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Current Topics in Medicinal Chemistry

Lívia Viganor, Orla Howe, Pauraic McCarron, Malachy McCann, Michael Devereux
The "antibiotic era", characterized by the overuse and misuse of antibiotics, over the last half-century has culminated in the present critical "era of resistance". The treatment of bacterial infections is challenging because of a decline in the current arsenal of useful antibiotics and the slow rate of new drug development. The discovery of a new gene (mcr-1) in 2015, which enables bacteria to be highly resistant to polymyxins (such as colistin), the last line of antibiotic defence left, heralds a new level of concern as this gene is susceptible to horizontal gene transfer, with alarming potential to be spread between different bacterial populations, suggesting that the progression from "extensive drug resistance" to "pan-drug resistance" may be inevitable...
October 3, 2016: Current Topics in Medicinal Chemistry
Valerie W C Soo, Brian W Kwan, Héctor Quezada, Israel Castillo-Juárez, Berenice Pérez-Eretza, Silvia Julieta García-Contreras, Mariano Martínez-Vázquez, Thomas K Wood, Rodolfo García-Contreras
Despite the fact that bacterial infections are one of the leading causes of death worldwide and that mortality rates are increasing at alarming rates, no new antibiotics have been produced by the pharmaceutical industry in more than a decade. The situation is so dire that the World Health Organization warned that we may enter a "post-antibiotic era" within this century; accordingly, bacteria resistant against all known antibiotics are becoming common and already producing untreatable infections. Although several novel approaches to combat bacterial infections have been proposed, they have yet to be implemented in clinical practice...
September 30, 2016: Current Topics in Medicinal Chemistry
Marcus Lívio Varella Coelho, Andreza Freitas de Souza Duarte, Maria do Carmo de Freire Bastos
One of the biggest challenges faced presently by clinicians is the emergence of multi drug--resistant pathogens that can infect humans and animals.To control the infections caused by such pathogens the development of new drugs is required. Bacteria are a rich source of ribosomally-synthesized antimicrobial peptides known as bacteriocins, which are characterized by the presence of a self-defense immunity system. Labionin-containing lantibiotics and sactibiotics are post-translationally modified bacteriocins with peculiar features...
September 30, 2016: Current Topics in Medicinal Chemistry
Patrícia de Brum Vieira, Tiana Tasca, W Evan Secor
Trichomoniasis is a sexually transmitted disease (STD) caused by infection with the protozoan parasite Trichomonas vaginalis. It is considered the most prevalent non-viral sexually transmitted disease worldwide. Recently, the infection has been associated with adverse outcomes of pregnancy and increased risks of HIV acquisition and transmission, besides the association with cervical and prostate cancers. The consequences of trichomoniasis are likely much greater than previously recognized, both at the individual and the community level...
September 30, 2016: Current Topics in Medicinal Chemistry
Muriel Primon-Barros, Alexandre José Macedo
Microbial infections affect people worldwide, causing diseases with significant impact on public health, indicating the need for research and development of new antimicrobial agents. Animal venoms represent a vast and largely unexploited source of biologically active molecules with attractive candidates for the development of novel therapeutics. Venoms consist of complex mixtures of molecules, including antimicrobial peptides (AMPs). Since the discovery of AMPs, they have been studied as promising new antimicrobial drugs...
September 30, 2016: Current Topics in Medicinal Chemistry
Elena A Chugunova, Alexander R Burilov
Hybrid drug strategy is based on the combination of two or more pharmacophores into a new chemical entity to improve the properties of the original compounds or to obtain double action of resulting molecule. Hybrid molecules, comprised of some pharmacophore and nitric oxide (NO) donor moiety, constitute one of the more promising approaches for the design of drugs. Furoxans and benzofuroxans are considered NO releasing prodrugs and are of great interest for researchers. In this review we will focus on furoxan and benzofuroxan hybrids described in literature during the last years (from 2005 to 2016)...
September 27, 2016: Current Topics in Medicinal Chemistry
V Kishore, Nagend Nagendra Sastry Yarla, Anupam Bishayee, Swathi Putta, Ramarao Malla, Nageswara Rao Reddy Neelapu, Yallappa Shiralgi, Gurumurthy Hegde, Bhadrapura Lakkappa Dhananjaya
Andrographis paniculata (A. paniculata), a medicinal plant used in the traditional Indian and Chinese medicinal systems for its various beneficial properties owing to the presence of a diterpene lactone called 'andrographolide'. Several biological activities like anti-inflammatory, antitumour, anti-hyperglycaemic, anti-fertility, antiviral, cardio protective and hepatoprotective properties are attributed to andrographolide and its analogs. The studies have shown that not only this diterpene lactone (andrographolide), and other related terpenoid analogs from A...
