Determination of circular dichroism and ultraviolet spectral parameters of norgestimate- and other Delta(4)-3-ketosteroid oxime isomers via normal phase HPLC method.

abstract：:Excitatory neurotransmission mediated by NMDA (N-methyl-D-aspartic acid) receptors plays a key role in both healthy and diseased processes in the brain. Therefore, bioactive compounds that can interact selectively with these receptors have been the aim of extensive research in the search of effective therapeutic agent...

journal_title：Current medicinal chemistry

authors： Bonaccorso C,Micale N,Ettari R,Grasso S,Zappalà M

更新日期：2011-01-01 00:00:00

abstract：:Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...

journal_title：Current medicinal chemistry

authors： Fanzani L,Porta F,Meneghetti F,Villa S,Gelain A,Lucarelli AP,Parisini E

更新日期：2015-01-01 00:00:00

abstract：:Antimicrobial resistance is an ever-increasing problem throughout the world and has already reached severe proportions. Two very common neglected tropical diseases are Chagas' disease and leishmaniasis. Chagas' disease is a severe health problem, mainly in Latin America, causing approximately 50000 deaths a year and m...

journal_title：Current medicinal chemistry

authors： Bandyopadhyay D,Samano S,Villalobos-Rocha JC,Sanchez-Torres LE,Nogueda-Torres B,Rivera G,Banik BK

更新日期：2017-01-01 00:00:00

abstract：:Synthetic compounds with a tri- and tetra-substituted imidazole scaffold are known as selective inhibitors of the p38 mitogen-activated protein (MAP) kinase responsible for proinflammatory cytokine release. The scope is to review the literature describing their design, synthesis and activity studies. To date a great p...

journal_title：Current medicinal chemistry

authors： Scior T,Domeyer DM,Cuanalo-Contreras K,Laufer SA

更新日期：2011-01-01 00:00:00

abstract：:Fluoxetine is an antidepressant drug, a potent and specific inhibitor of serotonin reuptake (SSRI). Evidence suggests that being compared with tricyclic antidepressants, fluoxetine may cause significantly fewer anticholinergic, antihistaminergic and cardiotoxic side effects in the treatment of major depressive disorde...

journal_title：Current medicinal chemistry

authors： Pacher P,Ungvari Z,Kecskemeti V,Furst S

更新日期：1998-10-01 00:00:00

abstract：:The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...

journal_title：Current medicinal chemistry

authors： Kalász H,Antal I

更新日期：2006-01-01 00:00:00

abstract：:During this past decade, science and engineering have seen a rapid increase in interest for nanoscale materials with dimensions less than 100 nm, which lie in the intermediate state between atoms and bulk (solid) materials. Their attributes are significantly altered relative to the corresponding bulk materials as they...

journal_title：Current medicinal chemistry

authors： Banerjee R,Katsenovich Y,Lagos L,McIintosh M,Zhang X,Li CZ

更新日期：2010-01-01 00:00:00

abstract：BACKGROUND:Chronic, degenerative diseases are often characterized by inflammation and aberrant angiogenesis. For these pathologies, including rheumatoid arthritis, cardiovascular and autoimmune diseases, cancer, diabetes, and obesity, current therapies have limited efficacy. OBJECTIVES:The validation of novel (chemo)p...

journal_title：Current medicinal chemistry

authors： Albini A,Bassani B,Baci D,Dallaglio K,Gallazzi M,Corradino P,Bruno A,Noonan DM

更新日期：2019-01-01 00:00:00

abstract：:Mast cells are best known as central effector cells in IgE-mediated type I allergic diseases including asthma and hay fever. An increasing amount of evidence, however, has demonstrated that mast cells are sentinel cells playing a critical role in host defense against invading microbes. Mast cells are located immediate...

