Dual-pharmacology muscarinic antagonist and β₂ agonist molecules for the treatment of chronic obstructive pulmonary disease.

abstract：:The current state of antimalarial drug resistance emphasizes the need for new therapies with novel modes of action that will add a significant benefit compared with current standards. In this regard, high throughput phenotypic whole-cell screening aids the discovery of novel antiplasmodial scaffolds that are inherentl...

journal_title：Future medicinal chemistry

authors： Paquet T,Gordon R,Waterson D,Witty MJ,Chibale K

更新日期：2012-12-01 00:00:00

abstract：:Metabolic stability is an important property of drug candidates and pharmaceutical companies often have human liver microsomal (HLM) data for a large number of molecules, enabling development of global quantitative structure-activity relationship models. RESULTS:This study describes a strategy for building a global H...

journal_title：Future medicinal chemistry

authors： Stålring J,Sohlenius-Sternbeck AK,Terelius Y,Parkes K

更新日期：2018-07-01 00:00:00

abstract：:Responsive optical probes play a vital role in following and understanding biological events. In this review, we focus on the use of lanthanide complexes as molecular probes, as they offer many advantages in imaging and assays, particularly when used in time-gated protocols. We describe systems that illustrate the key...

journal_title：Future medicinal chemistry

authors： Allain C,Faulkner S

更新日期：2010-03-01 00:00:00

abstract：:Mammalian carbonic anhydrases (CAs; EC 4.2.1.1) of which 16 isoforms are known, are involved in important physiological functions. Their inhibition is exploited pharmacologically for the treatment of many diseases (glaucoma, edema, epilepsy, obesity, hypoxic tumors, neuropathic pain, etc.) but the activators were less...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2018-03-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：:Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicina...

journal_title：Future medicinal chemistry

authors： Murphy KE,Sloan GF,Lawhern GV,Volk GE,Shumate JT,Wolfe AL

更新日期：2020-11-01 00:00:00

abstract：:VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. As an essential receptor protein tyrosine kinase propagating cellular signal transduction processes, VEGFR-2 is a central target for drug discovery against tumor-associated angiogenesis. Since the autophosphorylation of VEGFR-2 re...

journal_title：Future medicinal chemistry

authors： Huang L,Huang Z,Bai Z,Xie R,Sun L,Lin K

更新日期：2012-09-01 00:00:00

abstract：:PA-824 is an experimental anti-tubercular agent that has a novel mechanism of action. It is effective against both active and persistent forms of the disease and has recently shown early bactericidal activity in a Phase II clinical trial. This review summarizes recent studies on the mode of action of PA-824 and outlin...

journal_title：Future medicinal chemistry

authors： Denny WA,Palmer BD

更新日期：2010-08-01 00:00:00

abstract：AIM:The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. RESULTS:Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both the...

journal_title：Future medicinal chemistry

authors： Amin NH,El-Saadi MT,Hefny AA,Abdelazeem AH,Elshemy HA,Abdellatif KR

更新日期：2018-12-06 00:00:00

abstract：AIM:There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including MAO-A, DYRK1A and cytotoxicity to several select cancer cell lines. RESULTS:Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against ...

journal_title：Future medicinal chemistry

authors： Haider S,Alhusban M,Chaurasiya ND,Tekwani BL,Chittiboyina AG,Khan IA

更新日期：2018-06-01 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

abstract：:CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability in a variety of cancers, including difficult-to-treat breast, ovarian, colorectal, brain and pancreatic cancers, and is synthetic lethal with PARP,...

journal_title：Future medicinal chemistry

authors： Tadesse S,Duckett DR,Monastyrskyi A

更新日期：2021-01-01 00:00:00

abstract：:The EGFR is one of the most popular targets for anticancer therapies and many drugs, such as erlotinib and gefitinib, have got enormous success in clinical treatments of cancer in past decade. However, the efficacy of these agents is often limited because of the quick emergence of drug resistance. Fundamental structur...

journal_title：Future medicinal chemistry

authors： Guan H,Du Y,Ning Y,Cao X

更新日期：2017-05-01 00:00:00

abstract：:New Delhi Metallo β-lactamase-1 (NDM-1) is a member of the Metallo-β-lactamase family, capable of catalyzing the hydrolysis of all β-lactam antibiotics. The rapid dissemination of NDM producers, 'superbugs', has become a worldwide concern to health workers. Seventeen different variants of NDM have been reported so far...

