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Mini Reviews in Medicinal Chemistry

Federica Lanni, Andrea Carotti, Roccaldo Sardella, Antonio Macchiarulo, Lucia Pucciarini, Benedetto Natalini
In the last few decades, there has been a significant increase in the development of chiral compounds. Thus, access to enantiomerically pure compounds is currently a major focus of pharmaceutical research and, in particular, chiral HPLC separations have gained great importance for semi-preparative and industrial isolation of enantiopure compounds. Chemoinformatic procedures as well as molecular modelling and quantum chemistry techniques can be successfully applied to address chirality related problems especially when enantiomerically pure reference standards are missing...
October 18, 2016: Mini Reviews in Medicinal Chemistry
Luis E Bruno-Blanch, Luis Enrique
Despite the introduction of more than 15 third generation antiepileptic drugs to the market from 1990 to the moment, about one third of the epileptic patients still suffer from refractory of intractable epilepsy. Several hypotheses seek to explain the failure of drug treatments to control epilepsy symptoms in such patients. The most studied one proposes that drug resistance might be related with regional overactivity of efflux transporters from the ATP-Binding Cassette (ABC) superfamily at the blood-brain barrier and/or the epileptic foci in the brain...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Graziella Anselmo Joanitti, Rayane Ganassin, Mosar Rodrigues Corrêa, João Paulo Figueiró Longo, Cheng-Shi Jiang, Jinsong Gu, Sandra Milena Leal Pinto, Maria de Fátima Menezes Almeida Dos Santos, Ricardo Bentes de Azevedo, Luis Alexandre Muehlmann
Nanotechnology has provided powerful tools to improve the chemotherapy of cancer. Different nanostructures have been developed which deliver the anticancer drugs more selectively to tumor than to healthy tissues. The result has generally been the increase in efficacy and safety of classical anticancer drugs. In recent years, several studies have focused not only on the delivery of anticancer drugs to tumors, but also on delivering the drugs to specific organelles of cancer cells. Endoplasmic reticulum, Golgi apparatus, lysosomes, mitochondria, and nucleus have been the targets of different nanostructured drug delivery systems developed with the goal of circumventing drug-resistance, increasing drug efficacy, and so on...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Argelia Rosillo -de la Torre, Luisa Rocha, Hermelinda Salgado-Ceballos, Perla E García Casillas, Gabriel Luna-Bárcenas
BACKGROUND: Pharmacoresistant epilepsy is a disabling neuronal disorder with harmful consequences that impact patient quality of life. Although psychiatric comorbidities are frequently present in patients with epilepsy, they are more common in those patients with pharmacoresistant epilepsy. Despite medical advances, the current existing therapeutic strategies for pharmacoresistant seizure control are not available for all patients and/or present disadvantages. Moreover, the conventional drug therapies for psychiatric comorbidities have several adverse effects...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Juan Francisco Morales, Sebastián Scioli Montoto, Pietro Fagilino, María Esperanza Ruiz
The blood brain barrier (BBB) is a physical and biochemical barrier that restricts the entry of certain drugs to the Central Nervous System (CNS), while allowing the passage of others. The ability to predict the permeability of a given molecule through the BBB is a key aspect in CNS drug discovery and development, since neurotherapeutic agents with molecular targets in the CNS should be able to cross the BBB, whereas peripherally acting agents should not, to minimize the risk of CNS adverse effects. In this review we examine and discuss QSAR approaches and current availability of experimental data for the construction of BBB permeability predictive models, focusing on the modeling of the biorelevant parameter unbound partitioning coefficient (Kp,uu) ...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Xiaoning Li, Oleh Taratula, Olena Taratula, Canan Schumann, Tamara Minko
Targeted delivery of therapeutic and diagnostic agents to cancer sites has significant potential to improve the therapeutic outcome of treatment while minimizing severe side effects. It is widely accepted that decoration of the drug delivery systems with targeting ligands that bind specifically to the receptors on the cancer cells is a promising strategy that may substantially enhance accumulation of anticancer agents in the tumors. Due to the transformed cellular nature, cancer cells exhibit a variety of overexpressed cell surface receptors for peptides, hormones, and essential nutrients, providing a significant number of target candidates for selective drug delivery...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Fang Liu, Shutao Ma
Infections caused by pathogenic bacteria are a major health concern throughout the world. Unfortunately, while resistance to current therapies is spreading rapidly, new antibacterial agents to treat these infections are few in number. Thus, there is a great need to develop novel antibacterial agents with new mechanisms of action. Lipopolysaccharides (LPS) are the main component of the outer membrane of Gram-negative bacteria, serving as a permeability barrier, which protects the bacteria from many antibiotics...
