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Current Topics in Medicinal Chemistry

Soraya M Z M D Ferreira, Hellem C Carneiro, Rosemeire B Alves, Ana Carolina S Batista, Eufranio N da Silva, Gleiston G Dias, Jarbas M Resende, Daniel A Santos, Debora L Oliveira, Marcio L Rodrigues, Rossimiriam P Freitas
The conjugation of the synthetic antimicrobial peptide fragment UBI 31-38 to a coumarin derivative showed to be an effective approach for the design of a novel anticryptococcal agent. In addition to antifungal activity, the conjugate exhibited intense fluorescence, which could be valuable to a better understanding of its mechanism of action. In this work, we studied the photophysical properties of the conjugate and used confocal scanning laser microscopy to investigate its distribution in Cryptococcus cell...
February 20, 2018: Current Topics in Medicinal Chemistry
Luana S M Forezi, Luana P Borba-Santos, Mariana F C Cardoso, Vitor F Ferreira, Sonia Rozental, Fernando De Carvalho Da Silva
Sporotrichosis is a serious public health problem in Brazil that affects human patients and domestic animals, mainly cats. Thus, the search for new antifungal agents is required also due to the emergence and to the lack of effective drugs available in the therapeutic arsenal. The aim of this study was to evaluate the in vitro antifungal profile of two synthetic series of coumarin derivatives against Sporothrix schenckii and Sporothrix brasiliensis. The three-components synthetic routes used for the preparation of coumarin derivatives have proved to be quite efficient and compounds 16 and 17 have been prepared in good yields...
February 20, 2018: Current Topics in Medicinal Chemistry
Qingcheng Ren, Chuan Gao, Zhi Xu, Yan Xu, Ming-Liang Liu, Xiang Wu, Jian-Guo Guan, Lianshun Feng
Bis-coumarins have caused great interests in recent years. These compounds exhibit diverse biological activities which are ascribed to their ability to exert noncovalent interactions with the various active sites in organisms. Some of them such as dicoumarolum and dicoumarol were approved for therapeutic purposes in clinical practice. Encouraged by the above facts, numerous bis-coumarin derivatives have been synthesized and screened for their biological activities, and many of them showed promising potency...
February 20, 2018: Current Topics in Medicinal Chemistry
Renu Chaudhary, Meenakshi Balhara, Deepak Jangir, Mrridula Dangi, Mehak Dangi, Savita Khatri, Anil K Chhillar
BACKGROUND: The impact of fungal infections on human health has increased considerably within a past few decades. Although drugs with antifungal properties are available, but they are less effective and are associated with side effects. OBJECTIVE AND METHOD: Screening of bacterial isolates from Sesamum indicum and to investigate the antifungal activity of the screened bacterial isolates against Aspergillus sp. Co-culture assay and agar overlay were used to scrutinize the anti-Aspergillus activity...
February 5, 2018: Current Topics in Medicinal Chemistry
Michelyne Haroun, Christophe Tratrat, Katerina Kositsi, Anthi Petrou, Bandar Al-Dhubiab, Mahesh Attimarad, Sree Harsha, Athina Geronikaki, Marina Sokovic, Jasna Glamoclija, Ana Ciric
Background Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. Objective The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. METHODS: The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution...
February 5, 2018: Current Topics in Medicinal Chemistry
Giuseppe Vitiello, Brigida Silvestri, Giuseppina Luciani
Microbial contamination still remains a major issue of the modern era, due to widespread drug- resistant pathogens. This has prompted researchers to come up with novel antimicrobial systems that could overcome antibiotic-resistance.In this context, nature can provide inestimable source of inspiration to design high-performance multifunctional materials with potent activity against drug- resistant pathogens. Actually, integrating the bio-inspired-approach with nanotechnology can provide cutting-edge solutions for drug-resistant infections...
February 5, 2018: Current Topics in Medicinal Chemistry
Daniela Santos Pontes, Rodrigo Santos Aquino de Araujo, Natalina Dantas, Luciana Scotti, Marcus Tullius Scotti, Ricardo Olimpio de Moura, Francisco Jaime Bezerra Mendonca-Junior
The ever increasing number of multidrug-resistant microorganism pathogens has become a great and global public health threat. Antibiotic mechanisms of action and the opposing mechanisms of resistance are intimately associated, but comprehension of the biochemical and molecular functions of such drugs is not a simple exercise. Both the environment, and genetic settings contribute to alterations in phenotypic resistance (natural bacterial evolution), and make it difficult to control the emergence and impacts of antibiotic resistance...
