Bacterial ribosomal subunit assembly is an antibiotic target.

abstract：AIM:The aim of this study is to synthesize, characterize and biological evaluation of 3-ethyl 5- methyl2-(2-aminoethoxy)-4-(2-chlorophenyl)-1,4-dihydropyridine-3,5-dicarboxylate derivatives. BACKGROUND:An efficient synthesis of two series of novel carbamate and sulfonamide derivatives of amlodipine, 3-ethyl 5-methyl 2...

journal_title：Current topics in medicinal chemistry

authors： Sudhana SM,Adi PJ

更新日期：2019-01-01 00:00:00

abstract：:The use of vaccines has led to tremendous decreases in disease burdens across the world. Many challenges remain in expanding vaccine coverage to new pathogens, however, a struggle further hampered by a lack of understanding into many of the fundamental processes through which vaccines elicit robust immunity. In this r...

journal_title：Current topics in medicinal chemistry

authors： Platt A,Wetzler L

更新日期：2013-01-01 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：:Internucleotide phosphodiester linkages in non-modified oligonucleotides are quickly degraded by nucleolytic enzymes present in the cells and this feature practically eliminates natural DNA and RNA molecules from medical applications and from many structural and mechanistic studies. P-chiral oligonucleotide analogs, i...

journal_title：Current topics in medicinal chemistry

authors： Guga P

更新日期：2007-01-01 00:00:00

abstract：:Cardiovascular disease represents an unparalleled proportion of the global burden of disease and will remain the main cause of mortality for the near future. Fortunately, most premature cardiovascular deaths are preventable. Therefore, prevention becomes vital and diet has shown beneficial effects to protect from CVD ...

journal_title：Current topics in medicinal chemistry

authors： Núñez-Córdoba JM,Martínez-González MA

更新日期：2011-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Scotti MT,Muratov EN,González-Díaz H

更新日期：2019-01-01 00:00:00

abstract：:Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters s...

journal_title：Current topics in medicinal chemistry

authors： Colabufo NA,Berardi F,Contino M,Niso M,Perrone R

更新日期：2009-01-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) are a class of peptides found across a wide array of organisms that play key roles in host defense. AMPs induce selective death in target cells and orchestrate specific or nonspecific immune responses. Many AMPs exhibit native anticancer activity in addition to antibacterial activity, and...

journal_title：Current topics in medicinal chemistry

authors： Rubin SJS,Qvit N

更新日期：2020-01-01 00:00:00

abstract：:Glucuronidation has been recognized as an important clearance mechanism in humans. Therefore, knowledge about the contribution of glucuronidation to clearance of drug candidates is of great value in early drug development. In this article, we discuss the recent progress made to predict in vivo glucuronidation paramete...

journal_title：Current topics in medicinal chemistry

authors： Wu B,Dong D,Hu M,Zhang S

更新日期：2013-01-01 00:00:00

abstract：:Multiple Gαi protein-coupled somatostatin receptors (SSTRs) are expressed in human kidney and liver tissues. Also, aberrant cAMP signaling has been shown to play a critical role in cysto-genesis and enlargement of the human kidney and liver. Thus, somatostatin (SST) analogs become potential and promising alternatives ...

journal_title：Current topics in medicinal chemistry

authors： Sun L,Yu CY,Mackey LV,Coy DH

更新日期：2015-01-01 00:00:00

abstract：:Liver cancer is the fifth (6.3% of all cancers i.e., 548,000 cases/year) and ninth (2.8% of all cancers i.e., 244,000 cases/year) most prevalent cancer worldwide in men and women, respectively. Although multiple choices of therapies are offered for Hepatocellular Carcinoma (HCC) like liver resection or transplant, rad...

journal_title：Current topics in medicinal chemistry

authors： Kumar S,Fayaz F,Pottoo FH,Bajaj S,Manchanda S,Bansal H

更新日期：2020-01-01 00:00:00

abstract：:The gradual alignment with all of drug metabolism with all aspects of drug discovery and development has led to a complete realignment of the way the work is conducted. From a background of conducting bespoke in vivo studies much of the work is now in a high throughput screening mode. Large technological advances have...

journal_title：Current topics in medicinal chemistry

authors： Smith DA

更新日期：2011-01-01 00:00:00

abstract：:Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. Aurora kinases have been regarded as a new target for cancer thera...

journal_title：Current topics in medicinal chemistry

authors： Qi G,Liu J,Mi S,Tsunematsu T,Jin S,Shao W,Liu T,Ishimaru N,Tang B,Kudo Y

更新日期：2018-01-01 00:00:00

abstract：:Several non-cardiovascular drugs have been withdrawn from the market due to their inhibition of hERG K+ channels that can potentially lead to severe heart arrhythmia and death. As hERG safety testing is a mandatory FDArequired procedure, there is a considerable interest for developing predictive computational tools to...

