Yasser Hussein Eissa Mohammed

The anti-invasive role of novel synthesized pyridazine hydrazide appended phenoxy acetic acid against neoplastic development targeting matrix metallo proteases

Neoplastic metastasis is a major process where tumor cells migrate from the primary tumor and colonize at other parts of our body to form secondary tumor. Cancer incidences are rising and novel anti-neoplastic compounds with new mechanism of actions are essential for preventing cancer related deaths. In the current examination, a novel series of pyridazine analogues 6a-l was synthesized and evaluated against metastatic neoplastic cells. Experimental data postulated compound 6j has potential cytotoxic efficacy with prolonged activity against various cancer cells, including A549, HepG2, A498, CaSki and SiHa cells. Moreover, compound 6j arrests the A549 migration and invasions markedly by counteracting matrix metalloproteinase (MMP)-2 and MMP-9 expressions. Also, compound 6j proved its potentiality against Daltons solid lymphoma progression in-vivo by abridging MVD and MMP expressions. Compound 6j interacts with MMP-2 and MMP-9 by H- bond in-silico, thereby down regulates the MMPs action in tumourigenesis. Altogether, we concluded that compound 6j down regulates MMP-2 and MMP-9 and thereby impairs metastatic cancer cell migration and invasions which can be translated into a potent anti-neoplastic agent.

Synthesis and amelioration of inflammatory paw edema by novel benzophenone appended oxadiazole derivatives by exhibiting cyclooxygenase-2 antagonist activity

Ten new 2(4-hydroxy-3-benzoyl) benzamide-5-phenyl-1,3,4-oxadiazole derivatives (10a-j) were synthesized by coupling 3-benzoyl-4-hydroxybenzoic acid (5) with 2-amino-5-phenyl-1,3,4-oxadiazoles (9a-j). The structures of these compounds were confirmed by IR, 1H, 13C NMR, and mass spectra, and also by elemental analyses. The anti-inflammatory activity of the compounds 10a-j were investigated by screening them against human red blood cells (HRBC) in-vitro. The results reveal that among this series, compound 10j with hydroxy substituent, particularly at the ortho position of the phenyl ring attached to the 5th carbon atom of the oxadiazole ring possess significant membrane stabilizing activity in comparison with the control. Further, in-vivo chick chorioallantoic membrane (CAM) and rat corneal anti-angiogenesis assays were performed to assess the effect of compound 10j on endothelial cell migration. This confirmed that compound 10j inhibits the proliferation of endothelial cells. Anti-inflammatory studies detected the amelioration of carrageen induced rat hind paw edema. Further in-vivo and in-silico approaches revealed the inhibition of inflammatory marker enzyme cyclooxygenase-2 (Cox-2) and myleoperoxidase (MPO). The study reports that the compound 10j effectively act against the inflammatory mediated anti-angiogenic disorders which could be translated into a new drug in future.

Statistical Analysis of Antimicrobial Data of 2-[2-(Aroyl)aroyloxy]methyl-1,3,4 Oxadiazoles analogues Using ANOVA

Heterocyclic chemistry has become one of the most important fields of research in pharmaceutical industry due to their many fold applications. Amongst all, heterocyclic molecules containing nitrogen and oxygen (like oxadiazole ring system) have shown most potent biological activities. Microorganisms are strictly attendant with the fitness and well-being of human beings. The present treatments of bacterial and fungal infections are a bit unsatisfactory, owing to rapidly developing drug resistance and side effects. The improved of antibacterial and antifungal agents results in resistant to drugs. A series of substituted Oxadiazoles analogues 4a-jwere synthesized and screened for their antibacterial and antifungal activities to evaluate zone of inhibition. The significant effect ofin-vitroantimicrobial and antifungal activities of compounds 4a-jwere studied using one way ANOVA. It was shown that the variables 4a-j series weresignificant. Further pairwise comparison of significant differences between the variables were analyzed using Tukey HSD. The data revels that compound 4a with 2-methyl and 3chloro group in phenyl and benzoyl ring respectively, have shown excellent activity and more potent among the 4a-j series.

Biological Evaluation of 2, 5-Di (4 Aryloylaryloxy Methyl) - 1, 3,4-Oxadiazoles Derivatives as Antimicrobial Agents

A series of potential biologically active substituted 2,5-di(4 aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a-j were evaluated for its potential antimicrobial activity comparing with the standard drugs-Streptomycin and Ketoconazole respectively. Compound 9a with fluoro group exhibited highest activity against both gram-positive and gramnegative bacteria. Compounds 9a with fluoro group and 9c with fluoro and bromo showed good activity against antifungal activities.

Anti-Diabetic Activity of Dracaen cinnabari Balf.f Extracts from Resin inSocotra Island-Yemen

In the developing countries, the medical plants play an important role in treatment diabetes mellitus. This significant comes due to their cost effectiveness. Diabetes mellitus, a metabolic disorder is becoming a serious threat to mankind health. The herbal drugs with anti-diabetic activity are till now to be commercially formulated as modern medicines, even though they have been acclaimed for their therapeutic properties in the traditional systems of medicine. In this paper, we have reported a study based on anti-diabetic properties of Dragon cinnabari resin. The resin of plant material was collected, shade dried and extracted with different solvents using soxhlet extraction procedure. In vitro anti diabetic activity is assayed with standard glucose uptake procedure against MCF-7 cell line. From the analysis it was found that, glucose uptake inducing activity of ethyl acetate extract was found to be higher than Metformin, whereas other extracts did not display much anti diabetic activity against MCF-7 breast cancer cell line. Based on the glucose uptake studies against MCF-7 cell line, the ethyl acetate extract could be used as potential source for anti-diabetic drugs.