Trypanocidal activity of nitroaromatic prodrugs: current treatments and future perspectives.

abstract：:The introduction of biochemical biomarkers in the evaluation of patients with cardiovascular disease has led to practice-changing advancements in the way these patients are diagnosed and managed. Measurements of cardiac troponins or brain-type natriuretic peptide (BNP) and its precursor, N-terminal brain-type natriure...

journal_title：Current topics in medicinal chemistry

authors： Giannopoulos G,Deftereos S,Panagopoulou V,Kossyvakis C,Kaoukis A,Bouras G,Pyrgakis V,Cleman MW

更新日期：2013-01-01 00:00:00

abstract：:Cancer research has progressed leaps and bounds over the years. This review is a brief overview of the cancer research, milestone achievements and therapeutic studies on it over the one hundred ten years which would give us an insight into how far we have come to understand and combat this fatal disease leading to mil...

journal_title：Current topics in medicinal chemistry

authors： Shastri S,Chatterjee B,Thakur SS

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly a...

journal_title：Current topics in medicinal chemistry

authors： Nandi S,Kaur R,Kumar M,Sharma A,Naaz A,Mandal SC

更新日期：2018-01-01 00:00:00

abstract：:Traditionally the role of sexual steroid hormones was focused primarily on reproductive organs: the breast, female reproductive tract (uterus, mammary gland, and ovary), and male reproductive tract (testes, epididymis and prostate), however our current understanding of tissue-specific effects of sex steroids has eluci...

journal_title：Current topics in medicinal chemistry

authors： Morimoto S,Jiménez-Trejo F,Cerbón M

更新日期：2011-01-01 00:00:00

abstract：:The Human Genome Project and the explosion of high-throughput data have transformed the areas of molecular and personalized medicine, which are producing a wide range of studies and experimental results and providing new insights for developing medical applications. Research in many interdisciplinary fields is resulti...

journal_title：Current topics in medicinal chemistry

authors： de la Iglesia D,García-Remesal M,de la Calle G,Kulikowski C,Sanz F,Maojo V

更新日期：2013-01-01 00:00:00

abstract：:Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However,...

journal_title：Current topics in medicinal chemistry

authors： Zhou XX,Littler E

更新日期：2006-01-01 00:00:00

abstract：:This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of ...

journal_title：Current topics in medicinal chemistry

authors： Nejera C,Sansano JM

更新日期：2014-01-01 00:00:00

abstract：:Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, n...

journal_title：Current topics in medicinal chemistry

authors： Bolognesi ML

更新日期：2011-11-01 00:00:00

abstract：:Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects largely synovial joints. It has been postulated that activated autoreactive CD4 T cells play a key role in triggering and/or maintaining the chronic inflammatory process in RA. Dendritic cells (DCs) are antigen-presenting cells that ac...

journal_title：Current topics in medicinal chemistry

authors： Rodríguez-Fernández JL

更新日期：2013-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is an irreversible multifaceted neurodegenerative disorder that gradually degrades neuronal cells. Presently, it is the most common reason for the memory loss and dementia in older individuals. It is patho-physiologically described by extracellular amyloid beta (Aβ) deposition, intracellular n...

journal_title：Current topics in medicinal chemistry

authors： Ul Islam B,Khan MS,Jabir NR,Kamal MA,Tabrez S

更新日期：2017-01-01 00:00:00

abstract：:The vesicular acetylcholine transporter (VAChT) is a glycoprotein responsible for the accumulation of acetylcholine into pre-synaptic vesicules of cholinergic neurons. Cholinergic innervation has been shown to be decreased at the earlier stages of Alzheimer's disease (AD). Thus, the expression of VAChT has been correl...

journal_title：Current topics in medicinal chemistry

authors： Giboureau N,Som IM,Boucher-Arnold A,Guilloteau D,Kassiou M

更新日期：2010-01-01 00:00:00

abstract：:Recent advances in DNA microarray technology have great impact on many areas of biomedical research and pharmacogenomics: discovering novel targets and genes, elucidating signatures of complex diseases, transcriptional profiling of models for diseases, and the development of individually optimized drugs based on diffe...

journal_title：Current topics in medicinal chemistry

authors： Hackl H,Sanchez Cabo F,Sturn A,Wolkenhauer O,Trajanoski Z

更新日期：2004-01-01 00:00:00

abstract：:Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic "histone code," thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overvi...

journal_title：Current topics in medicinal chemistry

authors： Moradei O,Vaisburg A,Martell RE

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND:Development of acetyl- (AChE) and butyrylcholinesterase (BuChE) inhibitors belongs to viable strategies for the treatment of dementia and other diseases related to decrease in cholinergic neurotransmission. OBJECTIVE:That is why we designed twenty-two analogues of a dual AChEBuChE salicylanilide inhibitor, ...

journal_title：Current topics in medicinal chemistry

authors： Krátký M,Jaklová K,Štěpánková Š,Svrčková K,Pflégr V,Vinšová J

更新日期：2020-01-01 00:00:00

abstract：:The atomic determination of the acetylcholine binding protein (AChBP), a molluscan cholinergic protein, homologous to the amino-terminal extracellular domain of nicotinic receptors (nAChRs), offers opportunities for the modeling of the acetylcholine binding site and its ligands. Recently, we constructed three-dimensio...

