Browsing by Author "Ade, C.F."
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Item Synthesis and Initial Testing of Novel Antimalarial and Antitubercular Isonicotinohydrazides(Elsevier B.V., 2022) Amewu, R. K.; Ade, C.F.; Otchere, I.D.; Morgan, P.; Yeboah-Manu, D.Malaria and tuberculosis (TB) though curable and preventable, remain serious public health problems globally, with devastating consequences. Co-infection of these two deadly diseases worsens the situation and particularly makes treatment very difficult. The current mainstay for malaria treatment is gradually losing their potency due to the development of resistance. Macobacterium tuberculosis (MTB) has developed Multi-drug Resistance (MDR) and Extensive Drug Resistance (XDR) to current antitubercular drugs due to patient incompliance resulting from long treatment regimen. A small library of isonicotinohydrazide were synthesised by incorporating 1,2,4,5- tetraoxane and hydrazine moieties. Evaluation of the compounds gave antimalarial activities in the range 0.060 ± 0.033–0.491 ± 0.012 μM against 3D7 strain of Plasmodium falciparum. We assessed antimycobacterial activity of selected compounds against the standard Mycobacterium tuberculosis reference strain H37Rv and M. aurum (a non-tuberculous mycobacteria) using the microplate Alamar blue (MABA) assay and found four compounds to be very potent against H37Rv but largely inactive against Macobacterium aurum. We followed up to estimate the minimum inhibitory concentrations of these active compounds and tested them against clinical M. tuberculosis strains resistant to isoniazid (INH) and rifampicin (RIF). The MICs of the active compounds against H37Rv were between 0.003 and 0.5 mg/mL however, they were largely inactive against drug resistant clinical strains except for the INH mono-resistant resistant strain which was very active with compounds 5 and 8 possessing MICs of 0.125 mg/mL.Item Synthesis of Novel Antimalarial and Antitubercular Isonicotinohydrazides(University Of Ghana, 2018-11) Ade, C.F.Malaria and tuberculosis (TB) though curable and preventable, remain serious public health problems globally, with devastating consequences. Co-infection of these two deadly diseases worsens the situation and particularly makes treatment very difficult. While the current mainstay for malaria treatment, artemisinins, may gradually lose their potency due to the development of resistance by P. falciparum, M. tuberculosis has developed Multi-Drug Resistance (MDR) and Extensive Drug Resistance (XDR) to current anti-TB drugs, due to patient incompliance resulting from long treatment regimen. This project focused on the synthesis of isonicotinohydrazides with the concept of molecular hybridisation, by incorporating 1,2,4,5- tetraoxane and hydrazine moieties to yield a single molecule that will exhibit both antimalarial and antitubercular activites. In all, ten novel hybrid molecules were designed, synthesised and characterised using FTIR, 1H and 13C NMR spectroscopy. All the compounds returned acceptable physicochemical parameters as well as good antimalarial activities against 3D7 strain of P. falciparum. In vitro IC50 values ranging from 0.060 ± 0.033 - 0.491 ± 0.012 μM were obtained. Five of the hybrid molecules tested against H37rv and M. aurum strains of Mtb using Microplate Alamar Blue Assay (MABA), gave satisfactory results while four of the compounds 101, 102, 103, 104, exhibited very good activity against H37rv with MIC values between 0.003-0.5 mg/mL, and M. aurum was resistant to all five tested compounds.