pylori causes severe stomach disorders and the use of enzyme inhibitors for treatment is one of the possible therapies. The great biological potential of imine analogs as urease inhibitors has been the focus of researchers in past years. In this regard, we have synthesized twenty-one derivatives of dichlorophenyl hydrazide.
View Article and Find Full Text PDFThis work reports the convenient approach for the synthesis of thiazole based thiourea derivatives from 2-bromo-1-(4-fluorophenyl)thiazole-1-one and phenyl isothiocyanates. The scope and diversity were achieved from readily available phenyl isothiocyanates. This protocol involves an oxidative C-S bond formation.
View Article and Find Full Text PDFAcetylcholinesterase prevails in the healthy brain, with butyrylcholinesterase reflected to play a minor role in regulating brain acetylcholine (ACh) levels. However, BuChE activity gradually increases in patients with (AD), while AChE activity remains unaffected or decays. Both enzymes therefore represent legitimate therapeutic targets for ameliorating the cholinergic deficit considered to be responsible for the declines in cognitive, behavioural, and global functioning characteristic of AD.
View Article and Find Full Text PDFThe human gut microbiome has been implicated in a host of bodily functions and their regulation, including brain development and cognition. Neuroinflammation is a relatively newer piece of the puzzle and is implicated in the pathogenesis of many neurological disorders. The microbiome of the gut may alter the inflammatory signaling inside the brain through the secretion of short-chain fatty acids, controlling the availability of amino acid tryptophan and altering vagal activation.
View Article and Find Full Text PDFInflammatory cascade plays a pivotal role in the onset and progression of major depressive disorder (MDD) and glioblastoma multiforme (GBM). Therefore, questing natural compounds with anti-inflammatory activity such as diosgenin can act as a double-edged sword targeting cancer and cancer-induced inflammation simultaneously. The blood-brain barrier limits the therapeutic efficiency of the drugs against intracranial pathologies including depression and brain cancers.
View Article and Find Full Text PDFRationale: Major depressive disorder is the leading cause of disability worldwide. The corticolimbic system plays a critical role in the emotional and cognitive aspects of major depressive disorder. Owing to the unsatisfactory efficacy of conventional antidepressants, there is a need to explore novel therapies.
View Article and Find Full Text PDFIndole based thiadiazole derivatives (1-18) were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The IC values of the synthesized analogues ranging between 0.17 ± 0.
View Article and Find Full Text PDFSynthesis of quinoline analogs and their urease inhibitory activities with reference to the standard drug, thiourea (IC = 21.86 ± 0.40 µM) are presented in this study.
View Article and Find Full Text PDFIn search of potent urease inhibitor indole analogues () were synthesized and evaluated for their urease inhibitory potential. All analogues () showed a variable degree of inhibitory interaction potential having IC value ranging between 0.60 ± 0.
View Article and Find Full Text PDFCoronavirus outbreak in Wuhan, China, turned into a pandemic in record time. Communication of disease presentation and mechanism of spread remain keys to getting ahead of the virus and limiting its spread beyond the capacity of management. Owing to huge academic focus and pandemic concern around the globe, this bibliometric analysis investigated research productivity related to coronavirus disease (COVID-19) pandemic using the Web of Science database.
View Article and Find Full Text PDFGlobal health estimates indicated approximately 322 million people living with depression. Rising cost of depressive illness treatment and non-responsiveness to existing therapies demand continued research to explore new and more potent therapies. Exploring the potential of natural compounds for their potent antidepressant potentials is becoming topic of interest for scientists.
View Article and Find Full Text PDFIn continuation of our work on enzyme inhibition, the benzofuran-based-thiazoldinone analogues (1-14) were synthesized, characterized by HREI-MS, H and CNMR and evaluated for urease inhibition. Compounds 1-14 exhibited a varying degree of urease inhibitory activity with IC values between 1.2 ± 0.
View Article and Find Full Text PDFβ-Glucuronidase is responsible for the catalytic deconjugation of β-d-glucuronides. β-Glucuronidase has evolved to be a viable molecular target for numerous therapeutic treatments. It plays a pivotal role in the metabolism of drugs and endogenous substances.
