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Central Nervous System Agents in Medicinal Chemistry

Klaudia T Amakali, Lesetja Jan Legoabe, Anel Petzer, Jacobus P Petzer
Chalcone has been identified as a promising lead for the design of monoamine oxidase (MAO) inhibitors. This study attempted to discover potent and selective chalcone-derived MAO inhibitors by synthesising a series consisting of various cyclic chalcone derivatives. The cyclic chalcones were selected based on the possibility that their restricted structures would confer a higher degree of MAO isoform selectivity, and included the following chemical classes: 1-indanone, 1-tetralone, 1-benzosuberone, chromone, thiochromone, 4-chromanone and 4-thiochromanone...
May 1, 2018: Central Nervous System Agents in Medicinal Chemistry
Idalet Engelbrecht, Jacobus P Petzer, Anel Petzer
The efficacy of L-dopa in the treatment of Parkinson's disease depends on its metabolic conversion to dopamine in the brain, however extensive peripheral metabolism of L-dopa diminishes its availability for uptake into the brain. L-Dopa is extensively decarboxylated in the gastrointestinal tract and peripheral tissues by aromatic L-amino acid decarboxylase (AADC), and AADC inhibitors are thus frequently combined with L-dopa therapy. When AADC is inhibited, 3-O-methylation catalysed by catechol-O-methyltransferase (COMT) becomes a dominant metabolic pathway for L-dopa, and COMT inhibitors may thus also be used as adjuncts to L-dopa in Parkinson's disease...
April 26, 2018: Central Nervous System Agents in Medicinal Chemistry
Meenakshi Gupta, Kamal Kant, Ruchika Sharma, Anoop Kumar
INTRODUCTION: Parkinson's disease is affecting millions of people worldwide. The prevalence of Parkinson's disease is 0.3% globally, rising to 1% in more than 60 years of age and 4% in more than 80 years of age and the figures are thought to be doubled by 2030. Thus, there is a great need to identify novel therapeutic strategies or candidate drug molecule which can rescue neuronal degeneration. β-asarone has potential to act as a neuroprotective agent but regarding its role in Parkinson disease, very few reports are available...
April 16, 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
Rameshwar S Cheke, Sandip D Firke, Ravindra R Patil, Sanjay B Bari
Epilepsy is one of the most significant chronic neurological disorders with high occurrence worldwide. Many epileptic patients are not completely treated with currently available marketed drugs as well as so many drugs have shown unfavorable side effect and drug interaction. Therefore, there are continuing interests to find new anticonvulsant drugs. Recently, there has been wide interest in compounds containing the isatin moiety with diverse biological effects. In view of the previous continuation of an ongoing program aiming at finding new structure leads to potential anticonvulsant activities, we are trying to compile recent efforts which have been made in the design and development of isatin derived anticonvulsant agents...
November 13, 2017: Central Nervous System Agents in Medicinal Chemistry
Amit Kumar Keshari, Aseem Tewari, Shweta Singh Verma, Shailendra K Saraf
BACKGROUND: Mannich bases are known to be an important pharmacophore or bioactive leads in the synthesis of various potential agents that have a variety of therapeutic activities like anticancer, antipsychotic, anticonvulsant, antimalarial, anti-inflammatory, antibacterial and so forth. Thus, in the present research, conjugation of moieties like 1,5-benzoxazepines and 1,5-benzothiazepines with secondary amines like piperazine, methyl piperazine and morpholine was carried out in a Mannich base with an anticipation of good anticonvulsant activity...
July 17, 2017: Central Nervous System Agents in Medicinal Chemistry
C S Ananda Kumar, B Veeresh, K C Ramesha, C S Ashok Raj, K M Mahadevaiah, S B Benaka Prasad
A series of novel diazaspiro compounds 6a-t were synthesised and biologically evaluated for their anticonvulsant activity in the maximal electroshock seizure (MES) assay. Most of the tested compounds exhibited moderate to weak activity in the MES screen test, The compounds 6f, 6h, 6i, 6j, 6p, 6s and 6n able to protect seizure effect significantly higher and this effect was similar when compared to standard drug treated rats.
July 12, 2017: Central Nervous System Agents in Medicinal Chemistry
Saganuwan Alhaji Saganuwan
Central nervous system (CNS) disorders are on increase perhaps due to genetic, enviromental, social and dietetic factors. Unfortunately, a large number of CNS drugs have adverse effects such as addiction, tolerance, psychological and physical dependence. In view of this, literature search was carried out with a view to identifying functional chemical groups that may serve as lead molecule for synthesis of compounds that may have CNS activity. The search revealed that heterocycles that have heteroatoms such as nitrogen (N), sulphur (S) and oxygen (O) form the largest class of organic compounds...
May 2, 2017: Central Nervous System Agents in Medicinal Chemistry
Airy Sanjeev, Venkata Satish Kumar Mattaparthi
Amyloid fibrils represent stable form of many misfolded proteins associated with numerous diseases like Parkinson's disease(PD),Type II diabetes and Alzheimer's disease(AD). Lewy Bodies(LB) are the pathological hallmark of PD where long fibrils disrupting the brain's activity that constitutes the main component, α-synuclein. However α-synuclein structure has eluded researchers due to its complexity, insolubility and difficulty of characterizing one protein within a fibril. Recently, a high resolution structure of α-synuclein protein that stacks together forming fibrils in brains of PD patients was identified...
April 27, 2017: Central Nervous System Agents in Medicinal Chemistry
Enrico Mongeau, Gengyang Yuan, Zachary Minden, Scott Waldron, Raymond Booth, Daniel Felsing, Mary Jo Ondrechen, Graham B Jones
The benzoxazepine JL13 is an analogue of the clozapine family which targets the 5-HT2A receptor, and has showed promise as an atypical antipsychotic agent. Following structure function analysis with a series of synthetic analogues, homology modeling was performed to determine key interaction sites with the receptor. An aza analogue was synthesized for evaluation, and demonstrated seventeen times greater affinity for the receptor. An improved synthetic route was developed to allow rapid modifications of the core and synthesis of related libraries...
April 26, 2017: Central Nervous System Agents in Medicinal Chemistry
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