Histamine H3 antagonists for treatment of cognitive deficits in CNS diseases.

abstract：:Implantable medical devices are increasingly important in the practice of modern medicine. Unfortunately, almost all medical devices suffer to a different extent from adverse reactions, including inflammation, fibrosis, thrombosis and infection. To improve the safety and function of many types of medical implants, a m...

journal_title：Current topics in medicinal chemistry

authors： Thevenot P,Hu W,Tang L

更新日期：2008-01-01 00:00:00

abstract：:For effective tumour imaging by magnetic resonance imaging (MRI) there is a clear need to develop organ, tissue and cell specific contrast agents that can selectively bind to tumour biomarkers. The versatility of a range of bioconjugation techniques and facile coupling chemistries has facilitated the synthesis of MRI ...

journal_title：Current topics in medicinal chemistry

authors： Kamaly N,Miller AD,Bell JD

更新日期：2010-01-01 00:00:00

abstract：:Compared with the increasing and widespread bacterial resistance to clinical medicines and the urgent need for cures of intractable diseases, there is a dramatic decline in the numbers of drugs reaching the market or clinical trials. Accordingly, it has become imperative to discover more rational and efficient strateg...

journal_title：Current topics in medicinal chemistry

authors： Wang T,Wu MB,Zhang RH,Chen ZJ,Hua C,Lin JP,Yang LR

更新日期：2016-01-01 00:00:00

abstract：:Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...

journal_title：Current topics in medicinal chemistry

authors： Meiera C,Renzea J,Ducho C,Balzarini J

更新日期：2002-10-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Liu W,Wang X,Zhu H,Duan Y

更新日期：2019-01-01 00:00:00

abstract：:Combinatorial chemistry has had a major impact on the discovery and optimisation of potential lead compounds. This review details some of the fundamental principles behind combinatorial chemistry and describes a variety of methods employed in the search for new therapeutically interesting compounds including the conce...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Martin RM,Mittoo S,Bradley M

更新日期：2004-01-01 00:00:00

abstract：:In the last few years, there has been a great increase in our understanding of pain mechanisms. Given the complexity of the mechanisms involved in pain modulation, it is surprising that the pharmacological control of pain through the application of relatively simple analgesics can be effective. Nevertheless, the appli...

journal_title：Current topics in medicinal chemistry

authors： Mico JA,Berrocoso E,Ortega-Alvaro A,Gibert-Rahola J,Rojas-Corrales MO

更新日期：2006-01-01 00:00:00

abstract：:Biomarkers in the clinical oncology field can have tremendous therapeutic impact especially if the marker is detected before clinical symptoms. This impact can be extended to the evaluation of clinical oncology treatments allowing evaluation of potential compounds to determine their efficacy in the disease treatment. ...

journal_title：Current topics in medicinal chemistry

authors： Belkowski SM,Polkovitch D,D'Andrea MR

更新日期：2005-01-01 00:00:00

abstract：:This review covers recent progress in the discovery of selective glucocorticoid receptor (GR) antagonists. Potential therapeutic applications of selective GR antagonists are described including the pharmacological rationale and, in some cases, clinical evidence that underlies these proposed uses. Disease areas that ar...

journal_title：Current topics in medicinal chemistry

authors： Clark RD

更新日期：2008-01-01 00:00:00

abstract：:The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines. These subtypes have been explored and structure-a...

journal_title：Current topics in medicinal chemistry

authors： Ferraris D,Belyakov S,Li W,Oliver E,Ko YS,Calvin D,Lautar S,Thomas B,Rojas C

更新日期：2007-01-01 00:00:00

abstract：:Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively....

journal_title：Current topics in medicinal chemistry

authors： Kucuksayan E,Ozben T

更新日期：2017-01-01 00:00:00

abstract：:Penile erection is a complex physiologic event resulting from the interactions of the nervous system on a highly specialized vascular organ. Activation of central nervous system melanocortinergic (MC) receptors with either endogenous or synthetic melanotropic ligands may initiate and/or facilitate spontaneous penile e...

journal_title：Current topics in medicinal chemistry

authors： King SH,Mayorov AV,Balse-Srinivasan P,Hruby VJ,Vanderah TW,Wessells H

更新日期：2007-01-01 00:00:00

abstract：:Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for...

journal_title：Current topics in medicinal chemistry

authors： Cadilla R,Turnbull P

更新日期：2006-01-01 00:00:00

abstract：:The Rho family small GTPases of the Ras superfamily play key roles in regulating diverse signaling pathways that control a myriad of fundamental cellular processes such as cytoskeletal dynamics, cell cycle progression, gene expression, cell polarity, migration and cell transformation. The Rho GTPases cycle between an ...

journal_title：Current topics in medicinal chemistry

authors： Ding F,Yin Z,Wang HR

更新日期：2011-12-01 00:00:00

abstract：:This article focuses on the GDNF family of neurotrophic factors as a potential new class of therapeutics for neuropathic pain, with a particular emphasis on the ligands, artemin and GDNF. In vivo activity of the ligands, expression of ligands and receptors after peripheral nerve injury, and modulation of nerve injury-...

journal_title：Current topics in medicinal chemistry

authors： Sah DW,Ossipov MH,Rossomando A,Silvian L,Porreca F

更新日期：2005-01-01 00:00:00

abstract：:For successful drug discovery it is important to understand the fundamentals of the underlying causes and consequences of the diseases for which the drug is being developed. One such physiological process in eukaryotic cells is protein phosphorylation, which is the main post-translational modification of proteins resp...