View Article and Find Full Text PDFElectroconvulsive therapy (ECT) is an effective treatment for severe medication-resistant depression. However, ECT frequently results in episodic memory impairments, causing many patients to discontinue treatment. The objective of this study was to explore the functional connectivity underpinnings of ECT-induced episodic memory impairments.
View Article and Find Full Text PDFObjective: To review the dynamics of neuroscience research in the Kingdom of Saudi Arabia (KSA) from 2013-2018.
Methods: Subject category of Neuroscience was selected in the SciVal feature of Scopus database, which includes all relevant categories of the field limiting it to Saudi Arabia.
Results: Saudi Arabia is ranked 39th in publishing neuroscientific research worldwide.
The purpose of this study was to analyze the published research on health sciences carried out by researchers in Saudi Arabia in the last decade by assessing bibliometric output. Data for 2008 to 2017 was retrieved from Scopus. During this period, there was significant growth, from 1332 publications in 2008 to 5529 in 2017, with an average annual growth rate of 14.
View Article and Find Full Text PDFA series of twenty-six analogs of benzimidazole based oxadiazole have been synthesized and evaluated against alpha-glycosidase enzyme. Most the analogs showed excellent to good inhibitory potential. Among the screened analogs, analog 1, 2, 3 and 14 with IC values 4.
View Article and Find Full Text PDFBovine babesiosis is an infectious protozoan disease and causes significant economic losses in terms of production loss and mortality. The genus Babesia belongs to the family Babesiidae order piroplasmida and is transmitted by ticks globally. The signs of disease are particularly prominent in old or immuno-compromised animals.
View Article and Find Full Text PDFSultan Qaboos Univ Med J
August 2019
Objectives: Mental health is a less frequently explored area of medical research as both developing and developed countries lack competent human resources and funding for this purpose. Reviewing mental health research can help medical professionals appreciate the progress of understanding and identify problems in this area. This systematic review examined the status of mental health research carried out in medical education institutions and tertiary healthcare hospitals across Pakistan over the past 70 years.
View Article and Find Full Text PDFWe have synthesized new series of bisindole analogs (-), characterized by HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC values ranging from 0.7 ± 0.
View Article and Find Full Text PDFDepression is considered as a maladaptive response to stress in adult life. Exposure to stress in early childhood is recognized as a risk factor for being unable to adapt to environmental changes in adult life. Early life stress (ELS) has been modelled in animals to help understand the behavioral outcome of the adversity.
View Article and Find Full Text PDFChromen-4-one substituted oxadiazole analogs - have been synthesized, characterized and evaluated for -glucuronidase inhibition. All analogs exhibited a variable degree of -glucuronidase inhibitory activity with IC values ranging in between 0.8 ± 0.
View Article and Find Full Text PDFWe have synthesized quinoxaline analogs (⁻), characterized by ¹H-NMR and HREI-MS and evaluated for thymidine phosphorylase inhibition. Among the series, nineteen analogs showed better inhibition when compared with the standard inhibitor 7-Deazaxanthine (IC = 38.68 ± 4.
View Article and Find Full Text PDFβ-glucuronidase is a lysosomal glycosidase enzyme which catalyzes the extracellular matrix of cancer and normal cells and the glycosaminoglycans of the cell membrane, which is important for cancer cell proliferation, invasion, and metastasis. Liver cancer, colon carcinoma, and neoplasm bladder are triggered by the increase of the level of β-glucuronidase activity. The most valuable structures are indole and oxadiazole which has gain immense attention because of its pharmacological behavior and display many biological properties.
View Article and Find Full Text PDFMonocytes are leading component of the mononuclear phagocytic system that play a key role in phagocytosis and removal of several kinds of microbes from the body. Monocytes are bone marrow precursor cells that stay in the blood for a few days and migrate towards tissues where they differentiate into macrophages. Monocytes can be used as a carrier for delivery of active agents into tissues, where other carriers have no significant access.
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