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Central Nervous System Agents in Medicinal Chemistry

Dusanka Skundric
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 current disease modifying therapies (DMT) and their actions at immune mechanisms of disease. Effects on DMT on CD4+Th1 cells and related cytokine and signaling pathways are discussed in more detail...
October 18, 2016: Central Nervous System Agents in Medicinal Chemistry
Poonam Piplani, Chhanda Charan Danta
BACKGROUND: In 2016, the statistical reports stated that Alzheimer is not just memory loss but it kills and has become the 6th leading cause of death. The number of dementia patients is increasing rapidly and expected to rise to 131.5 million by 2050. Still there is not a drug candidate that can cure the cognitive deficits completely. OBJECTIVE: Series of novel piperazine derivatives have been designed, synthesized and evaluated for cognition enhancing activity...
October 14, 2016: Central Nervous System Agents in Medicinal Chemistry
Laura Betti
No abstract text is available yet for this article.
September 8, 2016: Central Nervous System Agents in Medicinal Chemistry
Marcella Reale, Talma Brenner
The nicotinic acetylcholine receptor (nAChR) gene family encodes for subunits of acetylcholine gated ion channels. These receptors are expressed widely and have many functions: They mediate excitation at neuro-muscular junctions. In the central nervous system nAChRs have been implicated in memory, cognition, and addiction. And in non-excitatory cells they regulate differentiation, proliferation and inflammatory responses. The CHRNA7 gene encodes for the a7 nAChR subunit that assembles into a homomeric receptor having unusual properties...
August 29, 2016: Central Nervous System Agents in Medicinal Chemistry
Marcella Reale, Elanur Aydin
Thymol (THY), which is a monocyclic monoterpene, is one of the major constituent of the essential oils of thyme and origanum. To date, although various biological activities of THY have been demonstrated, its neurotoxicity has never been explored. We aimed to describe in vitro antiproliferative and/or cytotoxic properties (by 3-(4,5 dimetylthiazol-2-yl)-2,5 diphenlytetrazolium bromide (MTT) test), genotoxic damage potentials (by single cell gel electrophoresis (SCGE)) and oxidative effects (by total antioxidant capacity (TAC) and total oxidative stress (TOS) analysis) of THY...
August 23, 2016: Central Nervous System Agents in Medicinal Chemistry
Marcella Reale, Jole Fiorito
BACKGROUND: MRJF4, a novel haloperidol metabolite II prodrug, was obtained through the esterification of the secondary hydroxyl group of haloperidol metabolite II with 4-phenylbutyric acid. The activities of (±)-MRJF4 and its two enantiomers [(+)-MRJF4 and (-)-MRJF4] as tumor specific inducers of pro-apoptotic genes were evaluated on malignant C6 glioma cells. In particular, changes in Nf-kB signaling pathway, activity of nitric oxide synthases (NOS), metalloproteinases (MMPs), and membrane adhesion proteins were investigated...
August 23, 2016: Central Nervous System Agents in Medicinal Chemistry
Maria Di Bari, Giovanni Di Pinto, Marcella Reale, Guadalupe Mengod, Ada Maria Tata
Multiple sclerosis (MS) is an inflammatory and neurodegenerative disease of the central nervous system (CNS) characterized by leucocytes infiltration, demyelination, axonal degeneration and neuronal death. Although the etiology of MS is still unknown, inflammation and autoimmunity are considered to be key players of the disease. The severe alterations affecting the nervous system contribute to the motor and cognitive disabilities and are in large part dependent on severe inflammatory processes active in both central nervous system and immune system...
August 22, 2016: Central Nervous System Agents in Medicinal Chemistry
Himanshu Sharma
Background-The Placebo is defined as an inert substance with a potent therapeutic effect. Its effect is attributed to its psychological and neurobiological effect. Its use in Psychiatric drug practice in drug trials and clinical practice is common, especially in India .Currently there is a debate whether to use it or not as there are ethical, moral and legal issues. Also, its mechanism of action is not known. Discussion-The Indian Psychiatry scenario is muddled in relation to use of placebo in Randomized Controlled Trials or Psychiatric clinical practice...
