sensitivity and selectivity of this method make it a very attractive alternative to the other existing methods in the quality control laboratories.

Square wave adsorptive stripping voltammetric (SQWASV) method has been utilized to confirm and elucidate the possible complexation reaction between pantoprazole sodium and cobalt as a transition metal in Britton- Robinson buffer (pH=7.0). The current signal due to the oxidation process was a function of the amount of pantoprazole sodium, pH of the medium, cobalt concentration and accumulation time at the electrode surface. The oxidation peak current has varied linearly with the concentration over the range of 0.1–9.0 nM. The limit of detection was found to be 0.04 nM. The validity of the method was successfully applied for the determination of pantoprazole sodium in pharmaceutical formulations with a pharmacokinetic study in rabbit plasma. The simplicity, rapidity, sensitivity and selectivity of this method make it a very attractive alternative to the other existing methods in the quality control laboratories.

New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against hepatitis C virus (HCV) and hepatitis B virus (HBV). Their cytotoxicity was determined by the reduction in the number of viable cell. All of the synthesized compounds are inactive against HBV and some showed activity against HCV. In particular, two compounds showed significant activity, 2-{4-[(1-benzoylbenzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitro-phenyl)-acetamide (13) and 2-(4-{[1-(p-chlorobenzoyl)-benzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitrophenyl)-acetamide (17). The results give an insight into the importance of the substituent at position 2 of benzimidazole for the inhibition of HCV.

New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against hepatitis C virus (HCV) and hepatitis B virus (HBV). Their cytotoxicity was determined by the reduction in the number of viable cell. All of the synthesized compounds are inactive against HBV and some showed activity against HCV. In particular, two compounds showed significant activity, 2-{4-[(1-benzoylbenzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitro-phenyl)-acetamide (13) and 2-(4-{[1-(p-chlorobenzoyl)-benzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitrophenyl)-acetamide (17). The results give an insight into the importance of the substituent at position 2 of benzimidazole for the inhibition of HCV.

6-Chloro-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (1) was utilized as key intermediate for the synthesis of new 6-amino derivatives (2-17) by heating with a number of aliphatic amines. Heating 1 with aromatic amines under similar conditions failed to give the corresponding amino derivatives. The new compounds were fully characterized and some of them were preliminary screened for anticancer, COX inhibition and antimicrobial activities. The compounds are not cytotoxic and some of them are potent and selective COX-2 inhibitors. In particular compound 6-benzylamino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) with IC50 = 0.11 μM and SI = 33 for COX-2. 6-Hexylamino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (6) exhibited antifungual and antibacterial activities (Gram -ve) comparable to the reference drugs. The results show clearly that the natur of N-substituent significanlty affect the biological activity.

6-Chloro-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (1) was utilized as key intermediate for the synthesis of new 6-amino derivatives (2-17) by heating with a number of aliphatic amines. Heating 1 with aromatic amines under similar conditions failed to give the corresponding amino derivatives. The new compounds were fully characterized and some of them were preliminary screened for anticancer, COX inhibition and antimicrobial activities. The compounds are not cytotoxic and some of them are potent and selective COX-2 inhibitors. In particular compound 6-benzylamino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) with IC50 = 0.11 μM and SI = 33 for COX-2. 6-Hexylamino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (6) exhibited antifungual and antibacterial activities (Gram -ve) comparable to the reference drugs. The results show clearly that the natur of N-substituent significanlty affect the biological activity.

Pencil graphite electrode was success-fully modified with a thin film of poly (eriochrome black T) and applied for the sensitive and selective voltammetric simultaneous determination of pantoprazole sodium and domperidone in a binary mixture. The preparation and basic electrochemical behavior of poly (eriochrome black T) film on the Pencil graphite electrode were investigated. The modified electrode has exhibited very high electro-catalytic activity towards the cited mixture. The anodic peaks of the both species were well defined with enhanced oxidation peak currents. Under the optimum conditions, the linearity ranges were 0.4–55 ×10−7 M and 0.1–34 × 10−7 M for pantoprazole sodium and domperidone, respectively with detection limits of 0.12 × 10−7 M and 0.04 × 10−7 M for pantoprazole sodium and domperidone, respectively. The proposed sensor has been successfully applied in the analysis of pantoprazole sodium and domperidone in synthetic binary mixtures and human serum.

Pencil graphite electrode was success-fully modified with a thin film of poly (eriochrome black T) and applied for the sensitive and selective voltammetric simultaneous determination of pantoprazole sodium and domperidone in a binary mixture. The preparation and basic electrochemical behavior of poly (eriochrome black T) film on the Pencil graphite electrode were investigated. The modified electrode has exhibited very high electro-catalytic activity towards the cited mixture. The anodic peaks of the both species were well defined with enhanced oxidation peak currents. Under the optimum conditions, the linearity ranges were 0.4–55 ×10−7 M and 0.1–34 × 10−7 M for pantoprazole sodium and domperidone, respectively with detection limits of 0.12 × 10−7 M and 0.04 × 10−7 M for pantoprazole sodium and domperidone, respectively. The proposed sensor has been successfully applied in the analysis of pantoprazole sodium and domperidone in synthetic binary mixtures and human serum.

Pencil graphite electrode was success-fully modified with a thin film of poly (eriochrome black T) and applied for the sensitive and selective voltammetric simultaneous determination of pantoprazole sodium and domperidone in a binary mixture. The preparation and basic electrochemical behavior of poly (eriochrome black T) film on the Pencil graphite electrode were investigated. The modified electrode has exhibited very high electro-catalytic activity towards the cited mixture. The anodic peaks of the both species were well defined with enhanced oxidation peak currents. Under the optimum conditions, the linearity ranges were 0.4–55 ×10−7 M and 0.1–34 × 10−7 M for pantoprazole sodium and domperidone, respectively with detection limits of 0.12 × 10−7 M and 0.04 × 10−7 M for pantoprazole sodium and domperidone, respectively. The proposed sensor has been successfully applied in the analysis of pantoprazole sodium and domperidone in synthetic binary mixtures and human serum.

The antitubercular drug; para-aminosalicylic acid (PAS) was used as the core scaffold for the design of a series of 1H-1,2,3-triazolylsalicylhydrazones upon coupling with triazole and arylhydrazone moietis to furnish a single molecular architecture. The obtained derivatives were screened against Mycobacterium tuberculosis H37Rv revealing good to high activity for the active compounds (MIC values of 0.39–1.5 µg/mL) compared to the marketed drugs isoniazid, rifampicin and ethambutol. Moreover, the most active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potent than PAS and equipotent to rifampicin (MIC 0.39 µg/mL), while exhibiting low cytotoxicity with a selectivity index of >128. In addition, this compound was shown to be active against persistent forms of mycobacteria comparable to standard drugs in nutrient starvation model. Accordingly, we introduce compound 20 as a valuable lead for further development. A 3D-QSAR study was also conducted to help in explaining the observed activity and to serve as a tool for further development.