Small molecules as friends and foes of the immune system.

abstract：:The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mech...

journal_title：Future medicinal chemistry

authors： Dias C,Rauter AP

更新日期：2019-02-25 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：:The dynamic nature of histone post-translational modifications such as methylation or acetylation makes possible the alteration of disease associated epigenetic states through the manipulation of the associated epigenetic machinery. One approach is through small molecule perturbation. Chemical probes of epigenetic rea...

journal_title：Future medicinal chemistry

authors： Waybright JM,James LI

更新日期：2020-01-10 00:00:00

abstract：:Lysophosphatidic acid (LPA) and its receptors, LPA1-6, are integral parts of signaling pathways involved in cellular proliferation, migration and survival. These signaling pathways are of therapeutic interest for the treatment of multiple types of cancer and to reduce cancer metastasis and side effects. Validated ther...

journal_title：Future medicinal chemistry

authors： Parrill AL

更新日期：2014-05-01 00:00:00

abstract：AIM:To synthesize the new bioactive metabolites of mosapride (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxyben-zamide (R-isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxybenzamide (S-isomer) and evaluate their in vitro and in vivo pharmacological and ...

journal_title：Future medicinal chemistry

authors： Yao J,Li K,Song Y,He Z,Liu Z,Zhao L,Wang S

更新日期：2019-01-01 00:00:00

abstract：:Since their initial isolation from the marine alga Delisea pulchra, bromofuranones have been investigated as potential inhibitors of quorum sensing (QS) in various bacterial strains. QS is an important mechanism by which bacteria co-ordinate their molecular response to the environment. QS is intrinsically linked to ba...

journal_title：Future medicinal chemistry

authors： Lyons T,Gahan CG,O'Sullivan TP

更新日期：2020-11-01 00:00:00

abstract：:The compound class of 3-carboranyl thymidine analogues (3CTAs) are boron delivery agents for boron neutron capture therapy (BNCT), a binary treatment modality for cancer. Presumably, these compounds accumulate selectively in tumor cells via intracellular trapping, which is mediated by hTK1. Favorable in vivo biodistri...

journal_title：Future medicinal chemistry

authors： Khalil A,Ishita K,Ali T,Tjarks W

更新日期：2013-04-01 00:00:00

abstract：BACKGROUND:Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. DISCUSSION:Recent discoveries of non-nitrogenous...

journal_title：Future medicinal chemistry

authors： Lovell KM,Simpson DS,Cunningham CW,Prisinzano TE

更新日期：2009-05-01 00:00:00

abstract：BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

journal_title：Future medicinal chemistry

authors： Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

更新日期：2014-03-01 00:00:00

abstract：:Platinum-based anticancer agents have been widely used in the clinic to successfully treat many different types of cancer. However, the therapeutic efficacy of platinum drugs is limited by serious side effects and the occurrence of inherent or acquired resistance of tumor cells. Nanoparticulate drug-delivery systems h...

journal_title：Future medicinal chemistry

authors： Bryde S,de Kroon AI

更新日期：2009-11-01 00:00:00

abstract：:Spinal muscular atrophy (SMA) is an inherited neurodegenerative disease that results in progressive dysfunction of motor neurons of the anterior horn of the spinal cord. SMA is caused by the loss of full-length protein expression from the survival of motor neuron 1 (SMN1) gene. The disease has a unique genetic profile...

journal_title：Future medicinal chemistry

authors： Cherry JJ,Androphy EJ

更新日期：2012-09-01 00:00:00

abstract：:Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...

journal_title：Future medicinal chemistry

authors： Chung PY,Bian ZX,Pun HY,Chan D,Chan AS,Chui CH,Tang JC,Lam KH

更新日期：2015-01-01 00:00:00

abstract：:An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2016-01-01 00:00:00

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Kinetic and thermodynamic ligand-protein binding parameters are gaining growing importance as key information to consider in drug discovery. The determination of the molecular structures, using particularly x-ray and NMR techniques, is crucial for understanding how a ligand recognizes its target in the final binding c...

journal_title：Future medicinal chemistry

authors： Deganutti G,Moro S

更新日期：2017-04-01 00:00:00

abstract：AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...

journal_title：Future medicinal chemistry

authors： Al-Salahi R,Anouar EH,Marzouk M,Taie HA,Abuelizz HA

更新日期：2018-02-01 00:00:00

abstract：:The emergence of multidrug-resistant Mycobacterium tuberculosis strains has made many of the currently available anti-tuberculosis (TB) drugs ineffective. Accordingly, there is a pressing need to identify new drug targets. Filamentous temperature-sensitive protein Z (FtsZ), a bacterial tubulin homologue, is an essenti...

journal_title：Future medicinal chemistry

authors： Kumar K,Awasthi D,Berger WT,Tonge PJ,Slayden RA,Ojima I

更新日期：2010-08-01 00:00:00

abstract：:Mycobacterium tuberculosis (Mtb) acquires non-heme iron through salicylate-derived siderophores termed mycobactins whereas heme iron is obtained through a cascade of heme uptake proteins. Three proteins are proposed to mediate Mtb heme iron uptake, a secreted heme transporter (Rv0203), and MmpL3 and MmpL11, which are ...

