The medicinal chemistry of agents targeting monoacylglycerol lipase.

abstract：:Transition metal complexes with terpyridine ligands have attracted a widespread interest with respect to biomedical applications: [(tpy)PtCl]Cl and [(tpy)RuCl(3)] are potent anti-tumor agents with activities comparable to those of cisplatin and carboplatin. The Ru(II) complexes feature a high potential as reactive pro...

journal_title：Current topics in medicinal chemistry

authors： Winter A,Gottschaldt M,Newkome GR,Schubert US

更新日期：2012-01-01 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：:Results of various projects on Mexican Indian ethnobotany and some of the subsequent pharmacological and phytochemical studies are summarised focusing both on chemical-pharmacological as well as anthropological (ethnopharmacological) aspects of our research. We have identified taste and smell properties of medicinal (...

journal_title：Current topics in medicinal chemistry

authors： Heinrich M

更新日期：2003-01-01 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：:Plasmodium has a complex life cycle that spans between mosquito and human. For survival and pathogenesis it banks upon dynamic alterations in ionic transport across organelle and plasma membrane. Being a fundamental contributor of crucial biological processes in parasite, ionic balance facilitates parasite invasion, a...

journal_title：Current topics in medicinal chemistry

authors： Bharti H,Singal A,Raza M,Ghosh PC,Nag A

更新日期：2019-01-01 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

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：: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：:A proper balance between oxidants and antioxidants is necessary in maintaining health and longevity. Alterations in this balance may result in oxidative stress causing functional disorders and diseases. Oxidative stress is considered to play a vital role in the pathogenesis of diabetes and its complications. Flavanone...

journal_title：Current topics in medicinal chemistry

authors： Sharma M,Akhtar N,Sambhav K,Shete G,Bansal AK,Sharma SS

更新日期：2015-01-01 00:00:00

abstract：:Prenatal alcohol (ethanol) exposure (PAE) is the underlying cause for a variety of birth defects and neurodevelopmental deficits referred to as "Fetal Alcohol Spectrum Disorders (FASD)". The more visible phenotypes caused by PAE include growth retardation, and characteristic craniofacial abnormalities associated with ...

journal_title：Current topics in medicinal chemistry

authors： Liyanage VR,Curtis K,Zachariah RM,Chudley AE,Rastegar M

更新日期：2017-01-01 00:00:00

abstract：:Latest microarray-based technologies, including small molecule-, peptide-, protein- and cell-based arrays, and their applications in the field of proteomics are reviewed. ...

journal_title：Current topics in medicinal chemistry

authors： Chen GY,Uttamchandani M,Lue RY,Lesaicherrea ML,Yao SQ

更新日期：2003-01-01 00:00:00

abstract：:The human tuberculosis (TB) is primarily caused by Mycobacterium tuberculosis (Mtb) that inhabits inside and amidst immune cells of the host with adapted physiology to regulate interdependent cellular functions with intact pathogenic potential. The complexity of this disease is attributed to various factors such as th...

journal_title：Current topics in medicinal chemistry

authors： Borah P,Deb PK,Venugopala KN,Al-Shar'i NA,Singh V,Deka S,Srivastava A,Tiwari V,Mailavaram RP

更新日期：2020-12-11 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：: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：: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：:One of the major events occurring at biological interfaces is the specific recognition of bioactive ligands by their receptor proteins. The elucidation of interacting partners is an immediate entrance into the discovery of medicinal leads. The method of photoaffinity labeling enables the direct probing of target prote...

journal_title：Current topics in medicinal chemistry

authors： Hatanaka Y,Sadakane Y

更新日期：2002-03-01 00:00:00

abstract：:This chapter describes the life cycle, general morphology and ultrastructure of the larval and adult stages of Taenia solium, a parasitic flatworm of humans found in underdeveloped countries. Experimental results describing the role of proteins and glycoproteins in the host-parasite relationship, as well as the variou...