journal_title：Current medicinal chemistry

authors： Matsuguchi T

更新日期：2012-01-01 00:00:00

abstract：:The term Lewy body diseases (LBDs) refers to a subset of neurodegenerative disorders that share the accumulation of the so-called Lewy bodies (LB) including: Parkinson's disease (PD), dementia with Lewy bodies (DLB), and PD later characterized by the occurrence of dementia (PDD). Moreover, multiple system atrophy (MSA...

journal_title：Current medicinal chemistry

authors： Bauckneht M,Arnaldi D,Nobili F,Aarsland D,Morbelli S

更新日期：2018-01-01 00:00:00

abstract：:Chymase stored in mast cells activates matrix metalloproteinase (MMP)-9, which may relate to the progression of sinusoidal obstruction syndrome (SOS). We investigated the preventive effect of a chymase inhibitor, TY-51469, on monocrotaline-induced SOS in hamsters. Hamsters were orally administrated with a single dose ...

journal_title：Current medicinal chemistry

authors： Masubuchi S,Komeda K,Takai S,Jin D,Tashiro K,Li ZL,Otsuki Y,Okamura H,Hayashi M,Uchiyama K

更新日期：2013-01-01 00:00:00

abstract：:The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying...

journal_title：Current medicinal chemistry

authors： Rocha S,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-01-01 00:00:00

abstract：:Irinotecan, a camptothecin analogue, is a prodrug which requires bioactivation to form the active metabolite SN-38. SN-38 acts as a DNA topoisomerase I poison. Irinotecan has been widely used in the treatment of metastatic colorectal cancer, small cell lung cancer and several other solid tumors. However, large inter-p...

journal_title：Current medicinal chemistry

authors： Ma MK,McLeod HL

更新日期：2003-01-01 00:00:00

abstract：:Protein C is a vitamin K-dependent anticoagulant serine protease zymogen in plasma which upon activation by the thrombin-thrombomodulin complex down-regulates the coagulation cascade by degrading cofactors Va and VIIIa by limited proteolysis. In addition to its anticoagulant function, activated protein C (APC) also bi...

journal_title：Current medicinal chemistry

authors： Rezaie AR

更新日期：2010-01-01 00:00:00

abstract：:Selenium is an essential trace element. It is, however toxic at concentration little above which is required for health. Selenium is incorporated into proteins as selenocysteine, the 21(st) amino acid. Selenoproteins are found in bacteria, archaea and eukaryotes. Biochemical and physicochemical properties of selenium ...

journal_title：Current medicinal chemistry

authors： Soriano-Garcia M

更新日期：2004-06-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an age-related neurodegenerative disorder that is believed to have complex genetic and environmental influences in the pathogenesis, but etiologies are unidentified for most patients. Until the major causes are better defined, drug development is directed at downstream pathophysi...

journal_title：Current medicinal chemistry

authors： Blasco H,Mavel S,Corcia P,Gordon PH

更新日期：2014-01-01 00:00:00

abstract：:The immunophilin ligands cyclosporin A, FK506 and rapamycin are best known for their immunosuppressive properties and their clinical use in transplantation medicine. These compounds or their analogs are also clinically used or investigated in various types of cancer, coronary angioplasty, dermatology, hepatitis C infe...

journal_title：Current medicinal chemistry

authors： Gaali S,Gopalakrishnan R,Wang Y,Kozany C,Hausch F

更新日期：2011-01-01 00:00:00

abstract：:Cinnamic acid and its phenolic analogues are natural substances. Chemically, in cinnamic acids the 3-phenyl acrylic acid functionality offers three main reactive sites; substitution at the phenyl ring, addition at the α,β- unsaturation and the reactions of the carboxylic acid functionality. Owing to these chemical asp...

journal_title：Current medicinal chemistry

authors： De P,Baltas M,Bedos-Belval F

更新日期：2011-01-01 00:00:00

abstract：:The importance of organometallics can be noticed by their presence in all life organisms. The most known natural organometallic molecule is vitamin B12, a porphyrin containing a cobalt atom, useful for several enzymatic transformations. Based on the remarkable properties of this class of compounds, a new area of medic...

