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Central Nervous System Agents in Medicinal Chemistry

Siva G Somasundaram, Cristian Muresanu, Pamela Schield, Alfiya Makhmutovа, Elena V Bovina, Vladimir P Fishenko, Nusrat F Hasanov, Gjumrakch Aliev
The pathophysiology of the intervertebral discs plays a significant role in the people's life quality. There is not adequate research done in the pathogenesis and treatment of intervertebral disc degeneration. Alternately, self-educated physiology offers a novel and noninvasive method to reverse the degenerated discs. In this single case study report attempts have been made to highlight the effect of the self-educative physiology, on magnetic resonance imaging investigations, of progressive healing, on the degenerated intervertebral discs...
October 17, 2018: Central Nervous System Agents in Medicinal Chemistry
Airy Sanjeev, Venkata Satish Kumar Mattaparthi
BACKGROUND: α-Synuclein (αS) is the precursor protein present in Lewy Bodies that helps in the formation of highly ordered amyloid fibrils that is associated with the occurrence of Parkinson's disease, a neuro-degenerative disorder. Many reports have now been focused on finding the probable targets to weaken this debilitating disease. Recently γ-synuclein (γS), a presynaptic protein, was highlighted to inhibit the aggregation propensity of αS both in vivo and in vitro. However the nature, location and specificity of molecular interactions existing between the αS and γS is not known in spite of the potential importance of γS as an inhibitor of αS...
October 12, 2018: Central Nervous System Agents in Medicinal Chemistry
Dheyauldeen Shabeeb, Masoud Najafi, Mansor Kashavarz, Gholamreza Hasanzadeh, Mohammed Reza Hadian, Alireza Shirazi
Peripheral nerve lesion is a common clinical problem that may produce long-term functional defects. Usually, crush injuries, fractures, scars, lacerations, compression, or iatrogenic reasons are reasons of nerve injuries. Unsuccessful treatment of nerve injuries causes partial or total loss of sense, motor, and autonomic functions. Despite widespread experimental studies that aimed to improve nerve healing, healing results for peripheral nerve injuries are hardly reasonable. The successes of the regenerative procedure of the nerve repair in experimental research, with topical agents, can be assessed using different methods such as morphological, electrophysiological, biochemical and functional evaluation...
August 29, 2018: Central Nervous System Agents in Medicinal Chemistry
Oleg A Raevsky, Veniamin Y Grigorev, Alexander V Yarkov, Daniel E Polianczyk, Vadim V Tarasov, Elena V Bovina, Elena N Bryzhakina, John C Dearden, Marco Avila-Rodriguez, Gjumrakch Aliev
One promising target for novel psychotropic drugs is the 5-HT6 receptor, G-protein-coupled receptor (GPCR) family, displaying seven transmembrane domains. There is considerable interest in how both 5-HT6 receptor agonist and antagonist compounds can have marked pro-cognitive effects. An exact structure of the 5-HT6 receptor is not available, so application of powerful methods of (Q)SAR and molecular modelling, which play an essential role in modern drug design, are currently limited to structure-based homology models...
August 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Da-Yong Lu, Peng-Peng Zhu, Hong-Ying Wu, Nagendra Sastry Yarla, Bin Xu, Ting-Ren Lu
INTRODUCTION: Suicide is still a major event of human mortality worldwide. Yet human suicide prediction, prevention and therapeutic systems at this moment are generally ineffective in the clinic. No diagnostic system is reliable for significantly suicidal prevention and mortality reduction. As a result, human suicide etiopathologic investigation (especially at genetic/molecular levels in the clinical settings) is quite necessary. In order to boost human suicide researches, emerging human suicide diagnostic/treatment study will be transformed from clinical symptom observations into new generations of candidate drug targets and therapeutics...
August 16, 2018: Central Nervous System Agents in Medicinal Chemistry
Yuri Utkin
INTRODUCTION: The brain is the most complicated organ in a vertebrate's organism. In a human, it contains about two hundred billions of neurons and non-neuronal cells. To understand the mechanisms of the brain functions is the great challenge for the researchers. Much is already done on this way; however, it remains a lot to do still, and to get deeper knowledge, new approaches should be developed. One of this is to use benefits that nanotechnology brings in this area. Nanotechnology opens up unique opportunities, not only for material science research, but also for biology, medicine, and many other disciplines...
