An Important Potential Anti-Epileptic/Anticonvulsant Active Group: A Review of 1,2,4-Triazole Groups and Their Action

Drug Research ◽  
2021 ◽  
Author(s):  
Ying Wang ◽  
Dachuan Liu

AbstractEpilepsy is one of the most common encountered neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting new antiepileptic/anticonvulsant drugs are required. Triazole compounds are widely used in pharmaceuticals and have gained significant importance in medicinal chemistry. This article is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades through extensive literature research. The results show that triazole occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their capability to exhibit an array of properties and bioactivities, Therefore, 1,2,4-triazole seems to be an important pharmacophore, especially in the field of antiepileptic, which is of great explored potentiality and utilized value. Through in-depth research on this type of structure, it is believed that more 1,2,4-triazole compounds will be developed as anti-epileptic drugs for clinical use.

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.


Author(s):  
Margit L. Bleecker

This chapter describes neurologic disorders related primarily to occupational exposures along with presenting signs and symptoms. Acute or subacute occupational exposure to high levels of neurotoxic compounds, which occurred in the past and resulted in unique presentations of neurological disorders, occur infrequently today. Sections include the evaluation of toxic neuropathies and the approach to neurobehavioral impairment along with the cognitive domains commonly affected with exposure to neurointoxicants. A section describes the approach to a patient with exposure to neurointoxicants that includes the need for a temporal association between exposure and effect, a dose-effect relationship, biological plausibility, and other causes eliminated Effects of selected neurotoxins are described, including carbon monoxide, lead, organic solvents, and manganese.


2018 ◽  
Vol 10 ◽  
pp. 117957351881354 ◽  
Author(s):  
Thais Massetti ◽  
Talita Dias da Silva ◽  
Tânia Brusque Crocetta ◽  
Regiani Guarnieri ◽  
Bruna Leal de Freitas ◽  
...  

Background: Virtual reality (VR) experiences (through games and virtual environments) are increasingly being used in physical, cognitive, and psychological interventions. However, the impact of VR as an approach to rehabilitation is not fully understood, and its advantages over traditional rehabilitation techniques are yet to be established. Method: We present a systematic review which was conducted according to Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). During February and March of 2018, we conducted searches on PubMed (Medline), Virtual Health Library Search Portal databases (BVS), Web of Science (WOS), and Embase for all VR-related publications in the past 4 years (2015, 2016, 2017, and 2018). The keywords used in the search were “neurorehabilitation” AND “Virtual Reality” AND “devices.” Results: We summarize the literature which highlights that a range of effective VR approaches are available. Studies identified were conducted with poststroke patients, patients with cerebral palsy, spinal cord injuries, and other pathologies. Healthy populations have been used in the development and testing of VR approaches meant to be used in the future by people with neurological disorders. A range of benefits were associated with VR interventions, including improvement in motor functions, greater community participation, and improved psychological and cognitive function. Conclusions: The results from this review provide support for the use of VR as part of a neurorehabilitation program in maximizing recovery.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Amita Verma ◽  
Sunil Joshi ◽  
Deepika Singh

Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.


Cancers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 604
Author(s):  
Laura Vanderwaeren ◽  
Rüveyda Dok ◽  
Kevin Verstrepen ◽  
Sandra Nuyts

Clinical use of proton radiation has massively increased over the past years. The main reason for this is the beneficial depth-dose distribution of protons that allows to reduce toxicity to normal tissues surrounding the tumor. Despite the experience in the clinical use of protons, the radiobiology after proton irradiation compared to photon irradiation remains to be completely elucidated. Proton radiation may lead to differential damages and activation of biological processes. Here, we will review the current knowledge of proton radiobiology in terms of induction of reactive oxygen species, hypoxia, DNA damage response, as well as cell death after proton irradiation and radioresistance.


PEDIATRICS ◽  
1990 ◽  
Vol 86 (3) ◽  
pp. 457-459
Author(s):  
Michael A. Gerber ◽  
Richard R. Facklam ◽  
Martin F. Randolph ◽  
Kathleen K. DeMeo

During the last few years there has been a dramatic proliferation of rapid tests for the diagnosis of group A β-hemolytic streptococcal pharyngitis.1 It is important for physicians to realize that the Food and Drug Administration does not approve these diagnostic tests as it would approve a pharmacologic agent, but simply permits a manufacturer to sell the test. Consequently, unacceptably inaccurate rapid tests for group A streptococci have been marketed in the past and could potentially appear again at anytime. In 1986, we studied a new enzyme fluorescence procedure (Strep-A-Fluor, Bio-Spec Inc, Dublin, CA) for the rapid diagnosis of group A β-hemolytic streptococcal pharyngitis.2