February 5, 2018: Current Topics in Medicinal Chemistry
Harmeet Kaur, Balasubramanian Narasimhan
The development of new antimicrobial drugs is a very challenging task owing to the rapidly developing drug resistance among the existing drugs. The hybridization of active and novel compounds is a commonly used approach to combat this situation. The azo linkage (N=N) is successfully used to link two bioactive moieties to enhance the therapeutic effects. The hybrid derivatives linked by azo linkage have shown their activity by acting on target proteins in microorganisms, cell wall inhibitors, DHPS inhibitors, RNA Editing Ligase 1 inhibitors, the general protein secretory (Sec) pathway inhibitors, neuraminidase inhibitors, etc...
February 5, 2018: Current Topics in Medicinal Chemistry
Dany Siverio-Mota, Isabel Andujar, Yovani Marrero-Ponce, Rosa M Giner, Claudia Diaz Mendoza, Ganiveth Manjarrez Paba, Liliana Vicet-Muro, Maria Lorena Cordero-Maldonado, Peter A M de Witte, Alexander D Crawford, Maite Sylla-Iyarreta Veitia, Facundo Perez-Jimenez, Vicente J Aran
After the identification of the anti-inflammatory properties of the VA5-13l (2-benzyl-1-methyl-5-nitroindazolinone) in previous investigations, some analogous compounds of them were designed, synthesized and evaluated in two anti-inflammatory methods: LPS-enhanced leukocyte migration assay in zebrafish and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. Of the products evaluates (3, 6, 8, 9 and 10) showed the lower values of relative leukocyte migration at 30 µM (0.14, 0.07, 0.10, 0.13 and 0...
January 19, 2018: Current Topics in Medicinal Chemistry
M Walles, A Connor, D Hainzl
Non-cleavable linkers are used in a number of different modalities for various reasons, such as linking an active drug moiety to half-life extending molecules, to groups that enable a specific tissue or cell targeting or to facilitate active uptake into target cells. Non-cleavable linkers do not have a designated weak point in their structure that can lead to cleavage by proteases, hydrolases or chemically by pH changes. Consequently, when designing a conjugate, the choice of a non-cleavable over a cleavable linker is usually a consequence of pursuing a certain mode of action where the stability of the complex is more important than a fast liberation of the active moiety...
January 18, 2018: Current Topics in Medicinal Chemistry
L Nathan Tumey, Sean Amgen Com Han
The recent approval of trastuzumab emtansine (Kadcyla®) and brentuximab vedotin (Adcetris®) has spurred tremendous investment in new approaches for the targeted delivery of pharmaceutical agents. Targeted delivery approaches, such as antibody drug conjugates (ADCs), typically rely on an endogenous or exogenous "trigger" that results in the release of the pharmacologically active agent at the intended site of action. Lysosomal and intracellular triggers include proteolytic cleavage, glycolytic cleavage, phosphatase cleavage, hydrolytic cleavage, and reductive cleavage...
January 18, 2018: Current Topics in Medicinal Chemistry
Mario E G Moral, Teruna J Siahaan
Overexpressed cell-surface receptors are hallmarks of many disease states and are often used as markers for targeting diseased cells over healthy counterparts. Cell adhesion peptides, which are often derived from interacting regions of these receptor-ligand proteins, mimic surfaces of intact proteins and, thus, have been studied as targeting agents for various payloads to certain cell targets for cancers and autoimmune diseases. Because many cytotoxic agents in the free form are often harmful to healthy cells, the use of cell adhesion peptides in targeting their delivery to diseased cells has been studied to potentially reduce required effective doses and associated harmful side-effects...
January 18, 2018: Current Topics in Medicinal Chemistry
Mark Frigerio, Andrew F Kyle
Antibody Drug Conjugates (ADCs) use the targeting ability of monoclonal antibodies to deliver potent cytototoxic payloads to their intended target. The linker encompasses a conjugating functionality suitable for attachment to the antibody, a spacer unit that typically incorporates a hydrophilic element and a trigger which releases the potent cytototoxic warhead. Understanding the conflicting requirements of ADC design, providing stability in systemic circulation but efficient payload release once the ADC reaches its intended target, is crucial to effective linker development...
January 18, 2018: Current Topics in Medicinal Chemistry
Sandipan Chakraborty
Alzheimer's disease (AD) once considered a rare disorder emerges as a major health concern in recent times. The disease pathogenesis is very complex and yet to be understood completely. However, "Amyloid Cascade" is the central event in disease pathogenesis. Several proteins of the amyloid cascade are currently being considered as potential targets for AD therapeutics discovery. Many potential compounds are in clinical trials, but till now there is no known cure for the disease. Recent years have witnessed remarkable research interest in search of novel concepts in drug designing for AD...
