Pharmaceutical Sciences
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- ItemDESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF THIAZOLE-CARBOXAMIDE DERIVATIVES AS COX INHIBITORS(2022-12-26) Rozan Ghassan SabobehABSTRACT Non-Steroidal anti-inflammatory drugs (NSAIDs) are often employed to alleviate swelling and discomfort and lower high temperatures. They inhibit the cyclooxygenase enzyme (COX) required to convert arachidonic acid to Prostaglandins that are inflammatory. In this master's thesis, new thiazole derivatives with aniline derivatives were synthesized, specified, and estimated for their selectivity and potency at COX-1 and COX-2 by an in vitro COX inhibition assay kit. The synthesized compounds' cytotoxicity was estimated using an MTS assay against human hepatic stellate (LX-2) and the normal cell line (Hek293T). HRMS, 1H-NMR, and 13C-NMR techniques characterized all newly synthesized chemicals. The results demonstrated that the most effective compound against the COX-1 enzyme was 2b with an IC50 =0.239 µM. It also showed potent activity against COX-2 with IC50=0.191 µM with a selectivity ratio of 1.251. The highest selectivity ratio was (2.766) for 2a compound against COX-2 with an IC50 = 0.958 µM relating to celecoxib ratio (23.8) and its IC50 against COX-2 =0.002 µM. The 2j compound also showed good selectivity towards COX-2 (1.507) with an IC50 of 0.957 µM. All compounds showed negligible cytotoxic activity against the evaluated normal cell lines, and the IC50 values were more than 300 µM, except compound 2b, whose IC50 values were 203.711.89 and 116.96±2.05 µM against LX-2 and Hek293t cell lines, respectively. Keywords: Anti-inflammatory; Cyclooxygenase enzyme; COX inhibitors; Docking studies; Heterocyclic; Thiazole-carboxamide; NSAIDs.
- ItemBIOLOGICAL EVALUATION OF 2-OXO-BENZOXAZOLE DERIVATIVES(2023-09-07) Haneen Marwan Abu KatabBenzoxazole derivatives are essential building blocks for innovative drugs due to their wide range of biological activities in medicinal chemistry, particularly their pharmacological effects (such as analgesic, antibacterial, antifungal, anti-inflammatory, and anticancer properties). The importance of benzoxazole derivatives in drug development is emphasized by this work, which also highlights their potential as therapeutic targets with a variety of pharmacological actions and structural flexibility. This study investigates the 1,3-oxazole nucleus, which is a very effective molecule with antibacterial, anticancer, analgesic, and anti-inflammatory characteristics. These substances are created both naturally and artificially by several organisms, including bacteria and marine life. Pharmaceutical compounds belonging to the 1,3-oxazole family can be used to synthesize a wide range of molecules with various therapeutic applications, such as antiviral and anticancer effects. The fascinating possibility of benzoxazole derivatives inhibiting anaerobic choline metabolism and their possible anticancer effects is examined in this work. Certain compounds based on benzoxazoles exhibit enhanced cytotoxicity, especially towards particular cancer cell lines, suggesting that they may be useful in stopping the spread of cancer cells. The promise of benzoxazole derivatives in pharmaceutical research is highly praised, and more investigation into the benzoxazole scaffold and its functionalization is encouraged to find more powerful and selective molecules with enhanced activity and decreased toxicity. The study's findings on sixteen artificial chemicals tested against seven cancer cell lines are presented in the article. The compounds BNZ-2, BNZ-4, BNZ-7, BNZ-9, and BNZ-10 show promise as anticancer agents. Key moieties, such as chlorobenzoyl, piperazine, piperidine, morpholinomethyl, and 4-methylpiperidin-1-yl, that are responsible for their actions against different cell lines are identified by a structural analysis using Structure-Activity Relationship (SAR) study. BNZ-10 has a lower IC50 value than other well-known anticancer medications, which suggests that it may be a more effective treatment against particular cancer cell types. It's important to remember, nevertheless, that doxorubicin (DOX) has far lower IC50 values than the majority of BNZ-1-16 drugs and is nonetheless a powerful anticancer agent. The study concludes by highlighting the tremendous promise of benzoxazole derivatives in drug development, particularly in the treatment of cancer, and the significance of particular structural motifs in controlling their biological activity. Novel treatment approaches in hepG2-associated malignancies require further research on molecular interactions and processes, especially those that affect hepG2 cells. The research advances the hunt for new medicines and helps to rationally develop anticancer drugs. Keywords: Benzoxazole Derivatives; Anticancer Efficacy; Structure-Activity Relationship (SAR); IC50 Values
- ItemINFLUENCE OF FOOD INDUCED VISCOSITY ON DISSOLUTION AND DISINTEGRATION OF TABLETS: EFFECT OF FORMULATION AND PROCESS PARAMETERS ON TABLET MANUFACTURED BY WET GRANULATION(2023-06-05) Zain Alabedin ZanoonAbstract Postprandial elevation in gastric viscosity may retard tablet disintegration and delay drug dissolution from solid dosage forms, resulting in a significant decrease in drug bioavailability thereby affecting the therapeutic efficacy. This may be critical especially for medication where rapid onset of action is required. Deep understanding of the critical processing parameters on tablet disintegration and drug dissolution under fed conditions will help in designing a formulation with minimum viscosity mediated negative food effects. The current research aims to study the impact of formulation and processing factors on tablet disintegration and release of Active Pharmaceutical ingredient (API) under both fasting state and fed states. The effect of different types of fillers was investigated in different formulations: Lactose monohydrate, corn starch and Microcrystalline cellulose (MCC), as well as, Di-calcium phosphate dehydrate. Wet granulation is a critical manufacturing step for oral solid dosage forms. Wet granulation method was applied in the preparation of ten immediate release formulations with Paracetamol serving as the model drug. The effects of wet granulation parameters such as: the mode of incorporation of disintegrant and the type of the granulating solvent were highlighted. The study concluded that filler type is found to affect tablet disintegration: MCC based formulations gave the quickest drug disintegration in simulated fasted state, but they were the worst under viscous media. Lactose and Dicalcium Phosphate (DCP) based formulations provide rapid disintegration under fed state. Formulations prepared by using alcohol as solvent of granulation had shorter disintegration times compared to formulations using water in both fasting and fed states. The addition of Sodium Starch Glyclolate (SSG) intra-granularly results in shorter disintegration time compared to the extra-granular counterparts under fed condition. The study recommends that: the obtained results highlight the importance of formulation excipients (filler type) and manufacturing parameters on tablet disintegration. This study will provide guidance that help in design and development of formulation with minimal food effect. Keywords: Behaviour; Disintegration; Dissolution; Even Formula; Fasting State; Fed State; Odd Formula.