October 13, 2016: Mini Reviews in Medicinal Chemistry
Beata Mysliwa-Kurdziel, Katalin Solymosi
Thylakoids and chloroplasts harbor several vital metabolic processes, but are most importantly associated with photosynthesis. The undisturbed functioning of this process necessitates the ceaseless synthesis of photosynthetic pigments, including closed tetrapyrroles such as chlorophylls (Chls). Chls probably represent the most abundant natural pigment molecules which are via photosynthesis not only crucial for the autotrophic production of food sources for heterotrophic organisms but have also contributed to oxygen production essential for aerobic metabolism...
October 4, 2016: Mini Reviews in Medicinal Chemistry
Bernadett Berecz Berecz, Helga Zelenyánszki, Sára Pólya, Cecília Tamás-Nyitrai, Mária Oszvald
Vaccines produced in plants have opened up new opportunities in vaccination. Among the various categories of vaccines, the recombinant vaccine is generally regarded as the most economical and safest type because it cannot cause disease and does not require large-scale cultivation of pathogens. Due to the low cost of their cultivation, plants may represent viable alternative platforms for producing subunit vaccines. Genetic engineering of plastids is the innovation of the last three decades and has numerous benefits when compared to nuclear transformation...
October 4, 2016: Mini Reviews in Medicinal Chemistry
Katalin Solymosi, Attila Köfalvi
Cannabis is one of the earliest cultivated plants. Cannabis of industrial utility and culinary value is generally termed as hemp. Conversely, cannabis that is bred for medical, spiritual and recreational purposes is called marijuana. The female marijuana plant produces a significant quantity of bio- and psychoactive phytocannabinoids, which regained the spotlight with the discovery of the endocannabinoid system of the animals in the early 90's. Nevertheless, marijuana is surrounded by controversies, debates and misconceptions related to its taxonomic classification, forensic identification, medical potential, legalization and its long-term health consequences...
October 4, 2016: Mini Reviews in Medicinal Chemistry
Henrik Aronsson, Petter Larsson, Sandra Bains
Higher plants have been used in medicine throughout human history. While traditional medicinal uses relied on compounds produced naturally by plants, recent advances have enabled the use of plant-based factories to produce diverse agents including pharmaceuticals, antibiotics, and vaccines. The genes responsible for the production of these substances can be either transiently expressed in plants or integrated into their nuclear genome or plastid genome (plastome) by genetic transformation. This review focuses on the application of plastid transformation of higher plants to produce biopharmaceuticals for human applications that are neither antibiotics nor vaccines...
October 4, 2016: Mini Reviews in Medicinal Chemistry
Jiachun Liu, Yan-Ling Wu, Huri Piao, Xiaoyin Zhao, Wen Zhang, Yanli Wang, Minrui Liu
At present, diseases resulting from various reasons have been causing deadly fears to humans and previously incogitable losses to health. Meanwhile, the patient compliance has been weakening because of drug resistance and serious drug adverse effects. There is therefore an urgent need for the development of novel structural agents. Rhodanine derivatives have represented wide biological activities, as well as significant industrial applications, which suggests that rhodanine heterocycle represents a key structural motif in heterocyclic chemistry and occupies a prominent position in drug discovery...
September 28, 2016: Mini Reviews in Medicinal Chemistry
Xiaoli Zhang, Jiyong Wu, Yepeng Luan
Tip60, the founding member of MYST histone acetyltransferase family, was originally identified as a cellular acetyltransferase protein that interacts with HIV-1 Tat. Tip60 plays roles in many processes such as cellular signaling transmission, DNA damage repair, cell cycle and checkpoint control and apoptosis by acetylating its histone or non-histone substrates. Dysfunction of Tip60 could promote or suppress diseases including different kinds of cancers. Here, some main functions and its known inhibitors were summarized...
September 23, 2016: Mini Reviews in Medicinal Chemistry
Supaluk Prachayasittikul, Virapong Prachayasittikul, Ratchanok Pingaew, Apilak Worachartcheewan, Nujarin Sinthupoom, Veda Prachayasittikul, Somsak Ruchirawat
Cancer has been considered to be a global health concern due to the impact of disease on quality of life. The continual increase of cancer cases as well as the resistance of cancer cells to the existing drugs have driven the search for novel anticancer drugs with better potency and selectivity, improved pharmacokinetic profiles, and minimum toxicities. Pyridine and pyrimidine are presented in natural products and genetic materials. These pyridine/pyrimidine core structures have been noted for their roles in many biological processes as well as in cancer pathogenesis, which make such compounds become attractive scaffolds for discovery of novel drugs...
