Membrane-targeting antibiotics: recent developments outside the peptide space.

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：:Epothilone is a newly developed antitumor drug; its antitumor principle is to stop the cell cycle by binding to tubulin in tumor cells, promoting tubulin polymerization, inhibiting depolymerization of microtubules, and ultimately inducing apoptosis. There are many analogs of epothilone, such as epothilone B, epothilon...

journal_title：Future medicinal chemistry

authors： Cheng H,Huang G

更新日期：2018-06-01 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：: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：:New antibacterials that modulate less explored targets are needed to fight the emerging bacterial resistance. DNA gyrase and topoisomerase IV are attractive targets in this search. These are both type II topoisomerases that can cleave both DNA strands, and can thus alter DNA topology during replication or similar proc...

journal_title：Future medicinal chemistry

authors： Barančoková M,Kikelj D,Ilaš J

更新日期：2018-05-01 00:00:00

abstract：:Endogenous nucleotides have widespread actions in the cardiovascular system, but it is only recently that the P2X and P2Y receptor subtypes, at which they act, have been identified and subtype-selective agonists and antagonists developed. These advances have greatly increased our understanding of the physiological and...

journal_title：Future medicinal chemistry

authors： Kennedy C,Chootip K,Mitchell C,Syed NI,Tengah A

更新日期：2013-03-01 00:00:00

abstract：:Aim: The explosion of data based technology has accelerated pattern mining. However, it is clear that quality and bias of data impacts all machine learning and modeling. Results & methodology: A technique is presented for using the distribution of first significant digits of medicinal chemistry features: logP, logS, a...

journal_title：Future medicinal chemistry

authors： García-Sosa AT

更新日期：2019-09-01 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：AIM:The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS:Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhib...

journal_title：Future medicinal chemistry

authors： El-Bakhshawangy NM,El-Nassan HB,Kassab AE,Taher AT

更新日期：2018-06-01 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 use of 3D information has shown impact in numerous applications in drug design. However, it is often under-utilized and traditionally limited to specialists. We want to change that, and present an approach making 3D information and molecular modeling accessible and easy-to-use 'for the people'. METHODOLOGY/RES...

journal_title：Future medicinal chemistry

authors： Grebner C,Norrby M,Enström J,Nilsson I,Hogner A,Henriksson J,Westin J,Faramarzi F,Werner P,Boström J

更新日期：2016-09-01 00:00:00

abstract：AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...

journal_title：Future medicinal chemistry

authors： Morales F,Ramírez A,Morata-Tarifa C,Navarro SA,Marchal JA,Campos JM,Conejo-García A

更新日期：2017-03-01 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：: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：: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：: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：:Schistosomes, like many eukaryotic pathogens, typically display morphologically distinct stages during their life cycles. Epigenetic mechanisms underlie the pathogens' morphological transformations, and the targeting of epigenetics-driven cellular programs therefore represents an Achilles' heel of parasites. To speed ...

journal_title：Future medicinal chemistry

authors： Marek M,Oliveira G,Pierce RJ,Jung M,Sippl W,Romier C

更新日期：2015-01-01 00:00:00

abstract：:Chemokines and their receptors are integral components of the immune response, regulating lymphocyte development, homing and trafficking, and playing a key role in the pathophysiology of many diseases. Chemokine receptors have, therefore, become the target for both small-molecule, peptide and antibody therapeutics. Ch...

journal_title：Future medicinal chemistry

authors： Fricker SP,Metz M

更新日期：2014-01-01 00:00:00

abstract：:Aim: Anticancer immunochemotherapy represents an attractive paradigm to improve therapeutic responses and reduce side effects. Results & methodology: Here, we show that a naturally occurring host defense peptide, HN-1 inhibited multiple malignant cells proliferation and tumor growth in a xenografted human breast tumor...

journal_title：Future medicinal chemistry

authors： Qiao X,Yang H,Gao J,Cai S,Shi N,Wang M,Wang Y,Yu H

更新日期：2019-10-01 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：:In comparison with other virus infections, such as HIV, HBV, HCV, influenza and herpes virus, dengue virus infections have received relatively little attention from a (chemo)therapeutic viewpoint, despite their global incidence (2.5 billion people estimated to be at risk) and absence of an effective prophylactic measu...

journal_title：Future medicinal chemistry

authors： De Clercq E

更新日期：2010-04-01 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：:Aim: The orphan drug auranofin was recently found to exhibit antimicrobial properties. Materials & methods: We explored the efficacy of auranofin by evaluating the minimal inhibitory concentration against a collection of over 500 clinical isolates derived from multiple institutions, inclusive of drug resistant strains...

journal_title：Future medicinal chemistry

authors： Tharmalingam N,Ribeiro NQ,da Silva DL,Naik MT,Cruz LI,Kim W,Shen S,Dos Santos JD,Ezikovich K,D'Agata EM,Mylonakis E,Fuchs BB

更新日期：2019-06-01 00:00:00

abstract：:The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...

journal_title：Future medicinal chemistry

authors： Cottens S,Eaton M,Fuhr J,Geary S,Johnson DS,Li G,Raveglia L,Robertson GM,Westwell A

更新日期：2011-11-01 00:00:00

abstract：BACKGROUND:Due to the complex etiology of neurodegenerative diseases, there is growing interest in multitarget drugs. In this study we synthesized and evaluated a new series of compounds, with benzo[f]coumarin structure, as potential inhibitors of MAO-A, MAO-B, AChE and BuChE. RESULTS:In vitro studies show that most o...

journal_title：Future medicinal chemistry

authors： Matos MJ,Janeiro P,González Franco RM,Vilar S,Tatonetti NP,Santana L,Uriarte E,Borges F,Fontenla JA,Viña D

更新日期：2014-03-01 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：:Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positiv...

journal_title：Future medicinal chemistry

authors： Manetti D,Bellucci C,Chiaramonte N,Dei S,Teodori E,Romanelli MN

更新日期：2018-02-01 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：BACKGROUND:The understanding of biomolecular interactions ultimately depends on knowledge about the structural and dynamic details of the interacting system. Rational structure-based drug design implements computational methodology in this rationale. DISCUSSION:Together with increasing throughput of structural biology...

journal_title：Future medicinal chemistry

authors： Skjevik AA,Teigen K,Martinez A

更新日期：2009-04-01 00:00:00

abstract：:The protein kinase superfamily is one of the most important families of enzymes in molecular biology. Protein kinases typically catalyze the transfer of the γ-phosphate from ATP to a protein substrate (a highly ubiquitous cellular reaction), thereby controlling key areas of cell regulation. Deregulation of protein kin...

journal_title：Future medicinal chemistry

authors： Elphick LM,Lee SE,Anderson AA,Child ES,Bonnac L,Gouverneur V,Mann DJ

更新日期：2009-10-01 00:00:00