January 16, 2018: Current Topics in Medicinal Chemistry
Fatima Ardito, Giovanni Di Gioia, Mario Roberto Pellegrino, Lorenzo Lo Muzio
The use of nutraceuticals as protection drugs against chronic diseases gained a vast success. Many studies found that nutraceuticals may reduce the tumorigenic actions of carcinogens, inhibiting the adhesion and proliferation of tumor cells. Genistein is a natural isoflavone preventing osteoporosis, menopause problems and heart diseases. It is also known in China and Japan for its anticancer properties. The available treatment protocols for Head and neck squamous cell cancer (HNSCC) have led to poor results and new therapies are necessary...
January 16, 2018: Current Topics in Medicinal Chemistry
Nicola Sgaramella, Xiaolian Gu, Linda Boldrup, Philip J Coates, Robin Fahraeus, Luigi Califano, Gianpaolo Tartaro, Giuseppe Colella, Lena Norberg Spaak, Adrian Strom, Torben Wilms, Lorenzo Lo Muzio, Giovanni Dell'Aversana Orabona, Mario Santagata, Lotta Loljung, Riccardo Rossiello, Karin Danielsson, Klas Strindlund, Sandra Lillqvist, Karin Nylander
Squamous cell carcinoma of the head and neck, SCCHN, is a heterogeneous group of tumours not only concerning site of origin but also regarding aetiology. The 5-year survival for the whole group of SCCHN tumours has not significantly improved over the last 20-25 years. Apart from tumour spread to lymph nodes, N status, gains and losses of specific chromosomes are the only factors shown to be independent prognostic markers for these tumours. Worldwide an increasing number of people ? 40 years are seen being affected by tongue SCC, the most common tumour within the SCCHN group...
January 16, 2018: Current Topics in Medicinal Chemistry
Alejandro Romero, Jose Marco-Contelles
Tacrine was the first drug to displayed beneficial effects on cognitive impairment of Alzheimer disease (AD) patients. Unfortunately, many treated patients displayed related hepatotoxicity, and hence this drug was withdrawn. Notwithstanding, recent efforts have been directed to design small tacrine analogues targeting the underlying pathogenic mechanisms of AD. In this context, we have developed a number of pyranotacrines by changing the benzene fused ring in tacrine by a 4H-pyran. Based on this strategy, in this account we will show the tacrine analogues that we have designed, synthesized and evaluated as potential multipotent agents for AD in the last years...
January 12, 2018: Current Topics in Medicinal Chemistry
Maria J Oset-Gasque, Jose Marco-Contelles
Tacrine was the first drug approved by FDA (US) for the treatment of Alzheimer's disease suffering patients. Nowadays, this agent has been withdrawn from the clinics due to secondary effects, among them, and the most important, its hepatotoxicity. However, the research on new tacrine analogues devoid of these therapeutically undesirable effects, but benefiting of their high and well known positive cholinergic power, has produced a number of new non-hepatotoxic tacrines. In this context, in our laboratory, in the last years we have prepared a new heterocyclic tacrines by changing the benzene ring present in tacrine by appropriate heterocyclic motifs...
January 12, 2018: Current Topics in Medicinal Chemistry
Lhassane Ismaili, Maria do Carmo Carreiras
Alzheimer's disease (AD) is a multifactorial and fatal neurodegenerative disorder affecting around 35 million people worldwide, which is characterized by decline of cholinergic function, deregulation of amyloid beta (Aβ) oligomers formation and Aβ fibril deposition. Multi-target--directed ligands (MTDLs) have emerged as an original strategy for developing new therapeutic agents on AD. Multicomponent reactions (MCRs) are a useful alternative to sequential multistep syntheses, allowing scaffold diversity and a rapid and easy access to biologically relevant compounds...
January 12, 2018: Current Topics in Medicinal Chemistry
Linda L Eastham, Candace M Howard, Premalatha Balachandran, David S Pasco, Pier Paolo Claudio
Enthusiasm for the use of dietary bioactive compounds as chemopreventive agents and adjuvants for current therapies has increased laboratory research conducted on several types of cancers including Head and Neck Squamous Cell Carcinoma (HNSCC). The green chemoprevention movement is a modern approach to highlight healthy lifestyle changes that aim to decrease the incidence of HNSCC. A healthy diet can be an effective way to prevent the development of oral cancers. Discovery of the naturally occurring plant based compounds called phytochemicals has facilitated the development of new treatment strategies for patients that are at risk for, or have developed HNSCC...
January 12, 2018: Current Topics in Medicinal Chemistry
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