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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/27903231/new-analogues-of-mycophenolic-acid
#1
Agnieszka Głowacka, Michal Prejs, Grzegorz Cholewinski, Krystyna Dzierzbicka
Mycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH) [1,2]. This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection [3]. Until now clinically have been used two derivatives of MPA: mycophenolate mofetil (MMF, CellCept) and mycophenolate sodium (MPS, Myfortic). They cause, similar to MPA, although at lower degree, the side effects such as vomiting, abdominal pain, diarrhea, nausea, gastrointestinal, urogenital tract, blood or nervous system disorders...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903230/glucocorticoid-receptor-interacting-co-regulators-putative-candidates-for-future-drug-targeting-therapy
#2
Alessia Di Silvestre, Marianna Lucafò, Sara De Iudicibus, Alessandro Ventura, Stefano Martelossi, Gabriele Stocco, Giuliana Decorti
Glucocorticoids (GCs) are largely used in different inflammatory, autoimmune and proliferative diseases. To date their mechanism of action is not completely clear and more studies are necessary, in particular to explain the great interindividual variability in clinical response. In this panorama the glucocorticoid receptor (GR) has an important role: in fact it regulates the pharmacological response thanks to the capability to interact with different molecules (DNA, RNA, ncRNA and proteins) that are known to influence its activity...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903229/an-overview-of-neolignans-of-the-genus-piper-l-isolation-methods-and-biological-activities
#3
Arthur Ladeira Macedo, Thais Carvalho Costa Dos Santos, Alessandra Leda Valverde, Davyson de Lima Moreira, Thatyana Rocha Alves Vasconcelos
The genus Piper L. has the shikimic acid pathway predominantly expressed, biosynthesizing many cinnamic acid derivatives (CAD). Neolignans comprise an important class of CAD that exhibit a wide range of pharmacological properties such as antibacterial, antitumor, insecticidal, anti-inflammatory, antioxidant, smooth muscle relaxant, neuroprotective, antiprotozoal and against platelet aggregation factor. These substances have been extracted and isolated from Piper species using different technics. The present review aims to summarize extraction and isolation methods and biological activities of the different types of neolignans covering the period from 1968 to January 2016...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903228/synthesis-and-evaluation-of-the-hypoglycemic-and-hypolipidemic-activity-of-novel-sulfonamide-benzothiazole-derivatives-of-benzylidene-2-4-thiazolidnedione
#4
Abbas Ahmadi, Mohsen Khalili, Lida Sohrabi, Nazanin Delzendeh, Babak Nahri-Niknafs, Fariba Ansari
Thiazolidinediones (TZDs) and sulfonamides are important and highly consumption class of antidiabetic drugs having insulin sensitizing and stimulating properties in patients with type 2 diabetes, respectively. In this paper, some novel benzothiazole derivatives of TZD-sulfonamides were synthesized (I-IV) and evaluated for anti-hyperglycemic and anti-hyperlipidemic activities in the STZ-induced diabetic rat model. Results indicated that all new conjugated drugs showed significant hypoglycemic activities compared to the control animals that were better for I and IV than others...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903227/chemistry-of-heterocyclic-five-and-six-membered-enamino-nitriles-and-enamino-esters
#5
Moustafa Sherief Moustafa, Saleh Mohammed Al-Mousawi, Hesham R El-Seedi, Mohamed Hilmy Elnagdi
Progress in chemistry synthetic methodologies of cyclic enaminonitriles is reported. Due to this progress, it becomes possible to reactivate these molecules toward electrophiles, nucleophiles and as electron rich dienes in 2+3 dipolar additions and in 4+2 cycloadditions reactions. Synthetizing the polyfunctionalized 4H-pyrans and their fused derivatives is a fascinating field with a multitude of biological implications such as antitumor, cardiotonic, hepatoprotective, antihypertensive, antibronchitis, as well antifungal activity...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903226/protective-effects-of-caffeic-acid-and-the-alzheimer-s-brain-an-update
#6
Solomon Habtemariam
Caffeic acid (CA) and related phenylpropanoic acids are ubiquitous natural products of the shikimic acid pathway origin. Due to the presence of diorthohydroxyl aromatic (catecholic) moiety, CA is not only one of the most potent antioxidant phenyl propanoids but also display numerous other pharmacological effects ranging from antiinflammatory to anticancer effects. Recent studies also demonstrated that CA both in its free form or conjugated with other groups such as quinic acid and sugars display profound effects in the brain including protection from toxicity induced by a variety of agents and/or experimental models of Alzheimer's disease (AD)...
