Synthesis, Characterization, Theoretical Treatment and Antitubercular activity Evaluation of (E)-N’- (2,5-dimethoxylbenzylidene)nicotinohydrazide and some of its Transition Metal Complexes against Mycobacterium tuberculosis, H37Rv

(E)-N’-(2,5-dimethoxylbenzylidene)nicotinohydrazide) (HL) was synthesized by condensing nicotinic acid hydrazide and 2,5-dimethoxylbenzaldehyde with ONO coordination pattern. The structure of the hydrazone was elucidated by using CHN analyzer, ESI mass spectrometry, IR, 1H NMR, 13C NMR and 2D NMR (COSY and HSQC). The hydrazone was used to synthesized five metal complexes [Mo(V), VO(II), Mn(II) Ni(II) and Cu(II)] which were characterized by several physicochemical methods, namely elemental analysis, electronic spectra, infrared, EPR, molar conductivity and magnetic susceptibility measurements. An octahedral geometry was suggested for Mo(V), Ni(II) and Cu(II) complexes while tetrahedral was proposed for Mn(II) complex. VO(II) complex conformed with tetrahedral pyramidal. Structural geometries of these compounds were also suggested in gas phase by using Hyper Chem-8 program for the molecular mechanics and semi-empirical calculations. The energy (E) and eV for homo and lumo state for the prepared compounds were calculated by using PM3 method. In vitro antimycobacterial activity study of the compounds was evaluated against Mycobacterium tuberculosis, H37Rv, by using micro-diluted method. Some of the metal complexes displayed higher activity than the ligand (HL) and isoniazid (INH).Also some of the complexes showed moderate activity when compared to isoniazid. Generally, the results obtained revealed that the compounds exhibited promising antitubercular activity. However, the metal complexes were found to be more toxic than isoniazid drug

Synthesis of (E) -N'-(5-bromo 2-hydroxybenzylidene)nicotinohydrazide) and its Pt(II), Zn(II), Mn(II), Ni(II) and Mo(V) Complexes as potential Anti-tubercular agent

The cold condensation reaction of nicotinic acid hydrazide and 5-bromo-2-hydroxybenzaldehyde to form a tridentate Schiff base hydrazone ligand, (H2L3) was studied. The prepared ligand was characterized using CHN analyzer, ESI mass spectrometery, IR, 1H NMR,13C NMR, and 2D NMR such as COSY and HSQC. Therafter, five novel complexes [Pt(II), Zn(II), Mn(II), Ni(II) and Mo(V) of the hydrazone ligand were synthesized and characterized based on conductivity measurements,CHN analysis, AAS, magnetic measurement, UV/Vis, IR, ESR and TGA/DTA study. The proposed structures of the metal complexes were further supported through the use of powder X-ray analysis. The tubercular activity study of the compounds was evaluated against Mycobacterium tuberculosis, H37Rv by using micro- diluted method. The study revealed that H2L3 exhibited promising anti-tubercular activity with MIC value of 0.82 µg/mL. Also, metal complexes (Pt(H2L3)Cl)- 0.88 µg/mL, [Mn(H2L3)(CH3COO)2]-0.78 µg/mL, [Zn[H2L3)(CH3COO)2H2O]-0.62 µg/mL and [Ni(H2L3)Cl2]H2O-1.19 µg/mL exhibited significant inhibition as compared to the standard drug (isoniazid-0.91 µg/mL). Complexes 2 and 3 with coordinated acetates showed two-folds inhibition than standard isoniazid drug. However, complex 5 with coordinated chlorine atom displayed lower inhibition when compared to isoniazid