September 27, 2016: Current Topics in Medicinal Chemistry
Dhanya Sunil, Pooja R Kamath
Cancer is a multifactorial disease and most of its types still remain incurable, in spite of enormous efforts to explicate various tumor pathophysiology. The anti-cancer drug discovery paradigm "one-compound-one-target" has failed and subsequently shifted to two-drug cocktail and recently the "multi-target approach" in order to design and develop agents able to act simultaneously on multiple intracellular constituents and signaling pathways. Novel hybrid compounds are now designed by incorporating two covalently linked independently acting pharmacores, each efficient at combating cancer...
September 27, 2016: Current Topics in Medicinal Chemistry
Azizeh Abdolmalekia, Jahan B Ghasemi
Finding high quality beginning compounds is a critical job at the start of the lead generation stage for multi-target drug discovery (MTDD). Designing hybrid compounds as a selective multi-target chemical entity is a challenge, opportunity, and new idea to better act against specific multiple targets. One hybrid molecule is formed by two (or more) pharmacophore group's participation. So, these new compounds often exhibit two or more activities going about as multi-target drugs (mt-drugs) and may have superior safety or efficacy...
September 27, 2016: Current Topics in Medicinal Chemistry
Katarina Spilovska, Jan Korabecny, Eugenie Nepovimova, Rafael Dolezal, Eva Mezeiova, Ondrej Soukup, Kamil Kuca
Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder. Several hallmarks such as β-amyloid (Aβ) aggregation underlying amyloid plaque formation, τ-hyperphosphorylation leading to the production of neurofibrillary tangles, and decline in the number of cholinergic neurons appear to be fundamental in the pathophysiology of the disease. Other evidence points also to the involvement of oxidative stress, biometal dyshomeostasis, inflammation, and cell cycle regulatory failure. Taking into account such premises, many attractive targets for the development of anti-AD drugs have emerged...
September 27, 2016: Current Topics in Medicinal Chemistry
Krzysztof Kamiński
The multifunctional ligands approach is one of the modern strategies in drug discovery especially in relation to diseases with complex pathomechanism, such as Alzheimer's disease, cancer, or epilepsy. According to this method different molecules with given biological properties are combined in a single chemical entity to provide complex and broad activity. Thus, with the aim of obtaining more efficacious antiepileptic drugs (AEDs) that will suppress different types of human seizures, the new hybrid anticonvulsants based on the pyrrolidine-2,5-dione scaffold have been described...
September 27, 2016: Current Topics in Medicinal Chemistry
Khaled R A Abdellatif, Eman K A Abdelall, Rania B Bakr
Selective inhibition of cyclooxygenase-2 (COX-2) isozyme afforded a useful drug design concept that resulted in the development of effective anti-inflammatory drugs that are devoid of adverse side effects, in particular gastrointestinal irritation, ulcerogenicity and renal toxicity attributed to inhibition of the cytoprotective cyclooxygenase-1 (COX-1) isozyme. Unfortunately, some selective COX-2 inhibitory drugs such as rofecoxib and valdecoxib are believed to be responsible for cardiovascular complications...
September 27, 2016: Current Topics in Medicinal Chemistry
Patrycja Michalska, Izaskun Buendia, Laura Del Barrio, Rafael León
Alzheimer's disease (AD) is the most prevalent among the aging diseases known as neurodegenerative disorders. Drug design programs over the last two decades were mainly based on the cholinergic, the amyloid or the tau hypothesis. However, none of the new drugs have a real impact on the outcome of the disease. The complex nature of AD has led to new approaches for drug development programs, the multitarget drug design hypothesis. Based on this hypothesis, the generation of multitarget hybrid compounds from previously known active molecules has been one of the most widely used to obtain new candidates for the future treatment of AD...
September 27, 2016: Current Topics in Medicinal Chemistry
Haythem A Saadeh, Mohammad S Mubarak
Antimicrobial resistance to drugs is a serious threat to public health. Different strategies have been adopted to deal with antimicrobial resistance to known drugs, one such strategy is the use of drug hybrids; this is a promising strategy to address the growing problem of drug resistance. The present review covers the very recent examples of combining (hybrid) of two standard drugs in a single molecule for resistant bacteria and malaria, and to present evidence supporting that drug hybrids are the urgent and practical solution to stop or slow down the spread of drug resistance...