November 29, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27834131/recent-highlights-on-molecular-hybrids-potentially-useful-in-central-nervous-system-disorders
#7
Mariana Matias, Samuel Silvestre, Amílcar Falcão, Gilberto Alves
Molecular hybridization is a recent strategy based in the covalent fusion of two or more existing pharmacophores to create a single molecule with multiple mechanisms of action, which represents an encouraging approach in the development of new drugs with potential therapeutic application in several pathologies. This review provides a comprehensive perspective of the most relevant advances in the development of hybrid molecules acting in the central nervous system. For instance, several opioid hybrids based on endogenous opioid peptides, such as enkephalins, deltorphin and endomorphin, have been developed and γ-aminobutyric acid (GABA) agonists have also been designed for neuropathic pain control...
November 11, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27823560/redox-active-selenium-in-health-and-disease-a-conceptual-review
#8
Boguslaw Lipinski
Although it is generally accepted that selenium (Se) is important for life, it is not well known which forms of organic and/or inorganic Se compound are the most biologically active. In nature Se exists mostly in two forms, namely as selenite with fourvalent and selenate with sixvalent cations, from which all other inorganic and organic species are derived. Despite a small difference in their electronic structure, these two inorganic parent compounds differ significantly in their redox properties. Hence, only selenite can act as an oxidant, particularly in the reaction with free and/or protein-bound sulhydryl (SH) groups...
November 4, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27823559/biological-and-chemical-aspects-of-natural-biflavonoids-from-plants-a-brief-review
#9
Vanessa Silva Gontijo, Marcelo Henrique Dos Santos, Claudio Viegas
Biflavonoids belong to a subclass of the plant flavonoids family and are limited to several species in the plant kingdom. In the literature, biflavonoids are extensively reported for their pharmacological properties including anti-inflammatory, antioxidant, inhibitory activity against phospholipase A2 (PLA2) and antiprotozoal activity. These activities have been discovered from the small number of biflavonoid structures that have been investigated, although the natural biflavonoids library is likely to be large...
November 4, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27823558/natural-products-as-a-source-of-antiarrhythmic-drugs
#10
Arkadiy O Bryzgalov, Tatjana G Tolstikova, Elvira E Shults, Kristina O Petrova
Throughout all development of medicine the leading positions were taken by search of the new drugs blocked different types of arrhythmias. Over the past decade, attention has been paid to the selection of antiarrhythmic active substances from plant material. It has been shown that these compounds have good antiarrhythmic effect and their chemical modifications substantially increase their major effects while adding other pharmacological properties. In this regard work on the chemical modification of plant antiarrhythmics are actual for the creation of new and perspective drugs...
November 4, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27823557/structural-modifications-of-matrine-type-alkaloids
#11
Xiao-Hua Cai, Hui Guo, Bing Xie
Matrine-type alkaloids belong to quinolizidine analogues from Sophora flavescens Ait, Sophora subprostrata and Sophora alopecuroides L. possess numerous therapeutic properties and has caused continuous attention over the past few decades. In order to improve and amplify the activities and applicants of matrine-type alkaloids, many matrine-type dervatives have synthesed and evaluated for their biological activities in recent several years. These structural modifications have resulted in stronger activity and improvement of the pharmaco¬kinetic properties...
November 4, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804885/the-functions-of-heparanase-in-human-diseases
#12
Hao Jin, Shaobo Zhou
The study of the heparanase has long been paid wide attention. Heparanase ,an endo-β-D-glucuronidase, is capable of specifically degrading heparan sulfate(HS), one of the excellular matrix(ECM) components. It exerts its enzymatic activity catalyzing the cleavage of the β (1,4)-glycosidic bond between glucuronic acid and glucosamine residue. HS cleavage results in remodelling of the extracellular matrix as well as in regulating the release of many HS-linked molecules such as growth factors, cytokines and enzymes involved in inflammation, wound healing and tumour invasion...
November 1, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804889/process-variables-and-design-of-experiments-in-liposome-and-nanoliposome-research
#13
Alaleh Zoghi, Kianoush Khosravi-Darani
Liposomes vesicles consisting of one or more phospholipid bilayers are microcarriers used in numerous scientific disciplines. During the last decade, nanostructured liposomes, or nanoliposomes, have been utilized in biomedical investigations due to their unique characteristics including nanoscale size, sustained release, biocompatibility, and biodegradability. The extensive literature covering the field of liposomology is an indication of increasing interests and applications in many areas, especially as carriers of active substances in nanomedicine, agriculture, food technology, and cosmetics...