PHYSICO-CHEMICAL CHARACTERISTICS OF INDUSTRIAL EFFLUENTS IN LAGOS STATE, NIGERIA

The discharge of industrially polluted effluents into municipal drains in a populated and commercially vibrant state of Lagos, Nigeria stands to pose deleterious environmental threats. The aim of this study is to ascertain the inhibitive contributions of these industrial effluents even as they flow from municipal drains into the sink (River or Lagoon). Analysis such as pH, temperature, conductivity, Total Solids (TS), Dissolved Oxygen (DO), Biological Oxygen Demand (BOD), Chemical Oxygen Demand (COD), Oil/Grease and Heavy metal determination using Atomic Absorption Spectrophotometer (Spectra AA Varian 400 plus) were carried out. Five industrial effluents discharged at point sources were collected and analysed. The 1.36-4.91 pH range does not conform to the guide line stipulated by Federal Environmental Protection Agency (FEPA). Sample A and E have the highest microbial load which reflects in their high BOD5 as well as COD values. Unprecedented 10.54 mg/L Cd concentration in effluent B is highly unacceptable by FEPA and World Health Organisation (WHO). This study anchors on the need for treatment of industrial effluent before they are discharged into the environment

(E)-N'-(2, 4-dihydroxybenzylidene)nicotinohydrazide and its Metal Complexes: Synthesis, Characterisation and Antitubercular Activity

Nicotinic acid hydrazide and 2,4-dihydoxylbenzaldehyde were condensed at 20 °C to form an acylhydrazone (H3L1) with ONO coordination pattern. The structure of the acylhydrazone was elucidated by using CHN analyzer, ESI mass spectrometry, IR, 1H NMR, 13C NMR and 2D NMR such as COSY and HSQC. Thereafter, five novel metal complexes [Mn(II), Fe(II), Pt(II) Zn(II) and Pd(II)] of the hydrazone ligand were synthesized and their structural characterization were achieved by several physicochemical methods namely: elemental analysis, electronic spectra, infrared, EPR, molar conductivity and powder X-ray diffraction studies. An octahedral geometry was suggested for both Pd(II) and Zn(II) complexes while both Mn(II) and Fe(II) complexes conformed with tetrahedral pyramidal. However, Pt(II) complex agreed with tetrahedral geometry. In vitro antitubercular activity study of the ligand and the metal complexes were evaluated against Mycobacterium tuberculosis, H37Rv, by using micro-diluted method. The results obtained revealed that (PtL1) (MIC = 0.56 mg/mL), (ZnL1) (MIC = 0.61 mg/mL), (MnL1) (MIC = 0.71 mg/mL) and (FeL1) (MIC = 0.82 mg/mL), exhibited a significant activity when compared with first line drugs such as isoniazid (INH) (MIC = 0.9 mg/mL). H3L1 exhibited lesser antitubercular activity with MIC value of 1.02 mg/mL. However, the metal complexes displayed higher cytotoxicity but were found to be non-significant different (P > 0.05) to isoniazid drug

Synthesis of Silver Nanoparticles by Plant-Mediated Green Method: Optical and Biological Properties

In this study, silver nanoparticles (Ag NPs) were successfully synthesized by plant-mediated green route. The leaf extracts of locally sourced Canna indica and Senna occidentalis acted as the reducing agents/capping agents instead of toxic chemicals leading to unprecedented bioreduction which promoted nucleation and particle growth within 2 minutes of reaction. Optical measurements were characterized by high intensities of absorption revealed by narrow absorption peaks indicating confinement of excitons, with surface Plasmon resonance (SPR) bands of silver nanoparticles at 340–380 nm (S. occidentalis-stabilized Ag NPs) and 400–430 nm (C. indica-stabilized Ag NPs). Morphological characterization with scanning electron microscope coupled with energy dispersed spectrometer (SEM-EDS) and transmission electron microscope (TEM) revealed quasi-spherical, cubic and truncated edge Ag NPs with mean sizes of 9_10±1_12 nm and 9_4±1_95 nm. Formation of crystalline Ag NPs was also supported by X-ray diffraction (XRD) pattern and selected area electron diffraction (SAED) showing peak broadening. FTIR analysis revealed some characteristic vibrational bands of O–H, C O, C N functional groups at 3306, 1647 and 1246 cm−1 respectively in the organically capped silver nanoparticles. The mechanism of reaction in both syntheses was considered to be diffusion controlled Ostwald ripening process. The antimicrobial activity of the synthesized nanoparticles was tested against clinically isolated Gram positive bacteria: Staphylococcus aureus, Streptococcus pyogenes and clinically isolated fungus-Candida albicans. Significant growth inhibitions were found using analysis of variance (ANOVA), SPSS statistical tool at P <0_05. The highest activity of C. indica-synthesized Ag NPs was against C. albicans, while S. occidentalis derived Ag nanoparticles were most active against S. aureus and S. pyogenes. Hence, the findings of this research suggest potential applications of the bionanoparticles as optical materials, electronically conductive adhesives (ECA), and as a candidate for therapeutic drugs because of their biogenic nature