September 27, 2016: Current Topics in Medicinal Chemistry
Ertan Kucuksayan, Tomris Ozben
Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively. The recent new strategy for cancer treatment involves the design and synthesis of hybrid compounds as multitargeted anticancer agents. In this review, we focus on studies using hybrid compounds which were designed and synthesized from two or more different bioactive moieties conjugating them into a single hybrid drug...
September 27, 2016: Current Topics in Medicinal Chemistry
Hana Čipčić Paljetak, Linda Tomašković, Mario Matijašić, Mirjana Bukvić, Andrea Fajdetić, Donatella Verbanac, Mihaela Perića
5-LOX - 5-lipoxygenase; ACT - artemisinin-based combination therapies; ADME - absorption, distribution, metabolism and excretion; BAL - broncho alveolar lavage; CABP - community acquired bacterial pneumonia; cAMP - cyclic adenosine monophosphate; CAP - community-acquired pneumonia; CF - cystic fibrosis, BOS bronchiolitis obliterans syndrome; cGMP - cyclic guanosine monophosphate; COPD - chronic obstructive pulmonary disease; COX - cyclooxygenase; DPB - diffuse panbronchiolitis; HDACs - histone deacetylases; IBD - inflammatory bowel disease; IL-1p - interleukin 1p; IL-6 - interleukin 6; MIC - minimal inhibitory concentrations; MLSB - macrolide, lincosamide, streptogramin B; NSAIDs - non-steroidal anti-inflammatory drugs; OVA - ovalbumin; PDE4 - phosphodiesterase 4; PMA - phorbol 12-myristate 13-acetate; RA - rheumatoid arthritis; RTI - respiratory tract infections; SAHA - suberoylanilide hydroxamic acid; SAR - structure-activity-relationship; Th1 - type 1 helper T-cell; TNBS - trinitrobenzene sulfonic acid; TNF-α - tumour necrosis factor α; UN - United Nations, WHO - World Health Organisation...
September 27, 2016: Current Topics in Medicinal Chemistry
Michelle de Oliveira Pedrosa, Rayssa Marques Duarte da Cruz, Jéssika Oliveira Viana, Ricardo Olímpio de Moura, Hamilton Mitsugu Ishiki, José Maria Barbosa Filho, Margareth F F M Diniz, Marcus Tullius Scotti, Luciana Scotti, Francisco Jaime Bezerra Mendonça
Molecular Hybridization is an approach in rational drug design where new chemical entities are obtained by combining two or more pharmacophoric units from different bioactive compounds into a single molecule. Through this approach, medicinal chemists hope that the new hybrid derivative presents: better affinity and efficacy when compared to the parent drugs; a modified selectivity profile with improvement over pharmacokinetic and pharmacodynamic restrictions; dual or multiple modes of action; reduction of undesirable side effects; decreases in drug-drug interactions; reduced emergence or spread of drug resistance in microorganisms and protozoans; and lower cost...
September 27, 2016: Current Topics in Medicinal Chemistry
Alan Talevi
Hybrid drugs are multi-target chimeric chemicals combining two or more drugs or pharmacophores covalently linked in a single molecule. In the field of anti-infective agents, they have been proposed as a possible solution to drug resistance issues, presumably having a broader spectrum of activity and less probability of eliciting high level resistance linked to single gene product. Although less frequently explored, they could also be useful in the treatment of frequently occurring co-infections. Here, we overview recent advances in the field of hybrid antimicrobials...
September 27, 2016: Current Topics in Medicinal Chemistry
Eduardo Sobarzo-Sánchez
No abstract text is available yet for this article.
September 6, 2016: Current Topics in Medicinal Chemistry
Qian Xie, Bao Zhang, JianHai Yu, Qinghua Wu, Fangji Yang, Hong Cao, Wei Zhao
Dengue fever, a type of global and tropical infectious disease, and its prevention has become a challenging issue worldwide. Antibody-dependent enhancement effects and the virus pathogenic mechanism have not yet been fully elucidated, hindering the development of dengue fever prevention and suitable drug treatment. There is currently no specific prevention and therapy in clinical trials, however, in recent years, studies have focused on the pathogenesis and treatment of dengue. Research focusing on dengue virus nonstructural protein in special drugs for the prevention and control of dengue fever is a new progress leading to improved understanding regarding the prevention and control of dengue fever and suitable drugs for the treatment...
August 29, 2016: Current Topics in Medicinal Chemistry
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