Pyridines and Imidazopyridines with Medicinal Significance.

abstract：:The oxidative stress that is associated with the abnormal level of reactive oxygen species (ROS) is considered to be involved in the carcinogenesis process. The antioxidative defense system in the living organism regulates the toxic impact of ROS and there is strong evidence that the antioxidants prevent carcinogenesi...

journal_title：Current topics in medicinal chemistry

authors： Milaeva ER

更新日期：2011-01-01 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：INTRODUCTION:Structure-based drug design is a wide area of identification of selective inhibitors of a target of interest. From the time of the availability of three dimensional structure of the drug targets, mostly the proteins, many computational methods had emerged to address the challenges associated with drug desi...

journal_title：Current topics in medicinal chemistry

authors： Velmurugan D,Pachaiappan R,Ramakrishnan C

更新日期：2020-01-01 00:00:00

abstract：:The genetic material in humans contains approximately 6 billion base pairs in the nuclear genome and 16,569 base pairs in the mitochondrial genome [1-3]. In some cases the difference between a healthy and a sick individual consists in only one nucleotide. Thus, it is evident that the pristine replication of the genome...

journal_title：Current topics in medicinal chemistry

authors： Brieba LG

更新日期：2008-01-01 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：:The neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) family of hormones exhibit a wide variety of biological actions on the mammalian gastrointestinal tract through known G-protein coupled receptor pathways. At least four receptor subtypes, denoted as Y(1), Y(2), Y(4) an Y(5), each with specific ...

journal_title：Current topics in medicinal chemistry

authors： Vona-Davis LC,McFadden DW

更新日期：2007-01-01 00:00:00

abstract：:A large number of human disorders are caused by defects in protein folding resulting from genetic mutations or adverse physiological conditions, and these are collectively referred to protein misfolding diseases. Such disorders imply dysfunction of a cellular process either as a result of a toxic gain of function due ...

journal_title：Current topics in medicinal chemistry

authors： Gomes CM

更新日期：2012-01-01 00:00:00

abstract：AIMS:Computational modelling may help us to detect the more important factors governing this process in order to optimize it. BACKGROUND:The generation of hazardous organic waste in teaching and research laboratories poses a big problem that universities have to manage. METHODS:In this work, we report on the experime...

journal_title：Current topics in medicinal chemistry

authors： Montes-Bageneta I,Akesolo U,López S,Merino M,Anakabe E,Arrasate S

更新日期：2020-01-01 00:00:00

abstract：:HIV-1 integrase (IN) plays an important role in the life cycle of HIV and is responsible for integration of the virus into the human genome. We present computational approaches used to design novel HIV-1 IN inhibitors. We created an IN inhibitor database by collecting experimental data from the literature. We develope...

journal_title：Current topics in medicinal chemistry

authors： Guasch L,Zakharov AV,Tarasova OA,Poroikov VV,Liao C,Nicklaus MC

更新日期：2016-01-01 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：:Target-Related Affinity Profiling (TRAP) is a computational drug discovery technology that is based on 'affinity fingerprints', which are molecular descriptors derived from the protein binding preferences of small molecules. The underlying concepts of TRAP are reviewed. Affinity fingerprints are compared to molecular ...

journal_title：Current topics in medicinal chemistry

authors： Beroza P,Damodaran K,Lum RT

更新日期：2005-01-01 00:00:00

abstract：:Neuronal nicotinic acetylcholine ion channel receptors (nAChRs) exist as several subtypes and are involved in a variety of functions and disorders of the central nervous system (CNS), such as Alzheimer's and Parkinson's diseases. The lack of reliable information on the 3D structure of nAChRs prompted us to focus effor...

journal_title：Current topics in medicinal chemistry

authors： Nicolotti O,Altomare C,Pellegrini-Calace M,Carotti A

更新日期：2004-01-01 00:00:00

abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

journal_title：Current topics in medicinal chemistry

authors： Casazza V,Rossi F,Rizzi M

更新日期：2011-01-01 00:00:00

abstract：:In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is fast becoming an alternative to other existing strategies of drug development. These hybrids also known as 'dual drugs' or 'double drugs' are especially found to be effective in overcoming drug resistance prob...

journal_title：Current topics in medicinal chemistry

authors： Manohar S,Tripathi M,Rawat DS

更新日期：2014-01-01 00:00:00

abstract：:Cells rely on several transition metals to regulate a wide range of metabolic and signaling functions. The diversity and efficiency of their physiological functions are derived from atomic properties that are specific to transition metals, most notably an incomplete inner valence subshell. These properties impart upon...