August 13, 2018: Central Nervous System Agents in Medicinal Chemistry
O J Onaolapo, A Y Onaolapo, O A Adeyeba
BACKGROUND: Recorded history shows that malaria has plagued mankind for centuries, if not millennia, with the disease infecting and affecting several body tissues, organs and systems; including the central nervous system. Cerebral malaria is a severe form of malaria that may be associated with acute and chronic general behavioural, neurological or neuropsychiatric manifestations. The observation that the use of certain antimalaria drugs may also be associated with behavioural, neurochemical and structural brain changes complicates the picture, as both the infection and its treatment may cause significant changes in brain structure/function and behaviour...
July 16, 2018: Central Nervous System Agents in Medicinal Chemistry
Pricila Pfluger, Vanessa Rodrigues Coelho, Gabriela Gregory Regner, Lucas Lima da Silva, Karina Martinez, Alan Fonseca, Cassiana Macagnan Viau, Patricia Pereira
BACKGROUND: Gamma-decanolactone (GD) is a monoterpene compound that presents anticonvulsant effect in acute and chronic models of epilepsy and it acts as a noncompetitive glutamate antagonist. OBJECTIVE: This study evaluated the anticonvulsant profile and the possible mechanism of action of GD in seizures induced by isoniazid (INH; 250 mg/kg), picrotoxin (PCT; 5 mg/kg) and 4-aminopyridine (4-AP; 13 mg/kg) in male mice. METHOD: Thirty minutes before the convulsants administration, animals received a single administration of saline, GD (100 or 300 mg/kg) or the positive control diazepam (DZP; 2 mg/kg)...
June 10, 2018: Central Nervous System Agents in Medicinal Chemistry
Dusanka S Skundric
No abstract text is available yet for this article.
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Gregory S Hamilton
No abstract text is available yet for this article.
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Saganuwan A Saganuwan
BACKGROUND: The transport of CNS acting drugs across blood-brain barrier (BBB) is complex and guided by the molecular weight, pH, physicochemical and pathological state of the BBB among others. METHODS: In view of this, literatures were assessed for possible conversion of Non-CNS to CNS acting drugs, whose ability to penetrate CNS can be improved using polymers for biomedical applications. RESULTS: The findings have shown that compounds with pyridine, pyrrole, carboxamide, pyridone among others can be converted to CNS acting drugs that can be loaded in specialized carrier polymers for transportation across BBB...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Nimisha Jain, Jugnu Jaiswal, Ashish Pathak, Pradeep K Singour
BACKGROUND: According to the WHO, around 50 million people worldwide are suffering from epilepsy. It is due to the repeated occurring of seizures. These seizures are caused by sudden which may vary from a brief lapse of attention or muscle jerks, to severe and prolonged convulsions. OBJECTIVES: The aim of the present work was to synthesize 2-phenyl substituted quinazolinone derivatives and to evaluate them for anticonvulsant and neurotoxic activity. METHODS: A series of novel 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Dusanka S Skundric
INTRODUCTION: This overview is aimed at reevaluating fundamental approaches of current MS therapies with focus being placed on their targeted underlying immune, molecular and cellular mechanisms. Currently used therapies are discussed in regard to their mechanisms of action, clinical accomplishments and unwanted side effects and complications. Special emphasis is given to the current first generation Disease Modifying Therapies (DMT) and their actions at immune mechanisms of disease. Effects of DMT on CD4+Th1 cells and their associated cytokines and signaling pathways are discussed in more detail...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Rodrigo E Gonzalez-Reyes, Maria G Rubiano
BACKGROUND: Adequate function of the nervous system depends on the balance of glianeuron complex interactions. Astrocytes, in particular, are key elements in this process due to the significant participation of these cells in essential properties of the nervous system such as neuroinflammation, regulation of neurotransmitters, release of gliotransmitters and control of synaptic plasticity, among others. Astrocytes express the receptor for advanced glycation end products (RAGE) which is very important in the recognition of endogenous molecules released in the context of infection, physiological stress or chronic inflammation...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Mohammad R Shokrollahi, Khalil Shabanzadeh, Samileh Noorbakhsh, Azardokht Tabatabaei, Zahra Movahedi, Ahmad R Shamshiri
