Bradford Scholars
Bradford Scholars is the University of Bradford online research archive. Access is free to anyone interested in research being conducted at Bradford. In the repository you will find a range of materials from journal articles and conference papers to research reports and theses.
Contact the repository team via openaccess@bradford.ac.uk with any queries about Open Access or how to deposit your research papers.
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Publication Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents(2022-06)A series of uniquely functionalized 2,3,-dihydro-1H-pyyrolo[3,4-b]quinolin-1-one derivatives were synthesized in one to two steps by utilizing a post-Ugi modification strategy and were evaluated for antileishmanial efficacy against visceral leishmaniasis (VL). Among the library compounds, compound 5m exhibited potential in vitro antileishmanial activity (CC50 = 65.11 μM, SI = 7.79, anti-amastigote IC50 = 8.36 μM). In vivo antileishmanial evaluation of 5m demonstrated 56.2% inhibition in liver and 61.1% inhibition in spleen parasite burden in infected Balb/c mice (12.5 mg kg-1, i.p.). In vitro pharmacokinetic study ascertained the stability of 5m in both simulated gastric fluid and simulated intestinal fluid. All the active compounds passed the PAINS filter and showed no toxicity in in silico predictions.Publication Effectual Endeavors of Silk Protein Sericin against Isoproterenol Induced Cardiac Toxicity and Hypertrophy in Wistar Rats(2022-07-15)The silkworm cocoon has been used in the treatment of various ailments in different Asian countries. This research was designed to evaluate the effect of sericin on myocardial necrosis and hypertrophy in isoproterenol-challenged rats. The rats were administered with sericin (500 and 1000 mg/kg, p.o.) for 28 days, followed by administration of isoprenaline (85 mg/kg, s.c.) on the 29th and 30th days. The cardioprotective activity was assessed by various physical, enzymatic, and histopathological parameters along with apoptotic marker expression. The cardioprotective effect showed that pre-treatment of rats with sericin significantly increased the non-enzymatic antioxidants marker in serum and heart tissue (glutathione, vitamin E, and vitamin C). The results were the same in enzymatic antioxidant marker, mitochondrial enzymes, and protein. The grading of heart, heart/body weight ratio, gross morphology, cardiac markers, oxidative stress markers in serum and heart tissue, glucose, serum lipid profiling and Lysosomal hydrolases, heart apoptotic markers such as MHC expression by western blot, apoptosis by flow cytometry, total myocardial collagen content, fibrosis estimation, myocyte size were significantly decreased when compared with isoproterenol (ISG) group however histopathological studies showed normal architecture of heart in both control and treated rats. The pharmacological study reflects that sericin on both doses i.e., 500 mg/kg and 1000 mg/kg have potent cardioprotective action against the experimental model which was confirmed by various physical, biochemical, and histopathological parameters evaluated further research is required to examine the molecular mechanism of cardioprotective effect of sericin.Publication Adoption and Integration of Artificial Intelligence (AI) in UAE Public Safety and Security OrganisationsArtificial Intelligence (AI) usage is gaining momentum in the public sector due to its benefits. For instance, the need to reach more people faster, safely and securely has encouraged usage by the United Arab Emirates (UAE) public sector. However, it has been challenging integrating AI with existing system, thereby discouraging further AI adoption. This study aims to identify and assess factors that facilitate AI adoption, and AI integration in directorates responsible for UAE public safety and security. This study adopts the Unified Theory of Acceptance and Use of Technology (UTAUT) as a guide for determining factors that influence AI adoption in UAE public sector. Using quantitative approach, an online survey is completed by 411 officers from three directorates, and the data is analysed using Structural equation modelling (SEM). The findings reveal that performance expectancy and effort expectancy positively lead to AI behavioural intentions, and that AI behavioural intention positively influence AI adoption in the three sampled directorates. Further findings indicate that experience is crucial to integration of AI behavioural intention and AI adoption. Technology training is identified as a moderator of the relationship between facilitating conditions and AI usage. These findings offer new knowledge for security and safety scholars, technology adoption studies and for leaders in public safety and security by clarifying the factors that facilitate both AI adoption and integration. These results recommend the use of AI by applying the research framework to ensure successful AI adoption, and AI integration in the UAE public sector.Publication Techniques of Geophysical Prospection as applied to Near Surface Structure DeterminationThis thesis is an account of the research carried out by the author as a member of the Postgraduate School of Applied Physics at the University, during the years 1967 to 1970. The induced polarization and earth resistivity techniques of geophysical prospection are considered in detail, with respect to their application in the detection of discrete, near-surface features. The research includes the design and development of instruments to facilitate these measurements, in both laboratory and field environments. Field surveys over a variety of small scale features, are carried out to define the operation and usefulness of the instruments under such conditions. In the laboratory, the phenomena contributing to the induced polarization effect are investigated and a particular solution of the buried sphere problem is used to define the properties of several electrode configurations. The proposed solution is investigated by model experiments and is extended, with partial success, to include the responses from features of an arbitary shape. The interpretation of field data, by the use of a digital computer is studied and is applied to some of the survey examples.Publication Design and Synthesis of Topoisomerases-Histone Deacetylase Dual Targeted Quinoline-Bridged Hydroxamates as Anticancer Agents(2025-02-13)The multifactorial nature of cancer requires treatment that involves simultaneous targeting of associated overexpressed proteins and cell signaling pathways, possibly leading to synergistic effects. Herein, we present a systematic study that involves the simultaneous inhibition of human topoisomerases (hTopos) and histone deacetylases (HDACs) by multitargeted quinoline-bridged hydroxamic acid derivatives. These compounds were rationally designed considering pharmacophoric features and catalytic sites of the cross-talk proteins, synthesized, and assessed for their anticancer potential. Our findings revealed that the compound 5c significantly produced anticancer effects in vitro and in vivo by reducing the tumor growth and its size in the A549 cell-induced lung cancer xenograft model through multiple mechanisms, primarily by multi-inhibition of hTopoI/II and HDACs, especially HDAC1 via atypical binding. The present paper discusses detailed mechanistic biological investigations, structure–activity effects supported by computational docking studies, and DMPK studies and provides future scope for lead optimization and modification.