Application of combinatorial and parallel synthesis chemistry methodologies to antiparasitic drug discovery.

abstract：:Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as inc...

journal_title：Current medicinal chemistry

authors： Chen X,Hussain S,Parveen S,Zhang S,Yang Y,Zhu C

更新日期：2012-01-01 00:00:00

abstract：:Polycystic ovary syndrome (PCOS) is the most common endocrine and metabolic disorder affecting women in reproductive age. Although the etiology of PCOS remains unclear, it is believed to result from genetic, environmental and behavioral interactions. Women with PCOS have higher lifetime risk for cardiovascular disease...

journal_title：Current medicinal chemistry

authors： Vélez LM,Motta AB

更新日期：2014-01-01 00:00:00

abstract：:The bi-aryl urea multi-kinase inhibitor Sorafenib (BAY 43-9006, Nexavar) was initially approved for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Eleven years after its first description in PubMed, the therapeutic potential of Sorafenib has been evaluated in an increasing nu...

journal_title：Current medicinal chemistry

authors： Zauli G,Voltan R,Tisato V,Secchiero P

更新日期：2012-01-01 00:00:00

abstract：:Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...

journal_title：Current medicinal chemistry

authors： Eros D,Kövesdi I,Orfi L,Takács-Novák K,Acsády G,Kéri G

更新日期：2002-10-01 00:00:00

abstract：:Traditional opioids, mainly alkaloids, have been used in the clinical management of pain for a number of years but are often associated with numerous side-effects including sedation, dizziness, physical dependence, tolerance, addiction, nausea, vomiting, constipation and respiratory depression which prevent their effe...

journal_title：Current medicinal chemistry

authors： Garg S,Nurgali K,Mishra VK

更新日期：2016-01-01 00:00:00

abstract：:Heparins are used in "therapeutic doses" for systemic anticoagulation to treat patients who have confirmed venous thromboembolism, or in "prophylactic doses "for the prevention of venous thromboembolism: they are generally lower doses and are employed once a day. Structure-function relationships are strongly influence...

journal_title：Current medicinal chemistry

authors： Stratta P,Karvela E,Canavese C,Quaglia M,Lazzarich E,Fenoglio R,Pergolini P,Bellomo G,Cena T,Magnani C

更新日期：2009-01-01 00:00:00

abstract：:Phosphonated nucleosides represent a promising alternative in the improvement of the biological activity of nucleoside analogues in antiviral and anticancer chemotherapy. The basic concept, the chemistry, the different structural modifications and their effects on the antiviral potency will be discussed in this review...

journal_title：Current medicinal chemistry

authors： Piperno A,Chiacchio MA,Iannazzo D,Romeo R

更新日期：2006-01-01 00:00:00

abstract：:Type 2 diabetes mellitus is a metabolic disease widely spread across industrialized countries. Sedentary lifestyle and unhealthy alimentary habits lead to obesity, boosting both glucose and fatty acid in the bloodstream and eventually, insulin resistance, pancreas inflammation and faulty insulin production or secretio...

journal_title：Current medicinal chemistry

authors： Rosado JA,Diez-Bello R,Salido GM,Jardin I

更新日期：2019-01-01 00:00:00

abstract：:ATP binding cassette (ABC) transporters are involved in drug absorption, distribution and elimination. They also mediate multidrug resistance in cancer cells. Isoflavones, such as genistein (GNT), belong to a class of naturally-occurring compounds found at high concentrations in commonly consumed soya based-foods and ...

journal_title：Current medicinal chemistry

authors： Rigalli JP,Ciriaci N,Mottino AD,Catania VA,Ruiz ML

更新日期：2016-01-01 00:00:00

abstract：:Recent advances have identified the podocyte as a key target in glomerular injury. The podocyte is a highly specialized cell which is responsible for the glomerular permselectivity for proteins in the kidney. Podocyte injury or loss leads to proteinuria. Apoptosis has been shown to contribute to renal cell loss, inclu...

journal_title：Current medicinal chemistry

authors： Moreno JA,Sanchez-Niño MD,Sanz AB,Lassila M,Holthofer H,Blanco-Colio LM,Egido J,Ruiz-Ortega M,Ortiz A

更新日期：2008-01-01 00:00:00

abstract：:Cell products are live cells that are given to patients in order to replace or modify the function of missing or dysfunctional cells. Progress in technology and in the understanding of pathobiology may lead to the use of cell products in many areas. This review outlines the use of cell products in the treatment of aut...

journal_title：Current medicinal chemistry

authors： Ernerudh J,Berlin G,Ekerfelt C

更新日期：2002-08-01 00:00:00

abstract：:Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infection has been a global challenge. The complicated forms of the Coronavirus Disease 2019 (COVID-19) can evolve to multiple-organ failure, including several coagulopathies related to a sudden worsening of respiratory status. This article aimed to review s...

journal_title：Current medicinal chemistry

authors： Pena ALB,Oliveira RA,Severo RG,Simões E Silva AC

更新日期：2020-10-05 00:00:00

abstract：:The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five struc...

journal_title：Current medicinal chemistry

authors： Dannhardt G,Laufer S

更新日期：2000-11-01 00:00:00

abstract：:Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new c...

journal_title：Current medicinal chemistry

authors： Salas CO,Faúndez M,Morello A,Maya JD,Tapia RA

更新日期：2011-01-01 00:00:00

abstract：:In the human brain several cell types are capable of initiating and amplifying a brain specific inflammatory response involving the synthesis of cytokines, prostaglandins and oxygen free radicals. In Alzheimer's disease (AD), signs of an inflammatory activation of microglia and astroglia are present inside and outside...

