Auranofin is an effective agent against clinical isolates of Staphylococcus aureus.

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：: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：BACKGROUND:Due to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget drugs. RESULTS:Donepezil-ferulic acid hybrids (DFAHs) were prepared by the one-pot Ugi-4CR in low-to-moderate yields. DFAHs are potent antioxidant agents, showing oxygen radical absorbance capacity values...

journal_title：Future medicinal chemistry

authors： Benchekroun M,Ismaili L,Pudlo M,Luzet V,Gharbi T,Refouvelet B,Marco-Contelles J

更新日期：2015-01-01 00:00:00

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：: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：:Systematic investigation of the lipidome will reveal new opportunities for disease diagnosis and intervention. However, lipidomic research has been hampered by the lack of molecular tools to track specific lipids of interest. Accumulating reports indicate lipid recognition can be achieved with properly constructed sho...

journal_title：Future medicinal chemistry

authors： Gao J,Zheng H

更新日期：2013-05-01 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：:Carbonic anhydrases (CAs; EC 4.2.1.1) are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

journal_title：Future medicinal chemistry

authors： Supuran CT,Winum JY

更新日期：2015-01-01 00:00:00

abstract：:Aim: With the increasing emergence of drug-resistant bacteria, the need for new antimicrobial agents has become extremely urgent. This work was to develop sulfonyl thiazoles as potential antibacterial agents. Results & methodology: Novel hybrids of sulfonyl thiazoles were developed from commercial acetanilide and acet...

journal_title：Future medicinal chemistry

authors： Hu YY,Wang J,Li TJ,Yadav Bheemanaboina RR,Ansari MF,Cheng Y,Zhou CH

更新日期：2020-10-01 00:00:00

abstract：:Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...

journal_title：Future medicinal chemistry

authors： Rosini M,Simoni E,Caporaso R,Minarini A

更新日期：2016-04-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 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：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：:Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor ty...

journal_title：Future medicinal chemistry

authors： Chiba K,Adachi K

更新日期：2012-04-01 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：BACKGROUND:4'-seleno-homonucleosides were synthesized as next-generation nucleosides, and their cellular phosphorylation was studied to confirm the hypothesis that bulky selenium atom can sterically hinder the approach of cellular nucleoside kinase to the 5'-OH for phosphorylation. RESULTS:4'-seleno-homonucleosides (n...

journal_title：Future medicinal chemistry

authors： Yu J,Sahu PK,Kim G,Qu S,Choi Y,Song J,Lee SK,Noh M,Park S,Jeong LS

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:GABA derivatives are important for the development of drugs for disorders of the CNS and PNS. RESULTS:We describe a simple synthesis of N-benzyl γ-phenyl-γ-aminobutyric acids, via the reductive amination of the corresponding γ-keto acids with benzylamines using ammonia borane. CONCLUSION:This procedure pro...

journal_title：Future medicinal chemistry

authors： Ramachandran PV,Sakavuyi K,Mistry H

更新日期：2011-02-01 00:00:00

abstract：:Aim: Alzheimer's disease (AD) is known to be themajor cause of dementia among the elderly. The structural properties and binding interactions of the AD drug physostigmine (-)-phy, and its analogues (-)-hex and (-)-phe and (+)-phe, were examined, as well as their impact on the conformational changes of two different AD...

journal_title：Future medicinal chemistry

authors： Adeniyi AA,Conradie J

更新日期：2019-08-01 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：:During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...

journal_title：Future medicinal chemistry

authors： Graifer D,Malygin A,Karpova G

更新日期：2019-02-25 00:00:00

abstract：:Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

journal_title：Future medicinal chemistry

authors： Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

更新日期：2015-01-01 00:00:00

abstract：:Cyclin-dependent kinase 7 (CDK7) plays crucial roles in the regulation of cell cycle and transcription that are tightly associated with cancer development and metastasis. The recent identification of the first covalent inhibitor which possesses high specificity against CDK7 prompts intense studies on designing highly ...

journal_title：Future medicinal chemistry

authors： Wang M,Wang T,Zhang X,Wu X,Jiang S

更新日期：2020-05-01 00:00:00

abstract：:The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential applicati...

journal_title：Future medicinal chemistry

authors： Hui M,Jian Z,Peiyuan Z,Zhenwei W,Huibin Z

更新日期：2018-04-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：:PEGylation is the covalent conjugation of PEG to therapeutic molecules. Protein PEGylation is a clinically proven approach for extending the circulation half-life and reducing the immunogenicity of protein therapeutics. Most clinically used PEGylated proteins are heterogeneous mixtures of PEG positional isomers conjug...

journal_title：Future medicinal chemistry

authors： Ginn C,Khalili H,Lever R,Brocchini S

更新日期：2014-01-01 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：: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：:This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable br...

journal_title：Future medicinal chemistry

authors： Filler R,Saha R

更新日期：2009-08-01 00:00:00

abstract：:At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing a...

journal_title：Future medicinal chemistry

authors： Huang G,Huang H

更新日期：2017-10-01 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