With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC₅₀ values of 4.09 and 5.11 µM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.

Compounds containing arylpyrrole‐, 1,2,4‐triazole‐ and hydrazone structural frameworks have been widely studied and demonstrated to exhibit a wide range of pharmacological properties. Herein, an exploratory series of new 1,2,4‐triazole derivatives designed by amalgamation of arylpyrrole and 1,2,4‐triazole structural units via a hydrazone linkage is reported. The synthesised compounds were tested in vitro for their potential activity against Mycobacterium tuberculosis (MTB) H₃₇Rv strain. The most promising compound 13 – the derivative without the benzene ring appended to the pyrrole unit displayed acceptable activity (MIC₉₀=3.99 μM) against MTB H₃₇Rv, while other compounds from the series exhibited modest to weak antimycobacterial activity with MIC₉₀ values in the range between 7.0 and >125 μM. Furthermore, in silico results, predicated using the SwissADME web tool, show that the prepared compounds display desirable ADME profile with parameters within acceptable range.

Objective: Persea americana is a popular plant that is well known for its fruit, which is highly consumed due to its nutritional and medicinal values. The rich secondary metabolites content of P. americana creates an opportunity to utilize it as a functional food or standardized herbal preparations. The quality of a medicinal plant is determined by the active substances produced by the plant. Therefore, the purpose of the present study is to determine the secondary metabolites present in P. americana grown in uncultivated farmland in Ogbomoso, Oyo State Nigeria. Methods: The dried pulvurised leaves of P. americana from uncultivated farmland in Ogbomoso, Oyo State Nigeria were extracted with methanol by the maceration method and partitioned successively with solvents of increasing polarity. The extracts obtained were subjected to phytochemical screening and the total phenolics were determined spectrometrically using the folin–ciocalteu method. Results: The phytochemical screening showed that P. americana is rich in various secondary metabolites such as flavonoids, saponins, tannins, and alkaloids. The total phenolic content gave 500µg/g gallic acid equivalent. The total flavonoid content obtained was 250µg/g using quercetin as standard. The anti-oxidant assay of the crude extract showed a high activity of 89.05% at a concentration of 0.05g/ml. Conclusion: Total phenolic content of the plant is likely to be a key for determining the free radical scavenging and ROS reducing ability of the plant.