Evaluation of some 1H-pyrazole derivatives as a dual acting antimalarial and anti-leishmanial agents

The synthesis of a novel series of 1H-pyrazole derivatives was achieved by condensation of pyrazole aldehyde 1 with hydrazine hydrate to give hydrazone 7. On the other hand, cyclization of alpha, beta-unsaturated ketone counterpart 2 using hydrazine hydrate in liquid aliphatic acids rendered compounds 4-6 and hydrazine hydrate in ethanol afforded compound 3. The later was allowed to react with aroyl chloride giving rise to compounds 8, 9. All compounds were tested for their in vivo anti-malarial and in vitro antileishmanial activities. The anti-malarial activity was performed using Plasmodium berghei infected mice, while the anti-leishmanial activity of the compounds was determined against Leishmania aethiopica promastigotes using alamar blue reduction assay. Compound 3, 1-[4-methylphenyl]-3-phenyl-4-[3-[2-thienyl]-2-pyrazolin-5-yl]-1H-pyrazole, possessed the highest anti-malarial activity with suppression of 70.26%. The highest anti-leishmanial activity was exhibited by compound 2, 1-[4-methylphenyl]-3-phenyl-4-[1-[2-thienyl]-prop-2-en-1-one]-1H-pyrazole, with an IC[50] of 0.079 microg/ml. Hydrazone 7 showed appreciable dual anti-malarial [suppression = 62.30%] and anti-leishmanial activity [IC[50] = 1.823 microg/ml]

Validation of an HPLC method for the simultaneous determination of diminazene diaceturate and phenazone in injectable veterinary granules and bulk powders

A validated HPLC method for the simultaneous determination of diminazene diaceturate and phenazone has been established for the analysis of the compounds in veterinary granules for injection and in bulk powders. The compounds were separated using a Symmetry RP 18 analytical column and detected by UV absorbance at 250 nm. Linearity, accuracy as well as the intra-assay precision, inter-day precision and specificity of the method were established. The limits of detection and quantification were 3.2 and 9.7 microg mL[-1] for diminazene diaceturate and 9.57 and 28.99 microg mL[-1] for phenazone. Method had the potential to determine these drugs simultaneously from dosage forms without any interference with each other

Investigation of the fixed oil isolated from the roots of echinops kebericho mesfin

The investigation of the fixed oil of the roots of Echinops kebericho Mesfin [Family Compositae] was carried out for the first time. This study revealed the presence of the following fatty acids: Lauric myristic, myristoleic, palmitic, palmitoleic, stearic, oleic, linoleic, linolinic, arachidic and behenic acids in the saponifiable fraction. The unsaponifiable fraction was found to contain beta-sitosterol, stigmasterol, campesterol, beta-amyrin, lupeol and ursolic acid. The identification of ursolic acid was carried out by spectroscopic methods [H-NMR, 13C-NMR and MS]. The chemotaxonomic value of this study has been discussed