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CNS & Neurological Disorders Drug... 2023Drug design is one of the critical aspects of the drug development process. The present review focused on different heterocyclic molecules having anticonvulsant activity... (Review)
Review
Drug design is one of the critical aspects of the drug development process. The present review focused on different heterocyclic molecules having anticonvulsant activity with structural diversity and common pharmacophoric features. For the first time (1995), Dimmock and his team introduced specific arrangements of three important pharmacophores for anticonvulsant activity. These pharmacophores include two hydrophobic binding sites and one hydrogen binding site. After a few years (2012), Pandeya modified Dimmock's concept by adding one more pharmacophoric feature as an electron donor in the previously suggested pharmacophoric arrangement of the anticonvulsant. As a result, numerous scientists designed anticonvulsant drugs based on Dimmock's and Pandeya's concept. In addition, marketed anticonvulsant preparation containing Riluzole, Phenobarbital, Progabide, Ralitoline, etc., also holds the suggested pharmacophores by Dimmock and Pandeya's pharmacophoric concept. This review mainly focuses on the compilation of reported scientific literature in the last decade on the pharmacophoric features of different heterocyclic anticonvulsants, which will help develop new anticonvulsants.
Topics: Humans; Anticonvulsants; Seizures; Pharmacophore; Electroshock; Phenobarbital
PubMed: 35366788
DOI: 10.2174/1871527321666220401115529 -
Drugs Apr 1984A considerable amount of information is now available concerning the clinical pharmacology of the anticonvulsant drugs. Some of the more important data are reviewed in... (Review)
Review
A considerable amount of information is now available concerning the clinical pharmacology of the anticonvulsant drugs. Some of the more important data are reviewed in this article. In recent years, valproic acid (or sodium valproate) has found a place as a major anticonvulsant agent, while older drugs such as troxidone and sulthiame seem to be disappearing from use. Although much information is available, the essential mechanisms of action of the anticonvulsant drugs are still not understood, either at a molecular or at an electrophysiological level. The pharmacokinetics of the anticonvulsants in common use are now reasonably well documented, though some minor questions are still to be answered. Numerous interactions between anticonvulsants and endogenous substances or other drugs administered concurrently (including other anticonvulsants) have been recorded, but much work still needs to be done to elucidate the frequency and mechanisms of the various interactions. Many adverse effects of the anticonvulsants are known, but further unwanted effects of long-established drugs continue to emerge from time to time, including the still somewhat controversial matter of anticonvulsant-related dysmorphogenesis. The use of valproic acid and its sodium salt has been associated with a worrying incidence of serious liver and pancreatic toxicity. Adequate basic data are now available to put the clinical use of anticonvulsants on a rational basis, but much work remains to be done in this area. In particular, the question of 'therapeutic ranges' of plasma concentrations of the various drugs needs to be reinvestigated in a rigorous statistical fashion, and in relation to different clinical types of epilepsy. The usefulness of monitoring free rather than total drug concentrations also needs further investigation. The ultimate test of the validity of all background scientific pharmacological information about anticonvulsants is its usefulness in the treatment of patients with epilepsy.