journal_title：Current medicinal chemistry

authors： Hüll M,Lieb K,Fiebich BL

更新日期：2002-01-01 00:00:00

abstract：:The polystyrene-based 2-chlorotrityl resin was originally used in the synthesis of peptides using an Fmoc-amino acid/carboxyl-linked protocol. While traditionally employed to prepare a number of biologically active peptides, the resin has received increasing attention as a support for the synthesis of pseudopeptide an...

journal_title：Current medicinal chemistry

authors： Hoekstra WJ

更新日期：2001-05-01 00:00:00

abstract：:For more than 20 years there has been increasing interest in the development of novel therapies to raise levels of high-density lipoprotein cholesterol (HDL-C). However, well publicized failures of recent clinical trials of agents that raise HDL-C levels have stimulated considerable controversy with regard to the pote...

journal_title：Current medicinal chemistry

authors： Duong M,Nicholls SJ

更新日期：2014-01-01 00:00:00

abstract：:Protein-ligand docking is currently an important tool in drug discovery efforts and an active area of research that has been the subject of important developments over the last decade. These are well portrayed in the rising number of available protein-ligand docking software programs, increasing level of sophisticatio...

journal_title：Current medicinal chemistry

authors： Sousa SF,Ribeiro AJ,Coimbra JT,Neves RP,Martins SA,Moorthy NS,Fernandes PA,Ramos MJ

更新日期：2013-01-01 00:00:00

abstract：:HupA is a potent, reversible AChEI, which crosses the blood-brain barrier smoothly, and shows high specificity for AChE with a prolonged biological half-life. It has been approved as the drug for the treatment of AD in China, and marketed in USA as a dietary supplement. HupA has been the subject of investigations by a...

journal_title：Current medicinal chemistry

authors： Jiang H,Luo X,Bai D

更新日期：2003-11-01 00:00:00

abstract：:Evidence came out showing that oxidative stress has a pivotal role in development and maintenance of inflammation and aberrant immune responses. Biomarkers of oxidative stress may define the proportion of oxidative damage underlying pathological conditions, and also foresee and monitor the possible efficacy of therape...

journal_title：Current medicinal chemistry

authors： Cristani M,Speciale A,Saija A,Gangemi S,Minciullo PL,Cimino F

更新日期：2016-01-01 00:00:00

abstract：:The present paper summarizes the possible roles of frequent and unfavourable genetic variants in cerebrovascular disorders, such as stroke and leukoaraiosis. It also approaches the topic theoretically from functional and mathematical points of view, which can help make the accumulating data on genetic variants more un...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2009-01-01 00:00:00

abstract：:Cellular signaling is regulated by several biochemical reactions, whose dynamics depends on changes in the fluxes of specific ligands through the containment barriers that are the biological membranes. The regulation of this complex dynamic equilibrium is mainly due to the activity of border proteins, that must be abl...

journal_title：Current medicinal chemistry

authors： Dainese E,Oddi S,Maccarrone M

更新日期：2010-01-01 00:00:00

abstract：:Diabetes mellitus (DM) is characterized by hyperglycemia, resulting from defects in insulin secretion, insulin action or both. There are several factors such as hyperlipidemia and oxidative stress (OS), namely the production of reactive oxygen/nitrogen species (ROS/RNS), that actively contribute to the development and...

journal_title：Current medicinal chemistry

authors： Sousa A,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-05-24 00:00:00

abstract：:Flavonoids are natural plant-derived polyphenolic compounds with various biological properties particularly in the cardiovascular system, including antiatherogenic, antioxidant, vasodilation, antihypertensive, and antiplatelet activities. These biological properties have been evaluated in several experimental and clin...

journal_title：Current medicinal chemistry

authors： Almeida Rezende B,Pereira AC,Cortes SF,Lemos VS

更新日期：2016-01-01 00:00:00

abstract：:Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, cou...

journal_title：Current medicinal chemistry

authors： Wu L,Wang X,Xu W,Farzaneh F,Xu R

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:A great effort has been made to develop efficacious antiviral drugs, but many viral infections are still lack of efficient antiviral therapies so far. The related exploration of natural products to fight viruses has been raised in recent years. Natural compounds with structural diversity and complexity offer...

journal_title：Current medicinal chemistry

authors： Wu YH,Zhang BY,Qiu LP,Guan RF,Ye ZH,Yu XP

更新日期：2017-01-01 00:00:00

abstract：:Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform asso...

journal_title：Current medicinal chemistry

authors： Aparoy P,Reddy KK,Reddanna P

更新日期：2012-01-01 00:00:00

abstract：:The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to prov...

journal_title：Current medicinal chemistry

authors： Matute MS,Matute R,Merino P

更新日期：2016-01-01 00:00:00

abstract：:The cation-independent mannose 6-phosphate receptor is a multifunctional protein which binds at the cell surface to two distinct classes of ligands, the mannose 6-phosphate (M6P) bearing proteins and IGF-II. Its major function is to bind and transport M6P-enzymes to lysosomes, but it can also modulate the activity of ...

journal_title：Current medicinal chemistry

authors： Gary-Bobo M,Nirdé P,Jeanjean A,Morère A,Garcia M

更新日期：2007-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) and its splice variants, paralogs and human homologs represent a family of proteins with diverse tissue distribution, cellular localization and largely unknown function which have been explored only recently. While GCPII itself has been thoroughly studied from different perspectiv...

journal_title：Current medicinal chemistry

authors： Hlouchová K,Navrátil V,Tykvart J,Sácha P,Konvalinka J

更新日期：2012-01-01 00:00:00