Author(s):  
Igor Aleksandrovich Medyanik ◽  
Simon Quarteng Badu

The possibility of using only tractography as a preoperative diagnosis of anaplastic glioma is limited due to its inability to show the exact functional location of the tumor; therefore, the combination of tractography and fMRI seems to be a more promising complex diagnostic method. In neurooncology, complete resection without or with minimal neurological deficit is the goal of surgical intervention. The aim of the study was to investigate the advantages and limitations of the use of tractography and fMRI in the treatment of anaplastic glioma compared to standard CT or MRI. The study involved 48 patients who were divided into two groups based on the use of fMRI and tractography: group A (24 patients) and without it — group B (24 patients). The groups were compared in terms of age, sex, histological subtype of anaplastic glioma, degree of resection, postoperative complications, and dynamics of neurological disorders. The combination of fMRI and tractography is the best preoperative diagnosis, it is safe and allows localizing neural pathways, preserve them during surgery, and reduce postoperative neurological deficits.


1998 ◽  
Vol 79 (5) ◽  
pp. 388-391
Author(s):  
G. V. Cherepnev ◽  
Y. D. Slabnov ◽  
I. E. Zimakova

The relevance of pharmacological correction of immunological reactivity is obvious: many socially significant diseases are accompanied by an imbalance in immune homeostasis. In the past few years, a number of reviews on the classification and mechanisms of action of immunotropic drugs approved for clinical use in the Russian Federation have been published in the domestic press.


PEDIATRICS ◽  
1973 ◽  
Vol 52 (4) ◽  
pp. 586-600
Author(s):  
David H. Smith ◽  
David L. Ingram ◽  
Arnold L. Smith ◽  
Floyd Gilles ◽  
M. J. Bresnan

Prior to the introduction of specific antibacterial therapy, bacterial meningitis was a disease with a universally fatal or disastrous outcome. The introduction of typespecific antiserum, and then of the antibacterial drugs, improved this situation dramatically. Improvements in the general medical care of acutely ill children, and the introduction of a series of more potent antibiotics against its bacterial causes helped to generate an attitude that bacterial meningitis was, or soon would be, a disease of the past. The experience of the past two decades belies this thesis. Today, interest in many facets of this disease has been renewed by many physicians concerned with the health of children: the epidemiology, pathophysiology, diagnosis, and treatment. This symposium attempts to summarize for the practitioner the highlights of current knowledge in this area, and to outline certain areas in which recent advances can be anticipated, or will be studied. Tuberculous meningitis will be omitted for the sake of brevity, as will the special problems of meningitis in the newborn infant. There has been a resurgence of interest in developing vaccines to prevent Hemophilus influenzae b, pneumococcal, and meningococcal Group A, B, and C meningitis. These organisms cause almost all the bacterial meningitis after the first two months of life. If, as now seems possible, vaccines against most or all of these organisms will soon become available, those children having the greatest risk must be defined to determine who, and at what age should have priority in receiving the vaccine(s). A. THE CURRENT MAGNITUDE OF THE PROBLEM


Author(s):  
Paige Robinson ◽  
Gavin Mclaughlin ◽  
Michael O'Meara ◽  
Hilary Ouellette

Over the past five years, there has been an abundance of interest concerning the ecological effects of major Ontario highways on the habitats and ecosystems of many wildlife populations. The primary concern with multilane, high-traffic freeways is that they typically divide existing habitats into relatively isolated zones. Consequently, this separates individuals within a population from other members of the same population, and also excludes access to many natural resources. The majority of the resultant issues for wildlife fall under three main categories; the collision based mortalities of organisms and the consequences on local residents, the halting of gene flow amongst the wildlife populations, and the physical intrusion and/or noise pollution adversely affecting the quality of habitat for local species. Based on these concerning issues, it is crucial for a sustainable solution to be developed and implemented in appropriate areas within Kingston and the surrounding Frontenac County. Our approach involves an extensive literature review, which will assist us in observing similar problems around the globe, as well as various solutions that have been executed to fix these said problems. Furthermore, we will conduct a thorough investigation of local organizations’ existing studies to obtain relevant data and statistics which will assist us in determining the effects high-traffic freeways have on the surrounding ecological environment. It is through this research that we hope to present valid findings on the multilane highways impact to local ecosystems and landscapes, as well as produce possible planning options for intervention and suggest key areas for further examination.


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