- ItemMEASURES OF JUVENILES AND THE MECHANISM OF IMPLEMENTING THEM IN THE PALESTINIAN LAW(جامعة النجاح الوطنية, 2022-03-13) Ibrahim, MohammadBackground: There is an urgent need to understand the measures related to juveniles and the mechanism for implementation through researching these measures, especially after the issuance of the decision by Law No. 4 of 2016 regarding juvenile trial, which starts new stage in the development of Palestinian courts about the punitive measures imposed on juveniles in order to achieve the interest best event Purpose: The purpose of this research is to shed light on the measures stipulated in Decree-Law No. 4 of 2016 related to juveniles by examining the measures and their compatibility with the Palestinian reality, familiarity with the measures and the ability to differentiate between freedom- and non-custodial measures under the age of fifteen, as well as the measures relating to juveniles depriving of liberty issued over the age of fifteen, and to find out the mechanism for implementing judicial rulings issued by the competent courts regarding juveniles and the mechanism for monitoring implementation these measures in order to achieve the best interest of the juvenile. Method: The legal framework is determined in Decree-Law No. (4) of 2016, an analytical study of the texts of articles from Article 36-49 of Decree-Law No. 4 of 2016, Criminal Procedures Law No. (3) of 2001 in force in Palestine and Jordanian Penal Code No. 16 of 1960 The Jordanian Juvenile Reform Law of 1954 and Child Law No. 7 of 2004. Results: After the application of the decision by Law No. 4 of 2016, the decision by law under this study clarified how to implement the measure of the social control order in some detail, leaving the matter to the discretion of the Child Protection Guide and others who implement the measures related to juveniles. Likewise, the juvenile judge is not considered a full-time judge in cases involving juveniles, but rather he is a delegated judge who adjudicates juvenile cases and other cases that fall within the scope of his work and his jurisdiction, both criminally and civilly. Conclusion: Emphasis on the need to review the provisions of the decree-law as soon as possible, given the failure to achieve its main objective, which is to achieve the best interest of the juvenile, and to establish more vocational training centers and social welfare homes to distribute them in the Palestinian governorates in order to deposit juveniles sentenced to a measure due to the lack of A large number of such centers.
- ItemTHE LEVEL OF IRRATIONAL THOUGHTS AND IT’S RELATIONSHIP TO PSYCHOLOGICAL SECURITY, SOCIAL ADJUSTMENT, AND QUALITY OF LIFE AMONG AN-NAJAH NATIONAL UNIVERSITY STUDENTS(جامعة النجاح الوطنية, 2022-07-28) Hamdi Al-Bazian, YazanThis study aims to recognize the level of Irrational thoughts and its relationship to Psychological security, Social Adjustment, and the Quality of life Among An-Najah National University Students. This research relies on the descriptive correlational approach to extract its results. The study population include the students of An-Najah National University, and an accessible random sample is select that consist of 200 male and female students from the original research community. Four criteria are applied in the study: the Irrational thoughts scale, the Psychological security scale the Social Adjustment scale, and the Quality of life scale. The study sums up that the level of Irrational thoughts among An-Najah National University students is middle, and the existence of a statistically significant inverse correlation between the level of Irrational thoughts and Psychological security among them. Also, there is a statistically significant inverse correlation between the level of Irrational thoughts and the GPA, grade point average. Whereas there is no relationship with the rest of the variables (social adaptation and Quality of life). The study came out with several recommendations, the most important of which are, working to enhance rational thinking among students through programs that serve the process of strengthening this thinking across the various university platforms, and building specialized counseling programs in universities on problem-solving skills for university students, and improving their behavior, which It enhances the level of rational thoughts, and his sense of psychological security, in addition to including this in educational curricula at universities