BACKGROUND AND OBJECTIVE: Bacterial meningitis is a serious disease with high rate of mortality and morbidity in children. Invasion of pathogens causes brain and meningeal inflammation, which leads to the release of biomarkers into cerebrospinal fluid (CSF). Identification of these biomarkers can help the physicians to differentiate between bacterial and aseptic meningitis. In the current study, some of these biomarkers such as Procalcitonin, C reactive protein (CRP), and Ferritin, were compared in cerebrospinal fluid (CSF) of patients with bacterial and aseptic meningitis...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Veronica R Alonso, Jose de Jesus Flores Rivera, Yamel R Garci, Julio Granados, Thalia Sanchez, Lourdes Mena-Hernandez, Teresa Corona
INTRODUCTION: Neuromyelitis optica (NMO) and Multiple Sclerosis (MS) have been reported in different populations. NMO is more frequent in non-Caucasians, and clinical phenotype differences between populations are likely influenced by genetic susceptibility. In Brazil, it has been reported that NMO patients have a mainly European ancestry background. Like other autoimmune diseases, NMO has a multifactorial origin (i.e., genetics, environmental and infectious factors). Regarding the genetics of NMO, epidemiological findings suggest that a polygenic background has an important role in the development of this type of disease...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Yamel Rito, Ivan Torre-Villalvazo, Jose Flores, Veronica Rivas, Teresa Corona
INTRODUCTION: Multiple Sclerosis (MS) is a chronic, inflammatory, neurodegenerative demyelinating disease of the central nervous system (CNS). Unfortunately, MS causes important disability in young adults and its prevalence is increasing. While the etiology of MS etiology is not completely understood, it seems to be a multifactorial entity that is influenced by both genetic and epigenetic modifications. Epigenetic mechanisms add or remove different chemical groups for the activation or inhibition of gene expression to block the production of proinflammatory proteins...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Yara D Fragoso
BACKGROUND: Chronic demyelinating diseases of the central nervous system (CNS) are autoimmune conditions that, although rarely fatal, may lead to severe disability. Among these diseases, Multiple Sclerosis (MS) and neuromyelitis optica (NMO) are particularly important and subject of worldwide research. MS and NMO are chronic types of CNS disease, with recurrent episodes of demyelination. For many years, these two conditions were considered to be only one, but lately it is known that they have different epidemiological, physiopathological and prognostic characteristics...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Rosa M Gomez, Kemel Ghotme, Jackeline J Nino, Maria Quiroz-Padilla, Daniela Vargas, Andy R Dominguez, George E Barreto, Magdy Y Sanchez
BACKGROUND: A complete neurological exam contributes in establishing spinal cord injury severity and its extent by identifying the damage to the sensory and motor pathways involved in order to address a more case-specific and precise pharmacological therapy. However, assessment of neurologic function in spinal cord injury models is usually reported by using sensory or motor tests independently. METHODS: A reliable integral method is needed to precisely evaluate location and severity of the injury at baseline and, in further assessments, to establish the degree of spontaneous recovery...
January 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Pooja Mishra, Seema Kesar, Sarvesh K Paliwal, Monika Chauhan, Kirtika Madan
BACKGROUND: Glycogen synthase kinase-3β plays a significant role in the regulation of various pathological pathways relating to the Central Nervous System (CNS). Dysregulation of Glycogen synthase kinase 3 (GSK-3) activity gives rise to numerous neuroinflammation and neurodegenerative related disorders that affect the whole central nervous system. OBJECTIVE: By the sequential application of in-silico tools, efforts have been attempted to design the novel GSK-3β inhibitors...
2018: Central Nervous System Agents in Medicinal Chemistry
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