October 31, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804888/recent-advances-in-the-synthesis-and-anticancer-activity-of-molecules-other-than-nitrogen-containing-heterocyclic-moeities
#14
Md Jawaid Akhtar, M Shahar Yar, Ahsan Ahmed Khan, Zulphikar Ali, Md Rafi Haider
The present review article presented a detailed account of the design strategies and the structure activity relationship of different derivatives apart from nitrogen containing ring. These scaffolds play an important part in the drug discovery which showed anticancer activity against different human cancer cell lines through apoptosis, cell cycle arrest, inhibiting kinases, angiogenesis, disruption of cell migration, modulation of nuclear receptor responsiveness and others. Napthalenes amides/amidines, furan, podophyllotoxin, platinum compounds, steroids, and urea which form the core part or along with other N-heterocyclic rings are enclosed...
October 31, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804887/interaction-between-ionizing-radiation-and-phthalates-an-unrecognized-risk-for-human-health
#15
Giuseppe Latini, Lucia Dipaola, Maria Grazia Andreassi, Silvia Rocchiccioli, Marika Massaro, Eugenio Picano
Ionizing radiation has been shown to impact and possibly alter the normal structure and function of living cells and is dangerous for human health, especially when exposure occurs early in life. Additionally, radiation can interact with other dangerous substances in the same environment, such as phthalates. Phthalates are a group of multifunctional molecules used in a wide range of consumer products, as plasticizers to impart flexibility, durability and strength to otherwise rigid polyvinyl chloride. They are not chemically bound to polyvinyl chloride, and thus migrate into the environment with time and use, becoming ubiquitous environmental contaminants...
October 31, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27804886/recent-advances-of-metallocenes-for-medicinal-chemistry
#16
Miguel M Santos, Pedro Bastos, Isabelle Catela, Karolina Zalewska, Luis C Branco
The recent advances about synthesis and application of different metallocenes for Medicinal Chemistry is reviewed. The manuscript presents the different metallocene scaffolds, with special emphasis on ferrocene derivatives, and their potential pharmaceutical application. Over the last years, the synthesis of new metallocene compounds and their biological and medical effects against some types of diseases (e.g. anti-tumoral, antibiotics, anti-viral activities) have been reported. From the medicine point of view, the attractive properties of metallocene derivatives, such as their high stability, low toxicity and appealing redox behaviours, are particularly relevant...
October 31, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27781963/bioactive-natural-products-from-animal-symbionts
#17
Yuan Tian, Yan-Ling Li, Feng-Chun Zhao
Animal symbionts are miroorganisms living inside animal hosts during some parts of their life. In view of the special environment, it is considered that the unique microbes might be the producer of new compounds with diversity biological activities. This review summarizes new findings concerning the characteristics of various natural products that can be extracted from animal symbiotic microbes, highlighting that animal symbionts represent an underexplored reservoir for the discovery of natural products with unique scaffolds and promising biological activities...
October 24, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27781962/searching-for-novel-janus-kinase-2-inhibitors-using-a-combination-of-pharmacophore-modeling-3d-qsar-studies-and-virtual-screening
#18
Eleni Vrontaki, Georgia Melagraki, Antreas Afantitis, Thomas Mavromoustakos, George Kolliasc
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...
October 24, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27781961/microbe-bio-chemical-insight-reviewing-interactions-between-dietary-polyphenols-and-gut-microbiota
#19
Rishi Mahajan, Gunjan Goel, Sampan Attri
Polyphenols are widespread constituents of different food commodities. These are regarded as essential micronutrients because of their well-documented health benefits. These health benefits depend on the amount of polyphenols consumed and their bioavailability in the gut. The microbial transformation of polyphenols in gut is poorly characterized, where, these polyphenols may act as promoting factors for proliferation of beneficial gut inhabitants and inhibiting the pathogenic species. The aim of this review is to present a holistic view on occurrence of polyphenols, their health benefits and influence of dietary polyphenols on gut microbiota...
October 24, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27781960/angiotensin-mediated-oxidative-stress-and-neuroprotective-potential-of-antioxidants-and-at1-receptor-blockers
#20
Bharat Bhusan Subudhi, Pratap Kumar Sahu
Oxidative stress in brain underlies the major neurological disorders including Alzheimer's disease (AD) and Parkinson's disease (PD). Peripherally, Angiotensin-II is a major effector of inflammation. Identification of its capacity to access brain during hypertension, as well as location of central rennin angiotensin system have led to its recognition as the major effector of oxidative stress in brain. Clinical uses of antioxidants to antagonize this oxidative stress have mostly failed. In this scenario, AT1 blockers have been investigated to prevent neurodegeneration...
October 24, 2016: Mini Reviews in Medicinal Chemistry
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