journal_title：Current topics in medicinal chemistry

authors： Hamai D,Bondy SC,Becaria A,Campbell A

更新日期：2001-12-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Yu Y

更新日期：2019-01-01 00:00:00

abstract：:In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard t...

journal_title：Current topics in medicinal chemistry

authors： Johnson L,Goping IS,Rieger A,Mane JY,Huzil T,Banerjee A,Luduena R,Hassani B,Winter P,Tuszynski JA

更新日期：2017-01-01 00:00:00

abstract：:The problem in this work is the computational characterization of cyclodextrins, crown ethers and hyaluronan (HA) as hosts of inclusion complexes for nanosized drug delivery vehicles in pharmaceutical formulations. The difficulty is addressed through a computational study of some thermodynamic, geometric and topologic...

journal_title：Current topics in medicinal chemistry

authors： Torrens F,Castellano G

更新日期：2015-01-01 00:00:00

abstract：:In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During the last 10 years a number of novel p38 chemotypes were dis...

journal_title：Current topics in medicinal chemistry

authors： Diller DJ,Lin TH,Metzger A

更新日期：2005-01-01 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：:Structure-activity relationships of a 4-aminoquinoline MCH-1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4- and 6-positions of the original HTS hit. Improvements to the original screening lead were made by addition of lipophilic groups at the 2-position and biphenyl, cyc...

journal_title：Current topics in medicinal chemistry

authors： DeVita RJ

更新日期：2007-01-01 00:00:00

abstract：:Viral entry, the first process in the reproduction of viruses, primarily involves attachment of the viral envelope proteins to membranes of the host cell. The crucial components that play an important role in viral entry include viral surface glycoprotein gp120, viral transmembrane glycoprotein gp41, host cell glycopr...

journal_title：Current topics in medicinal chemistry

authors： Suttisintong K,Kaewchangwat N,Thanayupong E,Nerungsi C,Srikun O,Pungpo P

更新日期：2019-01-01 00:00:00

abstract：:Errors in the mitotic process are thought to be one of the principal sources of the genetic instability that hallmarks cancer. Unsurprisingly, many of the proteins that regulate mitosis are aberrantly expressed in tumour cells when compared to their normal counterparts. These may represent a good source of targets for...

journal_title：Current topics in medicinal chemistry

authors： Mortlock AA,Keen NJ,Jung FH,Heron NM,Foote KM,Wilkinson RW,Green S

更新日期：2005-01-01 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：:An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administ...

journal_title：Current topics in medicinal chemistry

authors： Sharpe PC,Richardson DR,Kalinowski DS,Bernhardt PV

更新日期：2011-01-01 00:00:00

abstract：:There exists a huge attrition rate of molecules in clinical trials. It was expected that high-throughput screening and combinatorial chemistry would make the task of producing drugs easier. However, the efforts of the past decade have not been an unvarnished success. As a result, a lot of experimental and computationa...

journal_title：Current topics in medicinal chemistry

authors： Ajay

更新日期：2002-12-01 00:00:00

abstract：:Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inh...

journal_title：Current topics in medicinal chemistry

authors： Goel R,Luxami V,Paul K

更新日期：2016-01-01 00:00:00

abstract：:Thermolysin (TLN) and other thermolysin-like zinc metalloproteinases (TLPs),are important virulence factors for pathogenesis of bacterial infections by suppressing the innate immune system of the host. Therapeutic inhibition ofTLPs is believed to be a novel strategy inthe development of a new generation antibiotics.In...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Dedachi K,Matsui T,Kurita N,Borgatti M,Gambari R,Sylte I

更新日期：2012-01-01 00:00:00

abstract：:Organic nitrates, such as nitroglycerin, have been used in clinical practice for more than one century for the treatment of angina, even before the identification of Nitric Oxide (NO) as the so-called Endothelium Derived Relaxing Factor (EDRF). Recently, multiple functions of this molecule in biology and pathophysiolo...

journal_title：Current topics in medicinal chemistry

authors： Bolla M,Almirante N,Benedini F

更新日期：2005-01-01 00:00:00

abstract：INTRODUCTION:Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as ho...

journal_title：Current topics in medicinal chemistry

authors： Pant A,Pasupureddy R,Pande V,Seshadri S,Dixit R,Pandey KC

更新日期：2017-01-01 00:00:00