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Central Nervous System Agents in Medicinal Chemistry

K Shinomol George, S Sunitha, Pankaj Satapathy, Ishtapran Sahoo, Farhan Zameer
Acrylamide is widely found in baked and fried foods, produced in large amount in Industries and is a prime component in toxicity. This review highlights various toxicities that are induced due to acrylamide, its proposed mode of action including oxidative stress cascades and ameliorative mechanisms using phytochemicals. Acrylamide formation, the mechanism of toxicity and the studies on the role of oxidative stress and mitochondrial dysfunctions are elaborated in this paper. The various type of toxicity caused by Acrylamide and the modulation studies using phytochemicals that are carried out on various type of toxicity like neurotoxicity, hepatotoxicity, cardiotoxicity, immune system, and skeletal system, as well as embryos have been explored...
February 7, 2019: Central Nervous System Agents in Medicinal Chemistry
Bijo Mathew
Due to the structural versatile, chalcones are considered as multi-targeted scaffold for the variety of enzyme targets. The present perspective focused our attention onto the monoamine oxidase inhibitory activity of synthetic chalcones which is synthesized in our lab recently. The studies clearly demonstrated that most of the chalcones showed selective, reversible and potent MAO-B inhibition compared to MAO-A depending upon the substituents bearing around α-β-unsaturated linker of the chalcone scaffold.
January 31, 2019: Central Nervous System Agents in Medicinal Chemistry
Da-Yong Lu, Peng-Peng Zhu, Hong-Ying Wu, Nagendra Sastry Yarla, Bin Xu, Jian Ding, Ting-Ren Lu
Suicide is still a major event of human mortality (2 %) worldwide. However, no magic bullet (high efficacy drug targeting suicide categories >80%) has been developed due to limitation of biological knowledge of suicide events and pharmacological progress. Influenced by complex environmental factors, social-economic conditions, diverse suicidal-associated genes/molecules, drug development grows slowly and narrow-spectra. In search of pharmaceutical options against human suicide, an accelerating pace of transition from psychoanalysis (cognitive, behavior and emotional) into psycho-morphology disciplines (genetics/image) through neurobiology study (neural-transmitter, receptors and different neural-locations) is more potential now...
January 15, 2019: Central Nervous System Agents in Medicinal Chemistry
Gokul Krishna, Ravikumar Hosamani, Muralidhara
Parkinson`s disease (PD) is characterized by alterations in cerebellum and basal ganglia functioning with corresponding motor deficits and neuropsychiatric symptoms. Involvement of oxidative dysfunction has been implicated for the progression of PD, and environmental neurotoxin exposure could influence such behavior and psychiatric pathology. Assessing dietary supplementation strategies with naturally occurring phytochemicals to reduce behavioral anomalies associated with neurotoxin exposure would have major clinical importance...
January 15, 2019: Central Nervous System Agents in Medicinal Chemistry
Neeraj Mishra, Sawarni Sharma, Rahul Deshmukh, Anoop Kumar, Ruchika Sharma
Introduction Parkinson's disease (PD) is one of the most common age-related neurodegenerative disorders which are marked with the loss of dopaminergic neurons. Present study performed on the nose to brain delivery of selegiline hydrochloride loaded nano lipid carrier, suggests that the nasal route is a good mean of targeting the drug directly into the brain. Method and Materials Nanostructured lipid carriers were prepared by using hot homogenization. Selegiline hydrochloride loaded NLCs and rotenone treatment were given at a dose of 10 mg/kg administered from 14th day to 28th day...
November 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Meena K Yadav, Laxmi Tripathi
N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin-2-yl] methyl}, 2-[(2-isopropyl-5-methyl) 1-cyclohexylidene] hydrazinecarboxamide QS11 was designed by computational study. It possessed essential pharmacophoric features for anticonvulsant activity and showed good docking with iGluRs (Kainate) glutamate receptor. QSAR and ADMET screening results suggested that QS11 would possess good potency for anticonvulsant activity. QS11 was synthesised and evaluated for its anticonvulsant activity and neurotoxicity. QS11 showed protection in strychnine, thiosemicarbazide, 4-aminopyridine and scPTZ induced seizure models and MES seizure model...
November 22, 2018: Central Nervous System Agents in Medicinal Chemistry
Della Grace Thomas Parambi, Fakhrya Aljoufi, Vikneswaran Murugaiyah, Githa Elizabeth Mathew, Sanal Dev, B Lakshminarayanan, Omnia Magdy Hendawy, Bijo Mathew
Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD). The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated. Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively...
November 18, 2018: 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
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