Some novel non‐ulcerogenic N‐substitutedphenyl‐6‐oxo‐3‐phenylpyridazines as COX‐2 inhibitors have been developed (Supplementary material Appendix 1). The novel aldehyde 3 was prepared by reacting 6‐phenylpyridazin‐3(2H)‐one with 4‐fluorobenzaldehyde. The aldehyde 3 was reacted with different hydrazines and thiazolidin‐4‐ones to obtain the novel N‐substitutedphenyl‐6‐oxo‐3‐phenylpyridazine derivatives. These were assessed for their anti‐inflammatory potential and gastric ulcerogenic effects. The molecular docking investigations were also undertaken. The spectroscopic data were coherent with the allocated structures of the compounds. The compounds 4a (IC50 = 17.45 nm; p < .05), 4b (IC50 = 17.40 nm; p < .05), 5a (IC50 = 16.76 nm; p < .05), and 10 (IC50 = 17.15 nm; p < .05) displayed better COX‐2 inhibitory activity than celecoxib (IC50 = 17.79 nm; p < .05). These findings were consistent with the molecular docking investigations of 4a, 4b, 5a, and 10. The in vivo anti‐inflammatory profile of 4a, 4b, 5a, and 10 was also superior to celecoxib and indomethacin. The compounds 4b, 5a, and 10 revealed no gastric ulcerogenic effects, wherein the compound 4a produced almost negligible gastric ulcerogenic effects than celecoxib and indomethacin. The compounds 4a, 4b, 5a, and 10 have been postulated as promising non‐ulcerogenic COX‐2 inhibitors.
Cyclooxygenase-2 (COX-2) is implicated in the development of chronic inflammatory diseases. Recently, pyridazine derivatives have emerged as a novel prototype to develop COX-2 inhibitors. Accordingly, some pyridazine-based COX-2 inhibitors are reported herein. The reaction of aldehyde 3 and different hydrazines yielded the corresponding hydrazones. The hydrazones were further derivatized to the title compounds, which were assessed for COX-1 and COX-2 inhibitory action, gastric ulcerogenic effects, and lipid peroxidation properties. Molecular docking studies and determination of the physicochemical parameters were also carried out. The allocated structures of the reported compounds were coherent with their spectroscopic data. The compounds 9a (IC50 = 15.50 nM, 114.77%), 9b (IC50 = 17.50 nM, 101.65%), 12 (IC50 = 17.10 nM, 104.03%), 16b (IC50 = 16.90 nM, 105.26%), and 17 (IC50 = 17.70 nM, 100.5%) displayed better COX-2 inhibition than celecoxib (IC50 = 17.79 nM, 100%). These outcomes were harmonious with the molecular docking studies of 9a, 9b, 12, 16b, and 17. These compounds also displayed comparable onset and the duration of action concerning celecoxib and indomethacin in the in vivo studies. No ulcerogenic effects were observed for 9a and 12, whereas 9b, 16b, and 17 showed an insignificant ulcerogenic effect compared to celecoxib. The compounds 9a, 9b, 12, 16b, and 17 displayed a better lipid peroxidation profile than celecoxib and indomethacin. The compounds 9a (%ABS = 84.09), 9b (%ABS = 84.09), 12 (%ABS = 66.87), 16b (%ABS = 75.02), and 17 (%ABS = 81.42) also displayed appreciable calculated absorption compared to celecoxib (%ABS = 82.09). The compounds 9a, 9b, 11, 16b, and 17 have been recognized and postulated as non-ulcerogenic COX-2 inhibitors with promising physicochemical parameters and gastric safety profile. These compounds may be useful candidates to combat diseases caused by higher levels of COX-2.
The objective of this study was to evaluate the anthelmintic, antimicrobial and antioxidant activities of Chenopodium album against gastrointestinal nematodes of sheep and some pathogenic microbes. A worm motility inhibition assay was used for in vitro study, and a faecal egg count reduction assay was used for an in vivo study. Various concentrations ranging from 100 to 500 μg/ml of the extract were subjected to antimicrobial screening by disc diffusion method against four selected bacterial (Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas multocida and Escherichia coli) and two fungal (Aspergillus flavus and Candida albicans) strains in order to estimate the medicinal potential of the herb. DPPH (1,1-diphenyl-2-picrylhydrazyl), riboflavin photo-oxidation, deoxyribose, lipid peroxidation assays were used for antioxidant activity. The extracts exhibited dose- and time-dependent anthelmintic effects on the Haemonchus contortus as compared to levamisole. The extract showed maximum inhibitory effect against S. aureus (28 ± 0.14 mm), while as mild inhibitory effect was observed against E. coli among the selected microbial strains. The effect produced by the different extract concentrations was comparable with the standard antibacterial agent streptomycin sulphate and antifungal agent nystatin, which were used as effective positive control in the study. The antioxidant activity showed that the extracts exhibited scavenging effect in concentration-dependent manner on superoxide anion radicals and hydroxyl radicals leading to the conclusion that the plant has broad spectrum anthelmintic, antimicrobial and antioxidant activities and could be a potential alternative for treating various diseases.
One year crossectional survey was carried out to determine and describe the prevalence and intensity of gastrointestinal parasite infections in hangul (Cervus elaphus hanglu) in Dachigam National Park of Kashmir through faecal examinations. Out of 153 faecal samples examined, 82 (53.59 %) were found infected with GIT helminthes. In present study seven helminth species were found, including five nematode [Haemonchus contortus (55.39 %), Trichuris ovis (39.75 %), Dictyocaulus viviparus (28.4.00 %), Oesophogostomum circumcincta (13.7 %) and Chabertia ovina (4.02 %)] one trematode [Fasciola hepatica (17.3 %)] and one cestode species [Moneizia expansa (6.05 %)]. Based on the severity of infection 81.7 % of hangul positive samples were severely infected (epg [ 1,500), 8.3 % heavily infected (epg = 1,100-1,500), 3.8 % moderately infected (epg = 800-1,000) and 7.2 % mildly infected (epg = 500). Season, sex and age were the factors that influenced the epidemiological prevalence of GIT helminths in hangul in the present study. The maximum helminth infection was observed in summer season and lowest in winter (P = 0.003). Lower age groups were more infected than adult animals (P [ 0.05). Prevalence was higher in males than females (P [ 0.05). The present study will initially be of great significance to add to existing knowledge of the epidemiology of GIT helminth of hangul which is the pioneering study on this animal in the valley and the findings will be quite helpful to devise the appropriate control and prophylactic strategies for GIT helminthiasis of hangul in the Dachigam national park.
A faunistical study of ectoparasites was carried out for a period of two years from January 2005 to December 2006 in rural free-range chicken purchased from different areas of Kashmir valley. Screening of a total of 478 birds revealed only lice infestation with an overall prevalence of about 100% and 97.69% birds harboring multiple species. The prevalence for various species of lice, during winter, spring, summer, autumn and overall prevalence respectively, was 90.32%, 99.14%, 100%, 98.34% and 96.86% for Lipeurus caponis; 33.87%, 48.71%, 57.75%, 39.66% and 44.76% for Goniodes gigas; 29.83%, 32.47%, 45.68%, 32.23% and 34.93% for Menopon gallinae; 28.22%, 32.47%, 39.65%, 32.23% and 33.05% for Menacanthus cornutus; 16.12%, 19.65%, 25%, 18.18% and 19.66% for Goniocotes gallinae and 6.45%, 12.82%, 13.79%, 4.95% and 9.41% for Eomenacanthus stramineus. The seasonal influence on nature and intensity of infestation was evident.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.