Xian-Qing Deng

Bio: Xian-Qing Deng is an academic researcher from Jinggangshan University. The author has contributed to research in topics: Anticonvulsant & Docking (molecular). The author has an hindex of 7, co-authored 19 publications receiving 149 citations. Previous affiliations of Xian-Qing Deng include Yanbian University.

Recent developments on triazole nucleus in anticonvulsant compounds: a review

Abstract: 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.

Synthesis and Anticonvulsant Evaluation of some New 6-(Substituted-phenyl)thiazolo[3,2-b][1,2,4]triazole Derivatives in Mice.

Abstract: Epilepsy is the most frequent nearological affiction and afflicts 1% about of the worlds population. Currently there is an urgent need for the development of novel anticonvulsants with higher levels of potency and lower levels of toxicity. In this paper, a series of new 6-(substituted-phenyl)thiazolo[3,2-b][1,2,4]triazole derivatives were synthesized and tested for their anticonvulsant activities using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (PTZ) screens, which are the most widely employed seizure models for early identification of candidate anticonvulsants. Their neurotoxicity was determined applying the rotarod test. In these compounds, 6-(4-fluorophenyl)thiazolo[3,2- b][1,2,4]triazole (3c) showed selective protection against the MES seizures with an ED 50 value of 49.1 mg/Kg and a TD 50 value of 94.1 mg/Kg, which provided compound 3c a protective index (PI = TD 50 /ED 50 ) of 1.9 in the MES test. 6-(4-Propoxyphenyl)thiazolo[3,2-b][1,2,4]triazole (5b) was found to be active in both models, i.e. MES test and PTZ test. In the PTZ screen, compound 5b gave an ED 50 of 63.4 mg/Kg and a TD 50 of 105.6 mg/Kg, resulting in a PI value of 1.7 which is higher than carbamazepine.

Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4-triazolone moiety.

Abstract: A novel series of benzoxazole derivatives containing 1,2,4-triazolone (5a-m) was designed. These compounds were synthesized in order to screen their anticonvulsant activities by the maximal electroshock seizure (MES) model and the subcutaneous pentylenetetrazole (sc-PTZ) seizure model in mice. The rotarod test was used to evaluate their neurotoxicities. Most of the compounds showed anti-MES activities at 100 and 300 mg/kg. Compound 5f, which showed potential anticonvulsant activity in the MES model with ED50 values of 22.0 mg/kg, was considered as the most promising one in this study. It exhibited greater safety than that of carbamazepine and valproate regarding neurotoxicity. The efficacy of compound 5f in inhibiting the tonic seizures and death induced by the convulsants 3-mercaptopropionic acid and BIC was also verified. In an enzyme-linked immunosorbent assay, compound 5f and the positive drug phenytoin significantly increased the γ-aminobutyric acid (GABA) level in the mouse brain. Further, pretreatment with an inhibitor of the GABA synthesizing enzyme dramatically raised the ED50 value of 5f in the MES model. These results confirmed that the compound 5f plays its anticonvulsive action via regulating the GABA function in the brain. Also, a docking study of the compound 5f in the benzodiazepine (BZD) binding site of the GABAA receptor confirmed possible binding of the compound 5f with BZD receptors.

Synthesis and evaluation of anticonvulsant and antidepressant activities of 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives

Abstract: Seventeen 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives were synthesized, and their anticonvulsant and antidepressant activities were evaluated in a mouse model. The anticonvulsant effect and neurotoxicity of the compounds were evaluated with a maximal electroshock test and a rotated test in mice, respectively. Most of the compounds had anticonvulsant activity; among the compounds studied, 7-(3-chlorobenzyl)-7H-tetrazolo[1,5-g]purine (3h) was found to be the most potent compound with a median effective dose (ED50) value of 28.9 mg/kg and a protective index value of 15.8, possessing better anticonvulsant activity and higher safety than the marketed drug carbamazepine. To explain the possible mechanism of anticonvulsant activity, compound 3h was tested in pentylenetetrazole-induced seizures tests, and the results suggest that compound 3h exerts anticonvulsant activity through a GABA-mediated mechanism. Forced swimming test showed that at a dose of 40 mg/kg, five compounds have significant antidepressant activity, the most active compound was 7-(2-chlorobenzyl)-7H-tetrazolo[1,5-g]purine (3g), which decreased immobility time by 56 %.

Harrison's Principles of Internal Medicine

Abstract: The 11th edition of Harrison's Principles of Internal Medicine welcomes Anthony Fauci to its editorial staff, in addition to more than 85 new contributors. While the organization of the book is similar to previous editions, major emphasis has been placed on disorders that affect multiple organ systems. Important advances in genetics, immunology, and oncology are emphasized. Many chapters of the book have been rewritten and describe major advances in internal medicine. Subjects that received only a paragraph or two of attention in previous editions are now covered in entire chapters. Among the chapters that have been extensively revised are the chapters on infections in the compromised host, on skin rashes in infections, on many of the viral infections, including cytomegalovirus and Epstein-Barr virus, on sexually transmitted diseases, on diabetes mellitus, on disorders of bone and mineral metabolism, and on lymphadenopathy and splenomegaly. The major revisions in these chapters and many

The Pharmacological Basis of Therapeutics

Abstract: The Pharmacological Basis of Therapeutics A Textbook of Pharmacology, Toxicology and Therapeutics for Physicians and Medical Students. By Prof. Louis Goodman and Prof. Alfred Gilman. Pp. xiii + 1383. (New York: The Macmillan Company, 1941.) 50s. net.

Genetics of epilepsy

Abstract: The last decade has witnessed rapid advances in understanding the role of genetic factors in epilepsy. Mutations and chromosomal defects underlying many inherited symptomatic epilepsies have now been identified, and several genes have been associated with rare idiopathic epilepsies transmitted in a mendelian manner. However, the genetic factors underlying inherited susceptibility to idiopathic epilepsy remain to be identified. The International League Against Epilepsy (ILAE) Classification of epileptic syndromes (published in 1989) divides seizure disorders along two main axes. First, epilepsies are classified as idiopathic, symptomatic or cryptogenic, and second, they are either generalised or focal. Within this classification, genetic factors have conventionally been thought to play the largest role in the idiopathic generalised epilepsies. A genetically determined increased excitability of neuronal circuits provides an attractive explanation why otherwise normal individuals should develop unprovoked seizures without an identifiable focus of onset. This view has, moreover, been supported by the finding that concordance rates for idiopathic generalised epilepsy are elevated among first degree relatives, and more so among monozygotic twins. Similar arguments and evidence apply to febrile seizures, which do not count as an epilepsy syndrome as such. However, recent studies have shown that genetic factors also play an important role in cryptogenic epilepsy (seizure disorders where a syndromic diagnosis is not possible), and also contribute to several partial epilepsies. Also single gene defects have been identified in a small number of families with epilepsy inherited in an autosomal dominant fashion. These rare monogenic epilepsies have shed a new light on the mechanisms by which disorders of neuronal function can cause epilepsy. Major advances have also been made in establishing the cause of a number of rare but often severe symptomatic epilepsies. This article will begin by considering a few genes responsible for symptomatic epilepsy, and then address recent progress in the …