journal_title：Current topics in medicinal chemistry

authors： Braga RC,Alves VM,Silva MF,Muratov E,Fourches D,Tropsha A,Andrade CH

更新日期：2014-01-01 00:00:00

abstract：:Identifying drug binding sites and elucidating drug action mechanisms are important components in a drug discovery process. In this review, we briefly compared three different approaches (sequence- based methods, structure-based methods and probe-based molecular dynamics (MD) methods) to identifying drug binding sites...

journal_title：Current topics in medicinal chemistry

authors： Wang Y,Lupala CS,Liu H,Lin X

更新日期：2018-01-01 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：:Many efforts are currently being made to connect small molecules to target proteins by extracting pharmacological data from bibliographic sources and storing them in annotated chemical libraries. Here, small molecules are further connected to biological pathways, with particular focus to pathways involving members of ...

journal_title：Current topics in medicinal chemistry

authors： Hettne K,Cases M,Boyer S,Mestres J

更新日期：2007-01-01 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：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 00:00:00

abstract：:Dementia is an increasing health problem in older aged populations worldwide. Age-related changes in the brain can be observed decades before the first symptoms of cognitive decline appear. Cognitive impairment has chronic inflammatory components, which can be enhanced by systemic immune activation. There exist mutual...

journal_title：Current topics in medicinal chemistry

authors： Leblhuber F,Steiner K,Geisler S,Fuchs D,Gostner JM

更新日期：2020-01-01 00:00:00

abstract：:Most drug discovery programs today originate by selection of 'hit' molecules resulting from assays against large compound screening libraries. The chemical space in which these hits reside has implications for its biological activity in vivo and likelihood of progression to a drug candidate. We have created a database...

journal_title：Current topics in medicinal chemistry

authors： Zuegg J,Cooper MA

更新日期：2012-01-01 00:00:00

abstract：:Salbutamol forms an important and widely administered β2 agonist prescribed in the symptomatic treatment of bronchial asthma. Unfortunately, a subset of patients show refractoriness to it owing to ADRB2 gene variant (rs 1800888). The variant substitutes Thr to Ile at the position 164 in the β2 adrenergic receptor lead...

journal_title：Current topics in medicinal chemistry

authors： Bandaru S,Tiwari G,Akka J,Marri VK,Alvala M,Gutlapalli VR,Nayarisseri A,Mundluru HP

更新日期：2015-01-01 00:00:00

abstract：:It is well established that matrix metalloproteinases (MMPs) contribute to the degradation of the extracellular matrix of coronary plaque and contribute to the thinning of the fibrous cap. As a result, the atheromatous plaque becomes unstable and prone to rupture with consequent clinical manifestations including acute...

journal_title：Current topics in medicinal chemistry

authors： Papageorgiou N,Tousoulis D,Hatzis G,Briasoulis A,Androulakis E,Giolis A,Siasos G,Latsios G,Vogiatzi G,Tentolouris C,Stefanadis C

更新日期：2012-01-01 00:00:00

abstract：:Glycopeptide antibiotics are complex natural products biosynthesized by several actinomycete genera. They inhibit bacterial growth by interfering with cell wall biosynthesis. Glycopeptide antibiotics consist of a heptapeptide skeleton highly modified through cross-links of the aromatic moieties. In addition, they are ...

journal_title：Current topics in medicinal chemistry

authors： Donadio S,Sosio M

更新日期：2008-01-01 00:00:00

abstract：:Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug di...

journal_title：Current topics in medicinal chemistry

authors： Leadley RJ Jr

更新日期：2001-06-01 00:00:00

abstract：:Interest in the chemistry and biological properties of non-nucleoside N-glycosidic compounds has gathered pace over the past several years; the occurrence of the N-glycoside moiety in glycoproteins and a range of active natural products has prompted the synthesis of a diverse spectrum of related materials with promisi...

journal_title：Current topics in medicinal chemistry

authors： Norris P

更新日期：2008-01-01 00:00:00

abstract：:Low drug productivity has been a significant problem of the pharmaceutical industry for several decades even though numerous novel technologies were introduced during this period. Currently pharmacologic dogma, "single drug, single target, single disease", is at the root of the lack of drug productivity. From a system...

journal_title：Current topics in medicinal chemistry

authors： Ye H,Wei J,Tang K,Feuers R,Hong H

更新日期：2016-01-01 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：:Parkinson's disease is a motor dysfunction that has been widely studied but many of the reports on commercial drugs for the treatment of this disease have afforded some undesirable side effects that generate an extensive and unviable treatment by economic costs and due to the bioavailability of the assayed compounds. ...

journal_title：Current topics in medicinal chemistry

authors： Fazel Nabavi S,Uriarte E,Rastrelli L,Modak B,Sobarzo-Sánchez E

更新日期：2016-01-01 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