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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28494732/pharmacokinetics-of-botanical-drugs-and-plant-extracts
#1
Gina Paola Domínguez Moré, Paola Andrea Cárdenas, Geison M Costa, Cláudia M O Simões, Diana Marcela Aragón
Botanical drugs contain plant extracts, which are complex mixtures of compounds. As with conventional drugs, it is necessary to validate their efficacy and safety through preclinical and clinical studies. However, pharmacokinetic studies for active constituents or characteristic markers in botanical drugs are rare. The objective of this review was to investigate the global state of the art in pharmacokinetic studies of active ingredients present in plant extracts and botanical drugs. A review of pharmacokinetics studies of chemical constituents of plant extracts and botanical drugs was performed, with a total of 135 studies published between January 2004 and February 2015 available in recognized scientific databases...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494731/microwave-assisted-grafting-of-gums-and-extraction-of-natural-materials
#2
Inderbir Singh, Priya Rani, Pradeep Kumar
Microwave assisted modification polymers has become an established technique for modifying the functionality polymers. Microwave irradiation reduces reaction time as well as the use of toxic solvents with enhanced sensitivity and yields of quality products. In this review article instrumentation and basic principles of microwave activation have been discussed. Microwave assisted grafting of natural gums, characterization of grafted polymers and their toxicological parameters have also been listed. Pharmaceutical applications viz...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494730/small-molecule-efflux-pump-inhibitors-in-mycobacterium-tuberculosis-a-rational-drug-design-perspective
#3
Erika Kapp, Sarel F Malan, Samantha L Sampson
Drug resistance in Mycobacterium tuberculosis (M. tuberculosis) complicates management of tuberculosis. Efflux pumps contribute to low level resistance and acquisition of additional high level resistance mutations through sub-therapeutic concentrations of intracellular antimycobacterials. Various efflux pump inhibitors (EPIs) have been described for M. tuberculosis but little is known regarding the mechanism of efflux inhibition. As knowledge relating to the mechanism of action and drug target is central to the rational drug design of safe and sufficiently selective EPIs, this review aims to examine recent developments in the study of EPIs in M...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494729/synthetic-methods-of-quinoline-derivatives-as-potent-anticancer-agents
#4
Vaibhav Sharma, Dinesh Kumar Mehta, Rina Das
On account of significant biological activities, quinoline derivatives have drawn more attention in the synthesis and biological activities in the search of new therapeutic agents. Several new synthetic approaches have been implemented to derive new molecules from quinoline and all the synthesized molecules showed effective anticancer activity. Some molecules are synthesised using quinolones as precursor reactant, which are another effective product of quinoline, also showed significant activity against malignant tumours...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494728/design-of-ru-arene-complexes-for-antitumor-drugs
#5
Wei Su, Yuchun Li, Peiyuan Li
Recently, a number of promising ruthenium complexes have been investigated as anticancer drugs. Ru-arene complexes with [(η6-arene)Ru(X)(Y)(Z)] type, which exhibit a great structural variety, offer much potential in drug design. In this review we provide an overview of the progress in the field of arene ruthenium chemistry. We focus our attention particularly on the molecular structures and the anticancer applications of the Ru-arene complexes. Recent developments in the chemistry of arene ruthenium complexes will provide information for the investigation of novel anticancer organometallic drugs...
May 9, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28462718/rubiscolins-highly-potent-peptides-derived-from-plant-proteins
#6
Renata Perlikowska, Anna Janecka
Rubiscolins are two naturally occurring, linear peptides, isolated from the pepsin digests of D-ribulose-1,5-bisphosphate carboxylase/oxygenase (RuBisCo) from spinach leaves. Their sequences are as follows: Tyr-Pro-Leu-Asp-Leu (YPLDL, rubiscolin-5) and Tyr-Pro-Leu-Asp-Leu-Phe (YPLDLF, rubiscolin-6, also known as rubixyl). Though their structure does not resemble typical opioid peptides, rubiscolins were found to exhibit high affinity and selectivity for the delta opioid receptor and an antinociceptive effect in mice after oral administration...