journal_title：Current topics in medicinal chemistry

authors： Grutter T,Le Novère N,Changeux JP

更新日期：2004-01-01 00:00:00

abstract：:Although bioactivation is a well-documented process and the role of active metabolites in the drug discovery field has long been recognized, drug metabolites are usually ignored in virtual screening campaigns oriented to drug repositioning. The present article discusses different issues related to overlooking of the a...

journal_title：Current topics in medicinal chemistry

authors： Talevi A

更新日期：2016-01-01 00:00:00

abstract：:The emergence of multi-resistant bacteria to drugs is recognized as a major cause of the increasing number of deaths in hospitals. Killing these bacteria require multiple expensive drugs that can have side effects. Metal nanoparticles may provide a new strategy to combat them. Due the antimicrobial and antiviral prope...

journal_title：Current topics in medicinal chemistry

authors： Oktar FN,Yetmez M,Ficai D,Ficai A,Dumitru F,Pica A

更新日期：2015-01-01 00:00:00

abstract：:This is a general review of currently available antimalarial drugs, these compounds are gathered according with its chemical structure and the biological targets. A great number of these new antimalarial agents are now moving actively in the pipeline from basic science to clinical studies. ...

journal_title：Current topics in medicinal chemistry

authors： Domínguez JN

更新日期：2002-11-01 00:00:00

abstract：:The knowledge about to which biomolecules a small molecule binds is highly valuable in the drug development process. Although analytical methods to dissect ligand-binding proteome have made substantial progress in the past decades, it is generally too costly, if not infeasible, to know where a small molecule binds at ...

journal_title：Current topics in medicinal chemistry

authors： Lin JH

更新日期：2012-01-01 00:00:00

abstract：:Thematic Analysis™ is a chemogenomic tool which has been developed and used to aid the process of GPCR drug discovery. This review covers the scientific rationale behind the development of this tool and provides examples of the successful application of the chemogenomic method in both hit finding and hit to lead stage...

journal_title：Current topics in medicinal chemistry

authors： Crossley R,Macritchie JA,Slater MJ

更新日期：2011-01-01 00:00:00

abstract：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00

abstract：:Iron chelators may be of value as therapeutic agents in the treatment of cancer. They may act by depleting iron, a necessary nutrient, and limiting tumor growth. Alternatively or additionally, they may form redox-active metal complexes that cause oxidative stress via production of reactive oxygen species, damaging cri...

journal_title：Current topics in medicinal chemistry

authors： Buss JL,Greene BT,Turner J,Torti FM,Torti SV

更新日期：2004-01-01 00:00:00

abstract：:Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and ...

journal_title：Current topics in medicinal chemistry

authors： Rayar AM,Lagarde N,Ferroud C,Zagury JF,Montes M,Sylla-Iyarreta Veitia M

更新日期：2017-01-01 00:00:00

abstract：:Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and recept...

journal_title：Current topics in medicinal chemistry

authors： Pereira TM,Franco DP,Vitorio F,Kummerle AE

更新日期：2018-01-01 00:00:00

abstract：:The development of computational tools for the prediction of passive transport is reviewed with particular reference to four diverse approaches: the rule-of-5, polar surface area, Volsurf and Abraham's General Solvation Equation. To illustrate the current state of the art, several examples of the application of in sil...

journal_title：Current topics in medicinal chemistry

authors： Clark DE,Grootenhuis PD

更新日期：2003-01-01 00:00:00

abstract：:The adenosine A(2A) receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A(2A) receptor with several pathological conditions such as neurodegenerative disorde...

journal_title：Current topics in medicinal chemistry

authors： Clementina M,Giuseppe S

更新日期：2010-01-01 00:00:00

abstract：AIMS:The need to find new antimicrobial agents to cope with this phenomenon increases. BACKGROUND:Infection diseases are illness caused by different microorganisms, such as bacteria, among those caused by resistant bacteria are associated with greater morbidity, mortality and cost of the treatment than those caused by...

journal_title：Current topics in medicinal chemistry

authors： Nocedo-Mena D,Garza-González E,González-Ferrara M,Del Rayo Camacho-Corona M

更新日期：2020-01-01 00:00:00

abstract：:PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...

journal_title：Current topics in medicinal chemistry

authors： Nanda BL,Nataraju A,Rajesh R,Rangappa KS,Shekar MA,Vishwanath BS

更新日期：2007-01-01 00:00:00

abstract：:The IkappaB kinases (IKKs) are essential components of the signaling pathway by which the NF-kappaB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFalpha). NF-kappaB signaling results in the expression of numerous genes i...

journal_title：Current topics in medicinal chemistry

authors： Bamborough P,Callahan JF,Christopher JA,Kerns JK,Liddle J,Miller DD,Morse MA,Rumsey WL,Williamson R

更新日期：2009-01-01 00:00:00

abstract：:Estrogens control a wide number of aspects of human physiology and play a key role in multiple diseases, including cancer. Estrogens act by binding to and activating the cognate receptor (ER), however numerous studies have revealed that the G protein-coupled receptor named GPR30/GPER mediates also estrogen signals. As...

journal_title：Current topics in medicinal chemistry

authors： Sinicropi MS,Lappano R,Caruso A,Santolla MF,Pisano A,Rosano C,Capasso A,Panno A,Lancelot JC,Rault S,Saturnino C,Maggiolini M

更新日期：2015-01-01 00:00:00