Topics: Absorption; Age Factors; Anticonvulsants; Bone and Bones; Chemical Phenomena; Chemistry; Drug Interactions; Drug Therapy, Combination; Epilepsy; Female; Fetus; Half-Life; Humans; Infant, Newborn; Kinetics; Liver; Male; Mononuclear Phagocyte System; Nervous System; Pregnancy; Protein Binding; Sex Factors; Synaptic Transmission; Tissue Distribution
PubMed: 6327221
DOI: 10.2165/00003495-198427040-00003 -
Current Topics in Medicinal Chemistry 2005The search for antiepileptic compounds with more selective activity and lower toxicity continues to be an area of intensive investigation in medicinal chemistry. This... (Review)
Review
The search for antiepileptic compounds with more selective activity and lower toxicity continues to be an area of intensive investigation in medicinal chemistry. This review describes new anticonvulsant agents representing various structures for which the precise mechanism of action is still not known. Many of the compounds presented in this review have been tested according to the procedure established by the Antiepileptic Drug Development Program of the Epilepsy Branch of the National Institute of Neurological Disorders and Stroke, National Institute of Health, USA. The newer agents include sulfonamides, amino acids, amides (analogs of gamma-vinyl GABA, N-benzylamides, 2,6-dimethylanilides, carboxyamides, hydroxyamides, alkanoamides); heterocyclic agents ((arylalkyl)imidazoles, pyrrolidin-2,5-diones, lactams, semi- thiosemicarbazones, thiadiazoles, quinazolin-4(3H)-ones, 2,5-disubstituted 1,2,4-thadiazoles, xanthones, derivatives of isatin) and enaminones. These new structural classes of compounds can prove useful for the design of future targets and development of new drugs.
Topics: Animals; Anticonvulsants; Drug Design; Drug Evaluation, Preclinical; Epilepsy; Humans; Structure-Activity Relationship
PubMed: 15638779
DOI: 10.2174/1568026053386944 -
The American Journal of Chinese Medicine 2018Traditional Chinese medicine (TCM) has a long history and been widely used in prevention and treatment of epilepsy in China. This paper is intended to review the... (Meta-Analysis)
Meta-Analysis Review
Traditional Chinese medicine (TCM) has a long history and been widely used in prevention and treatment of epilepsy in China. This paper is intended to review the advances in the active anticonvulsant compounds isolated from herbs in the prescription of TCM in the treatment of epilepsy. These compounds were introduced with the details including classification, CAS number specific structure and druggability data. Meanwhile, much of the research in these compounds in the last two decades has shown that they exhibited favorable pharmacological properties in treatment of epilepsy both in in vivo and in vitro models. In addition, in this present review, the evaluation of the effects of the anticonvulsant classical TCM prescriptions is discussed. According to these rewarding pharmacological effects and chemical substances, the prescription of TCM herbs could be an effective therapeutic strategy for epilepsy patients, and also could be a promising source for the development of new drugs.
Topics: Alkaloids; Anticonvulsants; Drug Combinations; Drugs, Chinese Herbal; Epilepsy; Flavonoids; Humans; Molecular Conformation; Phenols; Phytotherapy; PubMed; Triterpenes
PubMed: 29737210
DOI: 10.1142/S0192415X18500374 -
Journal of Enzyme Inhibition and... Dec 2018Epilepsy is one of the common diseases seriously threatening life and health of human. More than 50 million people are suffering from this condition and anticonvulsant... (Review)
Review
Epilepsy is one of the common diseases seriously threatening life and health of human. More than 50 million people are suffering from this condition and anticonvulsant agents are the main treatment. However, side effects and intolerance, and a lack of efficacy limit the application of the current anticonvulsant agents. The search for new anticonvulsant agents with higher efficacy and lower toxicity continues to be the focus and task in medicinal chemistry. Numbers of triazole derivatives as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have proved the importance of this heterocyclic nucleus in drug design and discovery. Recently many endeavours were made to involve the triazole into the anticonvulsants design, which have brought lots of active compounds. This work is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades.
Topics: Anticonvulsants; Epilepsy; Humans; Molecular Structure; Triazoles
PubMed: 29383949
DOI: 10.1080/14756366.2017.1423068 -
Current Developments in... 1981The literature concerning the relationship of anticonvulsant drugs to disturbances of behavior and cognitive abilities has been reviewed. It is indicated that although... (Review)
Review
The literature concerning the relationship of anticonvulsant drugs to disturbances of behavior and cognitive abilities has been reviewed. It is indicated that although completed studies are sparse and although many of the techniques currently used for evaluating the effects os such drugs on patients are inadequate, certain conclusions may be drawn. With regard to the effects on cognitive abilities, the drugs not only impair performance on psychological tests, but some drugs--particularly phenytoin--are associated with a progressive decline of intellectual abilities, which is often insidious and unrecognized. There is little systematic evidence to indicate which anticonvulsant drugs have adverse effects on behavior, but several studies have indicated improvements in behavior associated with carbamazepine and sulthiame. The possible reasons why anticonvulsant drugs should have those effects are discussed, and particularly the relationship of the drugs to abnormal folic acid and monoamine and metabolism are highlighted.