September 23, 2016: Mini Reviews in Medicinal Chemistry
Jia-Zhuo Lai, Meng-Han Zhang, Yang-Chang Wu, Da-Yong Zhang, Xiao-Ming Wu, Wei-Yi Hua
Extracted from Euphorbia, ent-Abietane lactones can be classified into several categories, such as Jolkinolides and Helioscopinolides, according to their structural features. Their bio-activities include anti-tumor activity, anti-inflammatory activity as well as anti-bacterial activity. Jolkinolides draw the most attentions for their activities of inducing apoptosis in cancer cells as well as their anti-inflammatory activities. In this review, we give a brief clarification of ent-Abietane lactones, as well as their bioactivities and synthesis...
September 23, 2016: Mini Reviews in Medicinal Chemistry
Leticia Riverón-Negrete, Cristina Fernandez-Mejia
In recent decades, it has been found that vitamins affect biological functions in ways other than their long-known functions. Vitamins A and niacin are the best known. Biotin is a water-soluble vitamin that serves as a covalently-bound coenzyme of carboxylases. It is now well documented that biotin participates in processes other than classical enzyme catalysis reactions. Several lines of evidence have shown that pharmacological concentrations of biotin have a wide repertoire of effects on systemic processes such as glucose and lipid metabolism, hypertension, reproduction, development, and immunity...
September 23, 2016: Mini Reviews in Medicinal Chemistry
Thaisa Marinho Dezani, André Bersani Dezani, Mônica Maria Coquemala Silva, Cristina Helena Dos Reis Serra
In 1995, the Biopharmaceutical Classification System (BCS) was proposed by Amidon and colleagues as a tool that considers two important parameters regarding to drugs: solubility and permeability. Since then, several methods for solubility and permeability studies have been developed for drug delivery and absorption prediction. In recent years, permeability has gained a great highlight and the interaction between a molecule and a biological membrane is not enough to predict the in vivo behavior of a compound...
September 21, 2016: Mini Reviews in Medicinal Chemistry
Eleni Vrontaki, Georgia Melagraki, Antreas Afantitis, Thomas Mavromoustakos, George Kollias
The Janus kinases (JAKs) play a pivotal role in cytokine receptor signaling pathways via activation of downstream signal transducers and activators of transcription (STAT) pathway. Intracellular pathways that include JAKs are critical to immune cell activation and pro-inflammatory cytokine production. Selective inhibitors of JAKs are potentially disease-modifying anti-inflammatory drugs for the treatment of rheumatoid arthritis (RA). Each of the four members of the JAK family plays an individual role in the oncogenesis of the immune system, and therefore, the development of potent and specific inhibitors for each member is needed...
September 19, 2016: Mini Reviews in Medicinal Chemistry
Fei Hong, Liju Wang, Sharon L Wu, Hong Chai Tang, Maria Sm Wai, David Tai Wai Yew
This review looks into the herbs gingko biloba, polygala tenuifolia, and lycii fructus for their widely studied neuroprotective properties. Effects of the interaction between the herbs are studied by behavior tests to evaluate memory, and examination of signal transduction enzyme, major neurotransmitters, cell death and antioxidation. For 6-month treated mice, behavior showed shorter escape latency in the water maze and faster arrival time in a consolidated memory task. Immunochemistry showed evident increase in superoxide dismutase (SOD) activities in the prefrontal cortex, which implies protection against harmful free radicals during aging...
September 19, 2016: Mini Reviews in Medicinal Chemistry
Jin Tian, Daowan Lai, Ligang Zhou
Acremonium fungi have been isolated from various sources, such as soil, plants, and marine organisms. The species in Acremonium have been proved to be rich sources of novel and bioactive secondary metabolites. Up to now, 317 metabolites belonging to steroids, terpenoids, meroterpenoids, polyketides, alkaloids, peptides, and miscellaneous have been isolated from Acremonium fungi. These metabolites displayed a wide range of biological activities including antimicrobial, cytotoxic, insecticidal, phytotoxic, antitumor, immunosuppressive, sphingomyelinase inhibitory, antioxidant, anti-inflammatory, antimalarial, and tremorgenic activities...
September 14, 2016: Mini Reviews in Medicinal Chemistry
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