journal_title：Current topics in medicinal chemistry

authors： Willms K

更新日期：2008-01-01 00:00:00

abstract：:Antimicrobial peptides (AMPs) establish the first line of host defense mechanism against invading microorganisms including bacteria, viruses, fungi and parasites. In recent years, emergence and spread of antibiotic resistance bacterial pathogens have dawn considerable interest in investigations of AMPs. The ability of...

journal_title：Current topics in medicinal chemistry

authors： Bhattacharjya S

更新日期：2016-01-01 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：:Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However,...

journal_title：Current topics in medicinal chemistry

authors： Zhou XX,Littler E

更新日期：2006-01-01 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：:A better understanding of the biology and pathogenesis of hematological malignancies has led to the development of immunotherapeutic and immunoregulatory drugs. Many of these agents have revolutionized the current treatment modalities, while others are under investigation. Rituximab (anti-CD20 antibody) has been estab...

journal_title：Current topics in medicinal chemistry

authors： Pangalis GA,Kyrtsonis MC,Vassilakopoulos TP,Dimopoulou MN,Siakantaris MP,Emmanouilides C,Doufexis D,Sahanas S,Kontopidou FN,Kalpadakis C,Angelopoulou MK,Dimitriadou EM,Kokoris SI,Panayiotidis P

更新日期：2006-01-01 00:00:00

abstract：:Although bioactivation is a well-documented process and the role of active metabolites in the drug discovery field has long been recognized, drug metabolites are usually ignored in virtual screening campaigns oriented to drug repositioning. The present article discusses different issues related to overlooking of the a...

journal_title：Current topics in medicinal chemistry

authors： Talevi A

更新日期：2016-01-01 00:00:00

abstract：:Three distinct chemical classes for the control of gastrointestinal nematodes are available: benzimidazoles, imidazothiazoles, and macrocyclic lactones. The relentless development of drug resistance has severely limited the usefulness of such drugs and the search for a new class of compounds preferably with a differ...

journal_title：Current topics in medicinal chemistry

authors： Lee BH,Clothier MF,Dutton FE,Nelson SJ,Johnson SS,Thompson DP,Geary TG,Whaley HD,Haber CL,Marshall VP,Kornis GI,McNally PL,Ciadella JI,Martin DG,Bowman JW,Baker CA,Coscarelli EM,Alexander-Bowman SJ,Davis JP,Zinser E

更新日期：2002-07-01 00:00:00

abstract：:Tuberculosis (TB) is caused by the bacterium Mycobacterium tuberculosis and is a common infectious disease with high mortality and morbidity. The increasing prevalence of drug-resistant strains of TB presents a major public health problem. Due to the lack of effective drugs to treat these drug-resistant strains, the d...

journal_title：Current topics in medicinal chemistry

authors： Koseki Y,Aoki S

更新日期：2014-01-01 00:00:00

abstract：:Sphingosine 1-phosphate (S1P) evokes a plethora of physiological responses by stimulating members of a G protein-coupled receptor family, known as S1P receptors. Currently five different mammalian S1P receptor subtypes, S1P₁₋₅, each with a different cellular expression pattern, were identified. The S1P₁ receptor in pa...

journal_title：Current topics in medicinal chemistry

authors： Bolli MH,Lescop C,Nayler O

更新日期：2011-01-01 00:00:00

abstract：:Schizophrenia (SZ) is a severe neuropsychiatric disorder. A leading hypothesis is that SZ is a brain dysconnection syndrome, involving abnormal interactions between widespread brain networks. Resting state functional magnetic resonance imaging (R-fMRI) is a powerful tool to explore the dysconnectivity of brain network...

journal_title：Current topics in medicinal chemistry

authors： Yu Q,Allen EA,Sui J,Arbabshirani MR,Pearlson G,Calhoun VD

更新日期：2012-01-01 00:00:00

abstract：:The invading microbial pathogens are controlled by the rapid and effective innate immune responses sequentially formation of the long-lasting adaptive memories. Toll-like receptors (TLRs) play a vital role in innate and adaptive immune response by function as a bridge to modulate the immune response. Further, genetic ...

journal_title：Current topics in medicinal chemistry

authors： Xu Q,Zhu G,Li J,Cheng K

更新日期：2017-01-01 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：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