Surface chemistry influences implant biocompatibility.

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：:Ropivacaine, the S-(-)-enantiomer of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinecarboxamide is a new long-acting local anesthetic. This review demonstrates that it is effective in brachial plexus anesthesia. It is at least as efficient as bupivacaine in terms of quality, duration of analgesia, anesthesia, and motor b...

journal_title：Current topics in medicinal chemistry

authors： Singelyn FJ

更新日期：2001-08-01 00:00:00

abstract：:Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivati...

journal_title：Current topics in medicinal chemistry

authors： Li HT,Zhu X

更新日期：2020-06-18 00:00:00

abstract：:Chagas disease and African sleeping sickness are trypanosomal infections that represent important public health problems in Latin America and Africa, respectively. The restriction of these diseases to the poorer parts of the world has meant that they have been largely neglected and limited progress has been made in th...

journal_title：Current topics in medicinal chemistry

authors： Wilkinson SR,Bot C,Kelly JM,Hall BS

更新日期：2011-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Nayarisseri A,Hood EA

更新日期：2018-01-01 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：: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：:Protein-ligand binding is among the most fundamental phenomena underlying all molecular biology, and a greater ability to more accurately and robustly predict the binding free energy of a small molecule ligand for its cognate protein is expected to have vast consequences for improving the efficiency of pharmaceutical ...

journal_title：Current topics in medicinal chemistry

authors： Abel R,Wang L,Mobley DL,Friesner RA

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：: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：:Protein kinases (Ser/Thr and Tyr) play a key role in signal transduction pathways. It has been shown that deregulation of the Cdk activity is linked to cell proliferation and cancer. Inhibition of cyclin-dependent kinases (Cdks) is an important target for potential new anti-cancer drugs. Following the discovery of Olo...

journal_title：Current topics in medicinal chemistry

authors： Haesslein JL,Jullian N

更新日期：2002-09-01 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：:Untargeted metabolomics is a promising approach for reducing the significant attrition rate for discovering and developing drugs in the pharmaceutical industry. This review aims to highlight the practical decision-making value of untargeted metabolomics for the advancement of drug candidates in drug discovery/developm...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Leo GC

更新日期：2017-01-01 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 dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinson's disease, Alzheimer's disease, schizophrenia, Tourette's syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as...

journal_title：Current topics in medicinal chemistry

authors： Runyon SP,Carroll FI

更新日期：2006-01-01 00:00:00

abstract：:The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

journal_title：Current topics in medicinal chemistry

authors： Aiello F,Valacchi G

更新日期：2014-01-01 00:00:00

abstract：:Computational toxicity modeling can have significant impact in the drug discovery process, especially when utilized as a sentinel filter for common drug safety liabilities, such as mutagenicity, carcinogenicity and teratogenicity. This review will focus on the strengths and limitations of the current computational mod...

journal_title：Current topics in medicinal chemistry

authors： Pearl GM,Livingston-Carr S,Durham SK

更新日期：2001-09-01 00:00:00

abstract：INTRODUCTION:Fabaceae are a rich source of protease inhibitors. METHODS:A proteinaceous protease inhibitor of 25 KDa designated as Macrotyloma uniflorum protease inhibitor (MUPI) was isolated from seeds of Macrotyloma uniflorum and purified to homogeneity by ammonium sulphate precipitation, DEAE Sepharose column and C...

journal_title：Current topics in medicinal chemistry

authors： Mohan M,Elyas KK

更新日期：2018-01-01 00:00:00

abstract：:In situ structural characterization of organic compounds attached to solid supports can be achieved by high-resolution magic angle spinning NMR (HRMAS NMR), a technique that provides solution-like spectra for resin-bound molecules. This review outlines the principles of the technique, the influence of the solid suppor...

journal_title：Current topics in medicinal chemistry

authors： Espinosa JF

更新日期：2011-01-01 00:00:00

abstract：:Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that ar...

journal_title：Current topics in medicinal chemistry

authors： Minkkilä A,Saario S,Nevalainen T

更新日期：2010-01-01 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：: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：: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：BACKGROUND:The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition. OBJECTIVE:This review surveys the state of developments in structural analysis, compound screening, and structure-based ...

journal_title：Current topics in medicinal chemistry

authors： Gewirth DT

更新日期：2016-01-01 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：: ...

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：:The majority of functionally important biological processes are regulated by allosteric communication within individual proteins and across protein complexes. The proteins controlling these communication networks respond to changes in the cellular environment by switching between different conformational states. Targe...

journal_title：Current topics in medicinal chemistry

authors： Persico M,Di Dato A,Orteca N,Fattorusso C,Novellino E,Andreoli M,Ferlini C

更新日期：2015-01-01 00:00:00

abstract：:Numerical characterization of molecular structure is a first step in many computational analysis of chemical structure data. These numerical representations, termed descriptors, come in many forms, ranging from simple atom counts and invariants of the molecular graph to distribution of properties, such as charge, acro...

journal_title：Current topics in medicinal chemistry

authors： Guha R,Willighagen E

更新日期：2012-01-01 00:00:00

abstract：:Anticancer drug screening can accelerate drug discovery to save the lives of cancer patients, but cancer heterogeneity makes this screening challenging. The prediction of anticancer drug sensitivity is useful for anticancer drug development and the identification of biomarkers of drug sensitivity. Deep learning, as a ...

journal_title：Current topics in medicinal chemistry

authors： Tan X,Yu Y,Duan K,Zhang J,Sun P,Sun H

更新日期：2020-01-01 00:00:00

abstract：:The sol-gel process provides a robust and versatile technology for the immobilization of biologicals. A wide range of inorganic, composites and hybrid materials can be prepared to encapsulate molecular drugs, proteins, antibodies/antigens, enzymes, nucleic acids, prokaryotic and eukaryotic cells into bulk gels, partic...

journal_title：Current topics in medicinal chemistry

authors： Wang X,Ahmed NB,Alvarez GS,Tuttolomondo MV,Hélary C,Desimone MF,Coradin T

更新日期：2015-01-01 00:00:00