August 10, 2016: Central Nervous System Agents in Medicinal Chemistry
Marcella Reale, Ada Maria Tata
The α7 nicotinic receptor consists of identical subunits and is one of the most abundant acetylcholine receptor in the mammalian central nervous system. However its expression is also found in the peripheral nervous system as well as in the immune system and various peripheral tissues. Its function is involved in the regulation of a range of activities such as classical excitatory neurotransmission in some brain regions, modulation of the release of several neurotransmitters, regulation of neurite outgrowth, and even neuronal survival/death...
July 29, 2016: Central Nervous System Agents in Medicinal Chemistry
A S Saganuwan
The use of Central nervous system acting drugs in the management of new degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical structure of piroxicam can be modified to yield new CNS stimulants and depressants that can be of great benefit to man and animals.
July 19, 2016: Central Nervous System Agents in Medicinal Chemistry
Ivana Cacciatore, Erika Fornasari, Lisa Marinelli, Antonio Di Stefano, Piera Eusepi, Hasan Turkez, Stefania Fulle, Ester Sara Di Filippo, Andrea Scarabeo
BACKGROUND: Medicinal chemistry approaches are presently under investigation to develop new multifunctional drugs able to simultaneously reduce oxidative stress, excitotoxicity, metal dyshomeostasis, and neuroinflammation that characterize neuropathological conditions, such as Alzheimer's Disease. RESULTS: Memantine (MEM) derivatives 1-6 were designed and synthesized as novel multifunctional entities with antioxidant and neuroprotective capabilities to manage neurodegenerative diseases, such as Alzheimer's Disease...
June 25, 2016: Central Nervous System Agents in Medicinal Chemistry
Y Echeverri Olga, A Salazar Diego, Alexander Rodriguez-Lopez, González Janneth, J Almeciga-Diaz Carlos, A Barrera Luis
The nervous system is responsible for the communication between the organism and its environment. This task is possible by the presence of the myelin sheath, which is a double membrane formed by about 75% lipids and 25% proteins. The sulfatide represents one of the main lipids of the myelin band; its degradation is catabolized by the enzyme Arylsulfatase A (ARSA), to generated galactosylceramide. Mutations affecting ARSA function lead to the neurodegenerative disease Metachromatic Leukodystrophy. This disease is characterized by accumulation of sulfatide within the band of myelin affecting its functionality...
May 10, 2016: Central Nervous System Agents in Medicinal Chemistry
P Del Negro, S Ciriaco, B Cataletto, G M Delogu, F Kokelj
Following in-depth analysis and examination, jellyfish toxins have been found to consist of a mixture of proteins, carbohydrates, and other non-proteinaceous components. What remains to be clarified is the specific chemical nature of jellyfish toxins due to their heat lability. This paper reviews current knowledge of the toxic properties of the most common Mediterranean scyphozoans (A. aurita, C. hysoscella, C. tuberculata, P. noctiluca, R. pulmo) and the activity of their venom.
May 5, 2016: Central Nervous System Agents in Medicinal Chemistry
Rodrigo E González-Reyes, María Graciela Rubiano
Adequate function of the nervous system depends on the balance of glia-neuron 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...
May 4, 2016: Central Nervous System Agents in Medicinal Chemistry
Quankun Zhuang, Cailing Dai, Linglong Yang, Huimin Wen, Hongyun Wang, Xiaoxue Jiang, Yuyang Zhang
Anandamide system is mainly made up of cannabinoid receptors, their endogenous ligands and some related enzymes. Activation of the system mediates various molecular events, thereafter leading to vasodilation, bradycardia and anti-inflammation. The stimulated cannabinoid receptors may take part in protection of endothelial cells from injury and therefore can be potential targets in therapy for some diseases, especially cardio or cerebral vascular disturbances. Cerebral ischemia is a deadly disease that modern people have to face and will probably face for a long period of time...
