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Start Over Author "Borcan F" Journal mini reviews in medicinal chemistry
2 results on '"Borcan F"'

1. Evaluation of the Pharmacological Descriptors Related to the Induction of Antidepressant Activity and its Prediction by QSAR/QRAR Methods

Author

Avram, S., Buiu, C., Duda-Seiman, D., Duda-Seiman, C., Borcan, F., and Mihailescu, D.

Abstract

Antidepressants are psychiatric agents used for the treatment of different types of depression, being at present amongst the most commonly prescribed drugs, while their effectiveness and adverse effects are still the subject of many studies. To reduce the inefficiency of known antidepressants caused by their side-effects, many research efforts have recently focused on the development of improved strategies for new antidepressants drug design. For this reason it is necessary to apply very fast and precise techniques, such as QSAR (Quantitative Structure-Activity Relationships) and QRAR (Quantitative Retention-Activity Relationship), which are capable to analyze and predict the biological activity for these structures, taking in account the possible changes of the molecular structures and chromatographic parameters. We discuss the pharmaceutical descriptors (van der Waals, electrostatic, hydrophobicity, hydrogen donor/acceptor bond, Verloops parameters, polar area) involved in QSAR and also chromatographic parameters involved in QRAR studies of antidepressants. Antidepressant activities of alkanol piperazine, acetamides, arylpiperazines, thienopyrimidinone derivatives (as preclinical antidepressants) and also the antidepressants already used in clinical practice are mentioned.

Published
2012

2. QSAR Approaches Applied to Antidepressants Induced Neurogenesis--in vivo and in silico Applications.

Author

Avram S, Borcan F, Borcan LC, Milac AL, and Mihailescu D

Subjects
Antidepressive Agents pharmacology, Humans, Protein Binding drug effects, Receptor, Serotonin, 5-HT1A metabolism, Receptors, sigma metabolism, Sigma-1 Receptor, Antidepressive Agents adverse effects, Models, Biological, Neurogenesis drug effects, Quantitative Structure-Activity Relationship
Abstract

Brain presents very complex advanced protective mechanisms. However, these mechanisms occasionally fail due to risk factors represented by genetic, environmental or social stress and consequently, severe psychiatric disorders such as depression, schizophrenia or psychotic depression are induced. Under such circumstances, latest strategies in experimental and in silico neuroscience consider essential to identify new applications of already clinically-approved drugs for the treatment of psychiatric disorders but also as promoters of neurogenesis and neurites outgrowth. Results of recent studies suggested that antidepressants are able to induce neurogenesis and neurites outgrowth by their agonistic effects on 5-hydroxytryptamine receptor (5-HT), especially 5-HT 1A, and sigma1 receptor (σ1R), but many molecular aspects of these processes are still unclear. Here we present structural aspects of molecular complexes (5-HT 1A and σ1R and their ligands) revealed by experimental and in silico studies. Here we present the chemical structures-biological activity relationship (SAR) of these molecules revealed by recent experimental and in silico studies, offering a new perspective on the antidepressants mechanism as neurogenesis and neurites outgrowth promoters.

Published
2015
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