journal_title：Current topics in medicinal chemistry

authors： Bhalla N,Estrela P

更新日期：2017-01-01 00:00:00

abstract：:Cytochrome P450 17A1 (CYP17A1; also P450c17and P450sccII) is a critically important enzyme in humans that catalyzes the formation of all endogenous androgens. It is an atypical cytochrome P450 enzyme in that it catalyzes two distinct types of substrate oxidation. Through its hydroxylase activity, it catalyzes the 17α-...

journal_title：Current topics in medicinal chemistry

authors： Porubek D

更新日期：2013-01-01 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：:After the identification of the anti-inflammatory properties of VA5-13l (2-benzyl-1- methyl-5-nitroindazolinone) in previous investigations, some of its analogous compounds were designed, synthesized and evaluated in two anti-inflammatory methods: LPS-enhanced leukocyte migration assay in zebrafish; and 12-O-tetradeca...

journal_title：Current topics in medicinal chemistry

authors： Siverio-Mota D,Andujar I,Marrero-Ponce Y,Giner RM,Diaz-Mendoza C,Paba GM,Vicet-Muro L,Cordero-Maldonado ML,de Witte PAM,Crawford AD,Veitia MS,Perez-Jimenez F,Aran VJ

更新日期：2018-02-09 00:00:00

abstract：:Hepatitis C virus (HCV) is a major cause of acute hepatitis and chronic liver disease, including cirrhosis and hepatocellular carcinoma (HCC). No vaccine is currently available to prevent hepatitis C, and the current standard of care (SOC) - pegylated interferon-α (PEG-IFN-α) in combination with ribavirin (RBV) - is o...

journal_title：Current topics in medicinal chemistry

authors： Avolio S,Summa V

更新日期：2010-01-01 00:00:00

abstract：:This review discusses the state of the art, challenges and perspectives in recent applications of electrochemistry in the life sciences. It deals mainly with the elucidation of molecular mechanisms of drug action, drug design and development, involving electron transfer, pharmaco-electrochemistry (the combination of e...

journal_title：Current topics in medicinal chemistry

authors： de Paiva YG,da Rocha Ferreira F,Silva TL,Labbe E,Buriez O,Amatore C,Fonseca Goulart MO

更新日期：2015-01-01 00:00:00

abstract：:Efflux pumps of the Resistance Nodulation Division (RND) superfamily play a major role in the intrinsic and acquired resistance of Gram-negative pathogens to antibiotics. Moreover, they are largely responsible for multi-drug resistance (MDR) phenomena in these bacteria. The last decade has seen a sharp increase in the...

journal_title：Current topics in medicinal chemistry

authors： Ruggerone P,Murakami S,Pos KM,Vargiu AV

更新日期：2013-01-01 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：:Psychiatric diagnosis has long been perceived as more of an art than a science since its foundations lie within the observation, and the self-report of the patients themselves and objective diagnostic biomarkers are lacking. Furthermore, the diagnostic tools in use not only stray away from the conventional medical fra...

journal_title：Current topics in medicinal chemistry

authors： Todeva-Radneva A,Paunova R,Kandilarova S,St Stoyanov D

更新日期：2020-01-01 00:00:00

abstract：:Isoindole derivatives constitute an important class of biologically active heterocyclic compounds and continue to attract considerable attention due to their diverse pharmacological profile such as, antimicrobial, anthelmintic, insecticidal, cyclooxygenase isoenzyme (COX-2) and thrombin inhibition with special emphasi...

journal_title：Current topics in medicinal chemistry

authors： Bhatia RK

更新日期：2017-01-01 00:00:00

abstract：:(2R,3R)-2,3-Butanediol has many industrial applications, such as it is used as an antifreeze agent and low freezing point fuel. In addition, it is particularly important to provide chiral groups in drugs. In recent years, this valuable bio-based chemical has attracted increasing attention, and significant progress has...

journal_title：Current topics in medicinal chemistry

authors： Xie NZ,Chen XR,Wang QY,Chen D,Du QS,Zhou GP,Huang RB

更新日期：2017-01-01 00:00:00

abstract：:Despite the tremendous progress in the field of drug designing, discovering a new drug molecule is still a challenging task. Drug discovery and development is a costly, time consuming and complex process that requires millions of dollar and 10-15 years to bring new drug molecules in the market. This huge investment an...

journal_title：Current topics in medicinal chemistry

authors： Singla D,Dhanda SK,Chauhan JS,Bhardwaj A,Brahmachari SK,Open Source Drug Discovery Consortium.,Raghava GP

更新日期：2013-01-01 00:00:00

abstract：:Asthma, a chronic inflammatory disease of the airways, is a significant burden on our healthcare system. There is high unmet need for treatments directed towards the underlying causes of the disease. The cell surface integrin VLA-4 (very late antigen-4; alpha4beta1; CD49d/CD29) plays an important role in the trafficki...

journal_title：Current topics in medicinal chemistry

authors： Singh J,Adams S,Carter MB,Cuervo H,Lee WC,Lobb RR,Pepinsky RB,Petter R,Scott D

更新日期：2004-01-01 00:00:00

abstract：:This review mainly covers last five year literature on CCK1R agonists and antagonists. These CCK1R ligands have been found following the two usual and complementary strategies for drug discovery: rational design based on structure activity relationships on the CCK-7 and CCK-4 peptide sequences of the endogenous ligand...

journal_title：Current topics in medicinal chemistry

authors： García-López MT,González-Muñiz R,Martín-Martínez M,Herranz R

更新日期：2007-01-01 00:00:00

abstract：:Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

journal_title：Current topics in medicinal chemistry

authors： Liu X,Cao J,Huang G,Zhao Q,Shen J

更新日期：2019-01-01 00:00:00