May 3, 2016: Central Nervous System Agents in Medicinal Chemistry
Rashmi Shukla, Ajeet Pal Singh, Pankaj K Sonar, Mudita Mishra, Shailendra K Saraf
A series of Schiff bases of benzothiazol-2-ylamine/thiazolo [5, 4-b] pyridin-2-ylamine was synthesized. Aniline/4-aminopyridine was converted to the corresponding thiourea derivatives, which were cyclized to obtain benzothiazol-2-ylamine/thiazolo [5, 4-b] pyridin-2-ylamine. Finally, these were condensed with various aromatic and heteroaromatic aldehydes to obtain twelve (I-XII) novel Schiff bases of benzothiazol-2-ylamine and thiazolo [5, 4-b] pyridin-2-ylamine. The synthesized compounds were characterized by spectral analysis and screened for their anticonvulsant activity using maximal electroshock (MES) test and isoniazid (INH) induced convulsions test, with phenytoin and diazepam, respectively, as the standard drugs...
April 28, 2016: Central Nervous System Agents in Medicinal Chemistry
Lucas Lima Vieira, Rafaela Gomes de Lima Soares, Stela Mirla da Silva Felipe, Felipe Carmo de Moura, Gerly Anne de Castro Brito, Christina Pacheco, Paula Matias Soares
BACKGROUND: Diabetes mellitus is a chronic degenerative disease responsible for hyperglycemic episodes through insulin secretion deficiency or cellular resistance. Clinical diagnosis in diabetic patients established that this disease affects the CNS, damaging the brain and impairing cognition, and thus establishing a clinical diabetic condition named diabetic encephalopathy. Despite the physiological mechanisms responsible for the development diabetic encephalopathy are still unclear, an excessive formation of reactive oxygen species, an alteration of acetylcholinesterase activity, and a reduction of growth factor levels, may be related with the pathogenesis of this condition...
April 28, 2016: Central Nervous System Agents in Medicinal Chemistry
Deepak K Jain, Avineesh Singh, Vijay K Patel, Ravichandran Veerasamy, Navneet Aggarwal, Harish Rajak
Anticonvulsant refers to a group of pharmaceuticals used in the treatment of epileptic seizures. The use of current antiepileptic drugs has been questioned due to the non-selectivity of the drugs and the undesirable side effects produced by them. This led to the search for antiepileptic compounds with more selectivity and lower toxicity. Semicarbazones have been developed as versatile anticonvulsant pharmacophore. It has displayed potent anticonvulsant effect in a wide variety of preclinical anticonvulsant models...
April 11, 2016: Central Nervous System Agents in Medicinal Chemistry
Harish Rajak, Deepak K Jain, Swati Singh, Avineesh Singh, Vijay K Patel, Ravichandran Veerasamy, Rajesh S Pawar
BACKGROUND: Epilepsy is a neurological disorder, characterized by seizures accompanied by loss or disturbance of consciousness affecting various physical and mental functions. Current anticonvulsant drugs are effective in controlling seizures in about 70% of cases, but their use is often limited by side effects like ataxia, megaloblastic anemia, hepatic failure. In search for a novel anticovulsant drug with better efficacy and lower toxicity, a series of novel pyrimidine based semicarbazone were designed and evaluated for antiepileptic activity...
March 30, 2016: Central Nervous System Agents in Medicinal Chemistry
Federica De Angelis, Ada Maria Tata
Chronic pain represents a research field on great clinical relevance and social impactful. It is associated to a variety of pathological events causing un altered excitability of peripheral nerves derived by tissue damage depending on physical, biological and chemical injury. In the last years much attention has been paid in the identification of novel molecules involved in mediating pain sensation useful as therapeutic tools for development of new analgesic drugs. Muscarinic receptors are widely distributed both in the central and peripheral nervous system...
March 1, 2016: Central Nervous System Agents in Medicinal Chemistry
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