journal_title：Current medicinal chemistry

authors： Chavain N,Biot C

更新日期：2010-01-01 00:00:00

abstract：:Fulvestrant is a novel endocrine therapy for breast cancer, with a unique structure and mode of action. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant has reached the clinic via extensive pre-clinical and clinic...

journal_title：Current medicinal chemistry

authors： Johnston SJ,Cheung KL

更新日期：2010-01-01 00:00:00

abstract：:Over the last centuries, there were many important discoveries in medicine that were crucial for gaining a better understanding of several physiological processes. Molecular modelling techniques are powerful tools that have been successfully used to analyse and interface medicinal chemistry studies with electrochemica...

journal_title：Current medicinal chemistry

authors： Almeida MO,Maltarollo VG,de Toledo RA,Shim H,Santos MC,Honorio KM

更新日期：2014-01-01 00:00:00

abstract：:Leukoaraiosis (LA), one of the most frequent causes of cognitive disturbances, is presumed to involve vascular demyelinization and cerebral small-vessel diseases. Although it has been suggested that the development of LA is associated with cerebral circulatory disturbances, the pathomechanism of this circulatory probl...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2007-01-01 00:00:00

abstract：BACKGROUND:The possibilities of treatment for oncological diseases are growing enormously in the last decades. Unfortunately, these developments have led to the onset of resistances with regards to the new treatments. This is particularly true if we face with the therapeutic field of Tyrosine Kinase Inhibitors (TKIs). ...

journal_title：Current medicinal chemistry

authors： Zanforlin E,Zagotto G,Ribaudo G

更新日期：2019-01-01 00:00:00

abstract：:Aberrant activation of the signal transducer and activator of transcription (STAT) 3 occurs in many human tumors. Constitutive STAT3 activity induces specific target genes that stimulate cell proliferation, prevent apoptosis, promote angiogenesis and facilitate tumor immune evasion. Thus, STAT3 is an attractive molecu...

journal_title：Current medicinal chemistry

authors： Zhao M,Jiang B,Gao FH

更新日期：2011-01-01 00:00:00

abstract：:Snake venoms are natural sources of biologically active molecules that are able to act selectively and specifically on different cellular targets, modulating physiological functions. Thus, these mixtures, composed mainly of proteins and peptides, provide ample and challenging opportunities and a diversified molecular ...

journal_title：Current medicinal chemistry

authors： Almeida JR,Resende LM,Watanabe RK,Carregari VC,Huancahuire-Vega S,da S Caldeira CA,Coutinho-Neto A,Soares AM,Vale N,de C Gomes PA,Marangoni S,de A Calderon L,Da Silva SL

更新日期：2017-01-01 00:00:00

abstract：:There is evidence that hyperglycemia results in the generation of reactive oxygen species, leading to oxidative stress in various tissues, including vascular system. An important link between oxidative stress, inflammatory response and insulin activity is now well established. The ability of antioxidants to protect ag...

journal_title：Current medicinal chemistry

authors： Nicolle E,Souard F,Faure P,Boumendjel A

更新日期：2011-01-01 00:00:00

abstract：:The chemokine receptor, CXCR4, is a GPCR that transduces signals of its endogenous ligand, CXCL12 (stromal cell-derived factor-1, SDF-1). The CXCL12-CXCR4 system plays an important role in the migration of progenitors during embryologic development of the cardiovascular, hemopoietic, central nervous systems, etc. This...

journal_title：Current medicinal chemistry

authors： Tamamura H,Tsutsumi H,Masuno H,Fujii N

更新日期：2007-01-01 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：:Fourier-transform infrared (FT-IR) based mapping and imaging is a fast emerging technology which is being increasingly applied to investigate tissues in the high-throughput mode. The high resolution close to the cellular level, the possibility to determine the bio-distribution of molecules of interest (proteins, pepti...

journal_title：Current medicinal chemistry

authors： Petter CH,Heigl N,Rainer M,Bakry R,Pallua J,Bonn GK,Huck CW

更新日期：2009-01-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00