No abstract

New thymol − 1,5-disubstitutedpyrazole hybrids were synthesised as dual COX-2/5-LOX inhibitors. Compounds 8b , 8g , 8c, and 4a displayed in vitro inhibitory activity against COX-2 (IC 50 = 0.043, 0.045, 0.063, and 0.068 µM ) nearly equal to celecoxib (IC 50 = 0.045 µM ) with high SI (316, 268, 204, and 151, respectively) comparable to celecoxib (327). All target compounds, 4a–c and 8a–i , showed in vitro 5-LOX inhibitory activity higher than reference quercetin. Besides, they possessed in vivo inhibition of formalin-induced paw oedema higher than celecoxib. In addition, compounds 4a, 4b, 8b, and 8g showed superior gastrointestinal safety profile (no ulceration) as celecoxib and diclofenac sodium in the population of fasted rats. In conclusion, compounds 4a , 8b, and 8g achieved the target goal. They elicited in vitro dual inhibition of COX-2/5-LOX higher than celecoxib and quercetin, in vivo potent anti-inflammatory activity higher than celecoxib and in vivo superior gastrointestinal safety profile (no ulceration) as celecoxib.

Background: Thymol has been reported to have a variety of antimicrobial and insecticidal activities but it has irritation side effect due to its phenolic nature. Methods: A new series of potential non-irritant non-phenolic thymol derivatives were designed to hybridize the well-known biologically active thymol scaffold with various five membered heterocyclic antimicrobial and insecticidal pharmacophores like 1,3,4-oxadiazole, 1,3,4-thiadiazole, 1,2,4-triazole, thiazole and 4-thiazolidinone through different spacers. The target compounds were biologically evaluated for their in vitro antibacterial, antifungal and insecticidal activities. Results: Compounds 4b and 9c showed weak antibacterial activity against S. aureus and B.subtilis with the inhibition zone diameters ranging from 2 to 7 mm and 4 mm respectively compared with ciprofloxacin with the inhibition zone diameter of 21 mm. Compounds 9a, 7d and 13b showed weak antibacterial compounds against B. subtilis with inhibition zone diameters 4, 4 and 6 mm respectively. Compounds 12b, 9c and 7a showed 20% insecticidal activity at a concentration of 0.157 mg/cm2 for each compound against Tribolium castaneum (Herbst) and Sitophilus oryzae (L.). Compound 6 showed moderate larvicidal activity against Culex pipiens with 40% mortality at a concentration of 1000 ppm. Conclusion: Compound 9c showed weak dual antimicrobial and insecticidal activities.

This study aimed to study the effect Zingiber officinale and Allium sativum crude extract on bacterial isolates from children suffer from urinary tract infection (UTI) and compare it with the activity of antibiotics. The bacterial isolated were collected from variety of hospitals during the period 6-1-2021 to 5-4-2022. The isolates were cultured and identified. 100 bacterial isolates identified as follows Pseudomonas aeruginosa (2), Escherichia coli (65), Staphylococcus aureus (20), Klebsiella pneumonia and Proteus mirabilis (2) for each, Scaphirhynchus albus, Morganella morganii and Micrococcus (1), Staphylococcus capitis, Staphylococcus epidermidis, Proteus vulgaris, Klebsiella oxytoca, Citrobacter freundii and Pseudomonas luteola (1). Different degrees of sensitivity were shown by the isolates for different types of antibiotics. Antibacterial activity of aqueous Z. officinale extract was (7–30) mm while the alcoholic extract of Z. officinale was (4–20) mm. aqueous A. sativum extract (3–26) mm while alcoholic extraction (5–22) mm.