journal_title：Future medicinal chemistry

authors： Owens CP,Chim N,Goulding CW

更新日期：2013-08-01 00:00:00

abstract：:Solomon Nwaka was born in Nigeria and grew up seeing at first hand the impact of neglected diseases. His research efforts have taken him across the globe, in both the developed and developing world. Following posts in academia, industry and at the Medicines for Malaria Venture, he is now at the WHO where he is engaged...

journal_title：Future medicinal chemistry

authors： Nwaka S

更新日期：2011-09-01 00:00:00

abstract：:Existing therapies for allergic asthma are far from perfect: the global prevalence of disease increases despite them and they are poorly effective in dealing with the exacerbations that account for hospitalization and asthma deaths. Commercially, there are pressures on these existing medicines too--a growing threat fr...

journal_title：Future medicinal chemistry

authors： Robinson C,Zhang J,Newton GK,Perrior TR

更新日期：2013-02-01 00:00:00

abstract：:Trichomonas vaginalis and Entamoeba histolytica are clinically important protozoa that affect humans. T. vaginalis produces sexually transmitted infections and E. histolytica is the causative agent of amebic dysentery. Metronidazole, a compound first used to treat T. vaginalis in 1959, is still the main drug used worl...

journal_title：Future medicinal chemistry

authors： Moya IA,Su Z,Honek JF

更新日期：2009-07-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the world today. Bronchodilators, particularly muscarinic antagonists and β(2) agonists, are recommended for patients with moderate to severe COPD. Dual-pharmacology muscarinic antagonist- β(2) agonist (MABA) molecules present an exc...

journal_title：Future medicinal chemistry

authors： Hughes AD,Jones LH

更新日期：2011-10-01 00:00:00

abstract：:Aim: Cysteine proteases are important molecular targets involved in the replication, virulence and survival of parasitic organisms, including Trypanosoma and Leishmania species. Methodology & results: Analogs of the 7-chloro-N-[3-(morpholin-4-yl)propyl]quinolin-4-amine were synthesized and their inhibitory activity ag...

journal_title：Future medicinal chemistry

authors： Andrade MM,Martins LC,Marques GV,Silva CA,Faria G,Caldas S,Dos Santos JS,Leclercq SY,Maltarollo VG,Ferreira RS,Oliveira RB

更新日期：2020-04-01 00:00:00

abstract：:Around 70-80% of drugs used in traditional Tibetan medicine (TTM) come from Qinghai Tibet Plateau, the majority of which are plants. The biological and medicinal culture diversity on Qinghai Tibet Plateau are amazing and constitute a less tapped resource for innovative drug research and development. Meanwhile, the pro...

journal_title：Future medicinal chemistry

authors： Hao DC,Xiao PG,Liu C

更新日期：2018-11-30 00:00:00

abstract：BACKGROUND:Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acu...

journal_title：Future medicinal chemistry

authors： Trifirò P,Cappa A,Brambillasca S,Botrugno OA,Cera MR,Zuffo RD,Dessanti P,Meroni G,Thaler F,Villa M,Minucci S,Mercurio C,Varasi M,Vianello P

更新日期：2017-07-01 00:00:00

abstract：:HIV/AIDS remains a formidable disease with millions of individuals inflicted worldwide. Although treatment regimens have improved considerably, drug resistance brought on by viral mutation continues to erode their effectiveness. Intense research efforts are currently underway in search of new and improved therapies. T...

journal_title：Future medicinal chemistry

authors： Ghosh AK,Anderson DD

更新日期：2011-07-01 00:00:00

abstract：:Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca2+-sensing receptors and Zn2+-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review prov...

journal_title：Future medicinal chemistry

authors： Pongkorpsakol P,Moonwiriyakit A,Muanprasat C

更新日期：2017-03-01 00:00:00

abstract：AIM:The assumption in scaffold hopping is that changing the scaffold does not change the binding mode and the same structure-activity relationships (SARs) are seen for substituents decorating each scaffold. Results/methodology: We present the use of matched series analysis, an extension of matched molecular pair analys...

journal_title：Future medicinal chemistry

authors： Hunt P,Segall M,O'Boyle N,Sayle R

更新日期：2017-01-01 00:00:00

abstract：:Due to the impermeable structure and barrier function of the blood-brain barrier (BBB), the delivery of therapeutic molecules into the CNS is extremely limited. Nanodelivery systems are regarded as the most effective and versatile carriers for the CNS, as they can transport cargo molecules across the BBB via various m...

journal_title：Future medicinal chemistry

authors： Kim KT,Lee HS,Lee JJ,Park EK,Lee BS,Lee JY,Bae JS

更新日期：2018-11-01 00:00:00

abstract：:Chronic pain is one of the most ubiquitous diseases in the world, but treatment is difficult with conventional methods, due to undesirable side effects of treatments and unknown mechanisms of pathological pain states. The endogenous peptide, dynorphin A has long been established as a target for the treatment of pain. ...

journal_title：Future medicinal chemistry

authors： Hall SM,Lee YS,Hruby VJ

更新日期：2016-01-01 00:00:00