April 26, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443521/synthesis-anticancer-screening-and-molecular-docking-studies-of-new-heterocycles-with-trimethoxyphenyl-scaffold-as-combretastatin-analogues
#7
Korany A Ali, Naglaa A Abdel Hafez, Mohamed A Elsayed, Manal M Elshahawi, Salwa M El-Hallouty, Abd El-Galil E Amr
In this study, synthesis, molecular docking and anticancer screening of new series of substituted heterocycles with trimethoxy phenyl scaffold as Combretastatin analogues were described. Substituted pyridines were synthesized via reaction of (E)-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (2)with active methylene reagents. Substituted pyrimidines were prepared by the reaction of the enaminone (2) with heterocyclic amines and 6-amino thiouracil. Furthermore, a series of pyrazoles substituted with trimethoxyphenyl scaffold were prepared by reaction of the enaminone 2, with selected examples of hydrazonoyl halides...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443520/recent-advances-on-3-hydroxyflavone-derivatives-structures-and-properties
#8
Burcu Butun, Gulacti Topcu, Turan Ozturk
Flavonoids are naturally occurring phenolic compounds named as 2-phenyl-1-benzopyran-4-one and classified into several subclasses according to their basic chemical structures such as flavones, flavonols, flavanones, flavanonols, and flavanols. Among them, flavonols (3-hydroxyflavone), containing a 3-hydroxyl group in association with its 4-keto group and double bond between 2- and 3- carbon atoms, have the best electron conjugated skeleton in flavonoid family, providing several resonance structures and chelating ability, through which various pharmacological activities such as antiviral, antitumor, anti-inflammatory, anticholinesterase, cytotoxicity, and particularly high antioxidant activity are demonstrated...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443519/atranorin-an-interesting-lichen-secondary-metabolite
#9
Elżbieta Studzińska-Sroka, Agnieszka Galanty, Wiesława Bylka
Atranorin, the compound with the depside structure, is one of the most common lichen secondary metabolites, characteristic for numerous lichen families but rarely found in some mosses and higher plants. Over the years various biological properties of atranorin were examined. This review summarises the studies on atranorin, focusing on a number of biological activities in different fields. The literature describes anti-inflammatory, analgesic, as well as wound healing, antibacterial, antifungal, cytotoxic, antioxidant, antiviral, and immunomodulatory activities of the depside...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443518/limitations-of-current-therapeutic-options-possible-drug-targets-and-scope-of-natural-products-in-control-of-leishmaniasis
#10
Neeraj Tiwari, Mallikarjuna Rao Gedda, Vinod K Tiwari, Surya P Singh, Rakesh K Singh
Soon after the identification of Leishmania parasites,the pentavalent antimony compounds have been the mainstay to treat leishmanial infections, worldwide. These compounds were also considered true antileishmanial but the growing incidences of resistance have forced clinicians to use other options. However, due to unavailability of antileishmanial compounds, few drugs like pentamidine (antimicrobial), amphotericin B (antifungal) or miltefosine (antitumor) agents, which are associated with serious side effects, are currently being used...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28440190/characterization-of-a-novel-polysaccharide-iron-iii-complex-and-its-anti-anemia-and-nonspecific-immune-regulating-activities
#11
Yun Zhang, Fanyi Ma, Jinhua Zhu, Zuliang Du, Yingyong Zhao, Xiuhua Liu
Dioscorea opposita Thunb. is the famous food and traditional medicine in China and it was rich in polysaccharides. Polysaccharides of D. Opposita Thunb. possess immunoregulatory activity, free radical scavenging activity and anti-diabetic activity. A novel polysaccharide-iron(III) complex (CYPIC) was synthesized by using crude polysaccharide extracted from Dioscorea opposita Thunb. The component, structure, morphology and molecular weights of CYPIC were analysed, and the anti-anemia, acute toxicity and nonspecific immune regulating activities of CYPIC were assayed...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425868/pomegranate-as-a-possible-treatment-in-reducing-risk-of-developing-wound-healing-obesity-neurodegenerative-disorders-and-diabetes-mellitus
#12
Manaf AlMatar, Md Rashedul Islam, Othman Albari, Işıl Var, Fatih Köksal
Four distinguished although overlying stages make up the methodical procedure of wound healing, which are hemostasis, inflammation, proliferation and remodelling. Multiple sclerosis (MS) comprises a persistent inflammatory infection of the central nervous system, and is related to demyelination, neurodegeneration, as well as susceptibility to oxidative pressure. Obesity signifies a swiftly developing danger to the wellbeing of populations in a rising number of nations. Usually called diabetes mellitus (DM) by medical practitioners, diabetes details a collection of metabolic diseases within which the individual has raised blood glucose, either due to an insufficiency of insulin generation, or the lack of suitable response by the body to insulin, or both...
April 19, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425867/chemokines-and-relevant-micrornas-in-the-atherogenic-process
#13
Dimitry A Chistiakov, Alexander N Orekhov, Yuri V Bobryshev
Chemokines play a significant role in initial and advanced steps of atherogenesis. In early steps, chemokines control the adhesion of leukocytes to endothelial cells (ECs) followed by transmigration of monocytes and their deposition in the intima where they differentiate to proinflammatory macrophages. Except proinflammatory activity, chemokines are responsible for homeostasis and homing of progenitor cells. Recently, microRNAs (miRs) were found to control expression and activity of chemokines in ECs, vascular smooth muscle cells (VSMCs), and macrophages at different steps of atherogenesis...
