Advertisement

Topics

Design, synthesis and biological evaluation of some novel benzimidazole derivatives for their potential anticonvulsant activity.

Summary of "Design, synthesis and biological evaluation of some novel benzimidazole derivatives for their potential anticonvulsant activity."

Selective GABA(A) receptor ligands are widely used clinically to reduce the occurrence of convulsions. Hence there is an intense interest in developing new benzimidazole derivatives demonstrating high selectivity and high affinity for GABA(A) receptors. With the purpose of designing new chemical entities with an enhanced binding affinity for GABA(A)/BZd receptor complex, we carried out a QSAR study on benzotriazine derivatives. We studied 28 potent GABA(A) receptor ligands; derivatives of benzotriazines, using a combination of various tested physicochemical, steric, electronic and thermodynamic descriptors to determine the quantitative correlation between binding affinity and structural features. The developed and validated final model showed a good correlative and predictive ability expressed by a squared correlation co-efficient (r(2)) of 0.954. The equation indicated that the binding affinity is strongly dependent upon the thermodynamic properties (CDE, DDE and PC). Correlation between these properties and anticonvulsant activity was used to synthesize compounds possessing potent anticonvulsant activity. Most of the compounds showed an ability to inhibit the maximum electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions. Compound 1A, i.e. 2-(4-Chloro-phenyl)-5-nitro-1H-benzimidazole exhibited maximum activity in both the convulsion models.

Affiliation

Computational & Synthetic Laboratory, Department of Pharmaceutical Chemistry, VNS Institute of Pharmacy, Bhopal, 462 044, MP, India.

Journal Details

This article was published in the following journal.

Name: Archives of pharmacal research
ISSN: 0253-6269
Pages: 971-80

Links

DeepDyve research library

PubMed Articles [22587 Associated PubMed Articles listed on BioPortfolio]

Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.

Following our research for new melatonergic ligands, herein we report the design, synthesis and biological evaluation of new series of naphthofuranic derivatives as MT1 and MT2 ligands. Binding affini...

Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones.

The synthesis and antiproliferative activity of new benzimidazole derivatives bearing an hydrazone mojety at the 2-position is described. The new N'-(4-arylidene)-1H-benzo[d]imidazole-2-carbohydrazide...

Coumarin heterocyclic derivatives: chemical synthesis and biological activity.

Covering: 2000 to 2014This review highlights the broad range of science that has arisen from the synthesis of coumarin-linked and fused heterocycle derivatives. Specific topics include their synthesis...

Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.

Aminopeptidase N (APN/CD13) over-expressed on tumor cells and tumor microenvironment, plays critical roles in tumor invasion, metastasis and angiogenesis. Here we described the design, synthesis and p...

Recent Development of Benzimidazole-Containing Antibacterial Agents.

Clinically significant antibiotic resistance is one of the greatest challenges of the twenty-first century. However, new antibacterial agents are currently being developed at a much slower pace than o...

Clinical Trials [2881 Associated Clinical Trials listed on BioPortfolio]

A Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis

Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...

Coronally Advanced Flap in Combination With Acellular Dermal Matrix and Enamel Matrix Derivatives for Root Coverage

The aim of this study is to compare the clinical outcomes of root coverage procedures, using coronally advanced flap in combination with acellular dermal matrix with or without enamel ma...

Effect of Nutrition on Muscle Protein Synthesis

The present proposal is designed to examine the effect of carbohydrate and protein co-ingestion on muscle protein synthesis during endurance type exercise activities. We hypothesize that m...

Rate-limiting Amino Acids in Endurance-trained Athlete

Protein requirements in individuals who participate in endurance-based exercise training have been suggested to be greater than the current recommended dietary allowance (RDA). The biolog...

Muscle Glycogen Synthesis When Caffeine and Protein is Co-Ingested With Carbohydrates

The aim of the present study is to investigate the effect of added protein+leucine or caffeine to 1.2 g/kg/h CHO on the rate of post-exercise muscle glycogen re-synthesis in healthy, recre...

Medical and Biotech [MESH] Definitions

A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.

Derivatives of ethylene, a simple organic gas of biological origin with many industrial and biological use.

Architecture, exterior and interior design, and construction of facilities other than hospitals, e.g., dental schools, medical schools, ambulatory care clinics, and specified units of health care facilities. The concept also includes architecture, design, and construction of specialized contained, controlled, or closed research environments including those of space labs and stations.

The architecture, functional design, and construction of hospitals.

Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.

Quick Search
Advertisement
 


DeepDyve research library

Relevant Topic

Biological Therapy
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...


Searches Linking to this Article