journal_title：Future medicinal chemistry

authors： Khan S,Ali A,Khan AU

更新日期：2018-01-01 00:00:00

abstract：:Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis acti...

journal_title：Future medicinal chemistry

authors： Pires CT,Scodro RB,Cortez DA,Brenzan MA,Siqueira VL,Caleffi-Ferracioli KR,Vieira LC,Monteiro JL,Corrêa AG,Cardoso RF

更新日期：2020-09-01 00:00:00

abstract：AIM:Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the acceler...

journal_title：Future medicinal chemistry

authors： de Almeida JR,Figueiro M,Almeida WP,de Paula da Silva CHT

更新日期：2018-05-01 00:00:00

abstract：BACKGROUND:Compound-quality scoring methods designed to evaluate multiple drug properties concurrently are useful to analyze and prioritize output from drug-design efforts. However, formalized multiparameter optimization approaches are not widely used in drug design. METHODS:We rank molecules synthesized in drug-disco...

journal_title：Future medicinal chemistry

authors： Nissink JW,Degorce S

更新日期：2013-05-01 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：: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：:With the goal of refining our discovery DMPK workflow, we conducted a retrospective analysis on internal Celgene compounds by calculating the physicochemical properties and gathering data from several assays including solubility, rat and human liver S9 stability, Caco-2 permeability, and rat intravenous (iv.) and oral...

journal_title：Future medicinal chemistry

authors： Kulkarni A,Riggs J,Phan C,Bai A,Calabrese A,Shi T,Moghaddam MF

更新日期：2014-02-01 00:00:00

abstract：:Epigallocatechin gallate (EGCG), one of polyphenols isolated from green tea, exhibits biology-benefiting effects with minimum severe adverse. EGCG is known to be a mitochondrion-targeting medicinal agent, regulating mitochondrial metabolism, including mitochondrial biogenesis, mitochondrial bioenergetics, and mitochon...

journal_title：Future medicinal chemistry

authors： Shi W,Li L,Ding Y,Yang K,Chen Z,Fan X,Jiang S,Guan Y,Liu Z,Xu D,Wu L

更新日期：2018-04-01 00:00:00

abstract：:Clinical development in brain diseases has one of the lowest success rates in the pharmaceutical industry, and many promising rationally designed single-target R&D projects fail in expensive Phase III trials. By contrast, successful older CNS drugs do have a rich pharmacology. This article will provide arguments sugge...

journal_title：Future medicinal chemistry

authors： Geerts H,Kennis L

更新日期：2014-01-01 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：:Background: Andrographolide and its benzylidene derivatives, SRJ09 and SRJ23, potentially bind oncogenic K-Ras to exert anticancer activity. Their molecular interactions with K-Ras oncoproteins that lead to effective biological activity are of major interest. Methods & results:In silico docking and molecular dynamics ...

journal_title：Future medicinal chemistry

authors： Quah SY,Tan MS,Ho KL,Manan NA,Gorfe AA,Deb PK,Sagineedu SR,Stanslas J

更新日期：2020-09-01 00:00:00

abstract：:Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% of deaths affecting the African region. Results/methodology: Microwave promoted the synthesis of cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmod...

journal_title：Future medicinal chemistry

authors： Rani A,Kumar S,Legac J,Adeniyi AA,Awolade P,Singh P,Rosenthal PJ,Kumar V

更新日期：2020-02-01 00:00:00

abstract：BACKGROUND:The pathogenicity of influenza A and B viruses depends on the function of influenza neuraminidase (NA). Emerging resistant influenza A viruses of subtype H1N1 increasingly challenge the effectiveness of established NA inhibitors. Recent computational studies have indicated several weak points of NA that can ...

journal_title：Future medicinal chemistry

authors： Kirchmair J,Rollinger JM,Liedl KR,Seidel N,Krumbholz A,Schmidtke M

更新日期：2011-03-01 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：: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：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：:The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...

journal_title：Future medicinal chemistry

authors： Zhang W,Fujii N,Naren AP

更新日期：2012-03-01 00:00:00