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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28093971/preparation-methods-and-antioxidant-activities-of-polysaccharides-and-their-derivatives
#1
Gangliang Huang, Fengying Zhao, Lu Zhou, Shiqi Huang, Hui Li
In recent years, the antioxidant effects of polysaccharides have become a hot spot in the field of polysaccharide research. Herein, the action mechanisms of polysaccharide antioxidation and scavenging free radicals were analyzed. The research progresses on the preparation methods and antioxidant properties of polysaccharides and their derivatives were reviewed. Investigating the antioxidant activities of polysaccharides and their derivatives can find useful polysaccharides and their derivatives, which have great potential as natural antioxidants used in functional foods or medicines...
January 16, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28029081/drug-discovery-for-paediatric-chagas-diseases
#2
Sreekanth Thota, Carlos M Morel
Congenital T. cruzi infection occurs in 1-10% of infants of infected mothers. Treatment of Chagas disease focuses on killing the parasite in acute infection and managing signs and symptoms in later stages. Mothers who test positive should not be treated until they have given birth and have finished breast-feeding. Screening of newborns and other children of infected mothers to provide early diagnosis and treatment. There are only two drugs currently available for the treatment of paediatric chagas disease, nifurtimox and benznidazole...
December 26, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28029080/synthesis-and-study-of-analgesic-and-anti-inflammatory-activities-of-amide-derivatives-of-ibuprofen
#3
Abbas Ahmadi, Mohsen Khalili, Zahra Olama, Shirin Karami, Babak Nahri-Niknafs
Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most widely used drugs worldwide and represent a mainstay in the therapy of acute and chronic pain and inflammation. The traditional NSAIDs like ibuprofen (I) contain free carboxylic acid group which can produce gastro-intestinal (GI) damage in long-term using of them. In order to obtain the novel NSAIDs with less side effects; carboxylic acid moiety has been modified into various amide groups which is the most active area of research in this family...
December 26, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28029079/facile-and-solvent-free-domino-synthesis-of-new-quinolidinyl-2-4-thiazolidinones-antifungal-activity-and-molecular-docking
#4
Dnyaneshwar D Subhedar, Mubarak H Shaikh, Santosh G Tupe, Mukund V Deshpande, Vijay M Khedkar, Prakash C Jha, Bapurao B Shingate
We have synthesized new quinolidinyl-thiazolidinones via knoevenagel condensation-alkylation catalyzed by [Et3NH][HSO4] has been developed. The present approach offers several advantages such as higher yields, eco-friendly reaction condition and economic availability of the catalyst. The synthesized compounds were evaluated for their in vitro antifungal activity against six fungal strains. Some of the synthesized conjugates were displays good to moderate antifungal activity. Again, the molecular docking study against the fungal sterol 14α-demethylase (CYP51) showed an excellent binding affinity towards the enzyme which could rationalize the promising antifungal activity portrayed by these derivatives and provides a platform for structure based drug design...
December 26, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28019642/recent-updates-on-melanocyte-biology-and-the-use-of-promising-bioactive-compounds-for-the-treatment-of-hypopigmentary-disorders-a-review
#5
Sharique A Ali, Ishrat Naaz, Kamal Uddin Zaidi, Ayesha Sharique Ali
Skin pigmentation is a broadly appearing phenomenon in nature which plays an important task of determining the appearance and biology of all vertebrates including human beings. Skin color is a crucial attribute, determined by the synthesis of melanin pigment within melanocytes by the process of melanogenesis and is regulated by many extrinsic as well as intrinsic factors. Tyrosinase catalyzes the key step of melanogenesis, dysfunction of tyrosinase leads to reduce melanin production which results in severe clinical and aesthetical problems of hypopigmentation...
December 23, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28019641/green-synthesis-and-molecular-docking-of-thiazolyl-thiazole-derivatives-as-potential-cytotoxic-agents
#6
Sobhi M Gomha, Mohamad R Abdelaziz, Hassan M Abdel-Aziz, Shaimaa A Hassan
A series of novel thiazolederivatives were synthesized in a good yield via reaction of 2-(1-(4-methyl-2-phenylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with hydrazonoyl halides. The reaction was performed in the presence of DABCO as an organocatalystin short reaction times, easy workup, good to excellent yields. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Ten compounds were evaluated for their anti-cancer activity against the colon carcinoma cell line (HCT-116)...
December 23, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28019640/semantic-dementia-a-mini-review
#7
Blanka Klimova, Michal Novotny, Kamil Kuca
BACKGROUND: At present there are about 47.5 million people suffering from different types of dementia and by 2030 this number should reach 75.6 million. This obviously brings about serious social and economic burden for people suffering from any kind of dementia. OBJECTIVE: The purpose of this article is to explore only semantic dementia (SD) as one of the forms of frontotemporal dementia (FTD) and provide the latest information on its diagnosis and treatment which play a significant role in the maintenance of quality of life of both patients and their caregivers...
December 23, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28019639/novobiocin-analogs-as-potencial-anticancer-agents
#8
Angelika Długosz, Anna Janecka
The aminocoumarin antibiotic, novobiocin, is a natural product that inhibits DNA gyrase, a bacterial enzyme involved in cell division. More recently, novobiocin was found to act also on eukaryotic cells by blocking the 90 kDa heat shock protein (Hsp90). Hsp90 is a molecular chaperone, critical for folding, stabilization and activation of many proteins, in particular oncoproteins responsible for cancer progression. As opposed to the geldanamycin and radicicol, the known inhibitors of Hsp90 that bind to the N-terminal region, the binding domain of novobiocin is localized in the C-terminal part of this protein...
December 23, 2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/27903231/new-analogues-of-mycophenolic-acid
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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