SYNTHESIS, ANTIBACTERIAL AND TOXICOLOGY STUDY OF MN(II), CO(II) AND NI(II) METAL COMPLEXES OF SULFADOXINE MIXED WITH PYRIMETHAMINE

Three mixed ligand metal complexes of Sulphadoxine and Pyrimethamine were prepared by using Mn(II), Ni(II) and Co(II) metal chloride hexahydrate and characterized by elemental analysis, molar conductivity, magnetic susceptibility measurement, AAS, IR and UV-Vis. spectroscopy. Some physical parameters were obtained using molar conductance measurement and melting point determination. Based on the analytical and spectroscopic data, the complexes were proposed to have the formulae: [ML1L2](Cl)2 (where M = Mn(II), Ni(II) and Co(II); L1 = sulphadoxine, L2 = pyrimethamine). The spectroscopic data proposed that L1 and L2 coordinated through N of NH2 groups in L1 and through N atom of NH group in L2. Thus, pyramethamine was proposed to be a tridentate ligand, while sulphadoxine was proposed to be a monodentate ligand. Micro-analysis further supported the proposed structure for the complexes. The antibacterial activity of the metal complexes were compared with their ligands by screening them against isolates of some strains of g(-) Escherichia coli, g(+) Proteus sp., g(+) Pseudomonas aureginosa and Salmonella typhi by using diffusion method. The results obtained showed the metal complexes to be more potent antibacterial than the parent drugs against the four species used. Toxicology tests against some tissues of albino rat (Rattus novergicuss) revealed toxicity of the complexes in the kidney as compared to the parent drugs. However, ALP values for metal complexes were found to be non-significantly different from the ALP values obtained for livers and the sera. This indicates that the metal complexes are not excessively toxic

Comparative Study of the Antibacterial Activity of N, N-Diethylamido Substituted p-Toluenesulfonamides to their α-Toluenesulfonamide Counterparts

Reaction of p-toluenesulfonyl chloride with amino acids gave sulfonamides p-T1a-k which upon amidation afforded p-T2a-k. Similarly, treatment involving α-toluenesulfonyl chloride and amino acids afforded the sulfonamides α-T1a-k. These two classes of sulfonamides were synthetically modified at their COOH end position to achieve N,N-diethylamido substituted p-toluenesulfonamides p-T2a-k and α-toluenesulfonamides α-T2a-k, respectively. The chemical structures of the compounds were validated with IR, Mass spectra, NMR as well as elemental analytical data. Both classes of compounds were screened against Escherichia coli and Staphylococcus aureus and their activity were compared. It was remarkable to note that the α-toluene sulfonamides α-T2a-k were more active than their p-toluenesulfonamide counterparts p-T2a-k. Compound 1-(benzylsulfonyl)-N,Ndiethylpyrrolidine-2-carboxamide α-T2a was the most potent antibacterial compound on S. aureus with MIC value of 3.12 μg mLG1 while N,N-Diethyl-3- phenyl-2-(phenylmethylsulfonamide) propanamide α-T2j emerged as the best antibacterial motif against E. coli with MIC value of 12.5 μg mLG1. Hence, these compounds especially the α-toluenesulfonamide core structural templates are good candidates for further study for future drug discovery