Abstract: Aspilia mossambicensis (Oliv.) Wild, Ocimum gratissimum (L.) Labiatae. and Toddalia asiatica (L.) Lam. (Rutaceae) were investigated with an overall aim of identifying and evaluating the bioactive antibacterial agents. Hexane, ethyl acetate and methanol realized yields of the range 0.5% Ocimum gratissimum stem bark ethyl acetate extract to 2.7% for Toddalia asiatica root bark methanol extract. The extracts were assayed for in vitro activity against gram positive; Methicillin Resistant Staphylococcus aureus and the gram negative; Pseudomonas aeruginosa, using disc diffusion method. The highest activity was with T. asiatica stem bark methanol extract (15 mm diameter zone of inhibition) against Methicillin Resistant Staphylococcus aureus. Bioactivity-guided fractionation of the T. asiatica (stem bark methanol extract) yielded up to four isolates labeled F1-C, F2-C, F3-C and F4-C. Preliminary phytochemical analysis gave positive results for mostly alkaloids, flavonoids, steroids and amines. By bioautographic selection the isolates showed antibacterial activity against Methicillin Resistant Staphylococcus aureus (0.3125 mg mL-1) which compared well to that of the standard drug gentamycin (0.5 mg mL-1).These results validate the ethno botanical use of Toddalia asiatica, a Kenyan medicinal plants for conditions that may be of bacterial etiology.