Topics: Animals; Anticonvulsants; Behavior; Behavior, Animal; Cognition; Epilepsy; Humans
PubMed: 7014113
DOI: 10.1007/978-94-011-8123-5_3 -
Mini Reviews in Medicinal Chemistry 2021Heterocyclic compounds and their derivatives gained more attention due to their valuable biological and pharmacological properties. Benzothiazole is a heterocyclic... (Review)
Review
Heterocyclic compounds and their derivatives gained more attention due to their valuable biological and pharmacological properties. Benzothiazole is a heterocyclic structure containing a bicyclic ring system with a large panel of applications. The benzothiazole is present in many new products undergoing research hoping that it possesses various biological activities. Epilepsy is a diverse group of diseases marked by neuronal excitability and hypersynchronous neuronal activity of motor, sensory or autonomic events with or without loss of consciousness. Presently, many antiepileptic drugs like lamotrigine, stiripentol tiagabine, pregabalin, felbamate, and topiramate are available and effective towards 60-80% of patients only, along with undesirable side effects, such as hepatotoxicity, gastrointestinal disturbance, drowsiness, gingival hyperplasia, and hirsutism. Thus, many attempts are still on-going to develop antiepileptic drugs with a safer profile. This review is mainly focused on the compilation of reported scientific literature data in the recent one-decade on the anticonvulsant activity of benzothiazole compounds.
Topics: Anticonvulsants; Benzothiazoles; Drug Development; Epilepsy; Humans; Molecular Structure
PubMed: 33355052
DOI: 10.2174/1389557521666201222145236 -
The Veterinary Clinics of North... Sep 2006This article reviews anticonvulsant therapies in current use for dogs and cats and briefly describes new modes of anticonvulsant therapy that are being investigated or... (Review)
Review
This article reviews anticonvulsant therapies in current use for dogs and cats and briefly describes new modes of anticonvulsant therapy that are being investigated or pending publication. Most of the information contained within the article is based on published information. Some of the information, however, is based on the author's clinical experience and is identified as such.
Topics: Animals; Anticonvulsants; Cat Diseases; Cats; Dog Diseases; Dogs; Epilepsy; Veterinary Drugs
PubMed: 16984829
DOI: 10.1016/j.cvsm.2006.05.005 -
Drug Research Mar 2022Epilepsy is one of the most common encountered neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting new... (Review)
Review
Epilepsy 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.
Topics: Anticonvulsants; Epilepsy; Humans; Seizures; Triazoles
PubMed: 34758502
DOI: 10.1055/a-1670-6992 -
Mini Reviews in Medicinal Chemistry 2016The derivatives of quinolinone and triazole exhibit antitumor, antiplatelet, antidepressant, and anticonvulsant properties in diverse experimental systems. In the past... (Review)
Review
The derivatives of quinolinone and triazole exhibit antitumor, antiplatelet, antidepressant, and anticonvulsant properties in diverse experimental systems. In the past decades, we have developed increasingly potent anticonvulsant agents by the structural modification of compounds derived from 3,4-DHQLO, triazole, and their analogs. Herein, we report the design and synthesis of a new series of 3,4-DHQLO and triazole and their derivatives; their anticonvulsant activity was evaluated. Moreover, we also reviewed the anticonvulsant activity of 3,4-DHQLO and triazole and their derivatives and new approaches.
Topics: Animals; Anticonvulsants; Drug Design; Epilepsy; Humans; Hydroquinones; Seizures; Structure-Activity Relationship; Triazoles
PubMed: 25553427
DOI: 10.2174/1389557515666150101100909