April 19, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28425866/recent-development-of-oridonin-derivatives-with-diverse-pharmacological-activities
#14
Weiyan Cheng, Chuanhui Huang, Weifeng Ma, Xin Tian, Xiaojian Zhang
Oridonin is one of the major components isolated from Isodon rubescens, a traditional Chinese medicine, and it has been confirmed to exhibit many kinds of biological activities including anticancer, anti-inflammation, antibacterial and so on. However, the poor pharmaceutical property limits the clinical applications of oridonin. So many strategies have been explored in the purpose of improving the potencies of oridonin, and structure modification is one thus way. This review outlines the landscape of recent development of oridonin derivatives with diverse pharmacological activities, mainly focusing on the biological properties, structure-activity relationships, and mechanism of actions...
April 17, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28403794/ultrasound-assisted-synthesis-of-quinoline-derivatives-in-the-presence-of-sncl2%C3%A2-2h2o-as-a-precatalyst-in-water-evaluation-of-their-antibacterial-activities
#15
A S G Prasad, T Bhaskara Rao, D Rambabu, Mandava V Basaveswara Rao, Manojit Pal
SnCl2•2H2O has been used as a convenient precatalyst for the one-pot and rapid synthesis of 2-substituted quinolines under ultrasound irradiation in water. The reaction involved a 3-component reaction of aniline, aldehydes and ethyl 3,3-diethoxypropionate in the presence of aerial oxygen to give the desired products in good yields. Several of these compounds showed antibacterial activities when tested against gram-positive and gram-negative species. One compound i.e. 4b showed promising activities across both the species...
April 12, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28325147/berberine-derivatives-with-different-pharmacological-activities-via-structural-modifications
#16
Daipeng Xiao, Zhenbao Liu, Shanshan Zhang, Mi Zhou, Fen He, Ming Zou, Junying Peng, Xiong Xie, Yanfei Liu, Dongming Peng
Berberine, a quaternary ammonium protoberberine alkaloid with an isoquinoline scaffold isolated from medicinal herbs, exhibits a wide spectrum of pharmacological activities. Berberine has been used in traditional Chinese medicine and Ayurvedic medicine. However, it has poor bioavailability, which seriously limits its application and development. The chemical transformation of natural products is an effective method to improve pharmacological activities. Researches have been carried out on the modification of berberine to obtain better pharmacological properties...
March 21, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302042/natural-anti-cancer-agents-implications-in-gemcitabine-resistant-pancreatic-cancer-treatment
#17
Bishal Marasini, Ravi P Sahu
Pancreatic cancer is one of the most lethal malignancy accounting for the fourth leading cause of cancer-related deaths in the United States. Among several explored anti-cancer agents, Gemcitabine, a nucleoside analogue remained a front line chemotherapeutic agent for the treatment of pancreatic cancer. However, gemcitabine exerts a low response rate with limited progression free survival in cancer patients due to cellular resistance of pancreatic tumors to this therapy. Several chemotherapeutic agents have been explored in combination with gemcitabine against pancreatic cancer with overall mixed responses and survival rates...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302041/promises-of-machine-learning-approaches-in-prediction-of-absorption-of-compounds
#18
Rajnish Kumar, Anju Sharma, Mohammed Haris Siddiqui, Rajesh Kumar Tiwari
The Machine Learning (ML) is one of the fastest developing techniques in prediction and evaluation of important pharmacokinetic properties such as absorption, distribution, metabolism and excretion. The availability of large number of robust validation techniques for prediction models devoted to pharmacokinetics have significantly enhanced the trust and authenticity in ML approaches. There are series of prediction models generated and used for rapid screening of compounds on the basis of absorption in last one decade...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302040/trypanothione-reductase-a-target-for-the-development-of-anti-trypanosoma-cruzi-drugs
#19
Karina Vázquez, Margot Paulino, Cristian O Salas, Juan J Zarate-Ramos, Brenda Vera, Gildardo Rivera
Chagas disease or American trypanosomiasis is a major parasitic disease in Latin America with treatment available via two drugs: nifurtimox and benznidazole. These two treatments are ineffective in the chronic phase of the disease. Therefore, there is a need for the development of new, efficient and safe drugs for the treatment of these diseases. With this goal, one of the promising targets proposed is the trypanothione reductase (TR), a key enzyme important in the metabolism of Trypanosoma cruzi. In this review, we analyze the importance of TR as a drug target, as well as their compounds inhibitors reported in the last decade as potential therapeutic agents for Chagas disease...
March 15, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28302039/bone-degeneration-inflammation-and-secondary-complications-of-arthritis-potential-targets-and-their-natural-inhibitors
#20
Mahadevappa Hemshekhar, Ram M Thushara, Somanatahpura K NaveenKumar, Paul Manoj, Mahalingam S Sundaram, Kempaiah Kemparaju, Kesturu S Girish
Arthritis is marked with joint deterioration that affects articular cartilage and subchondral bone. Though cartilage degradation is a major damage during arthritis, the subsequent bone loss cannot be neglected. Progress in the arthritis research has identified clinical importance of bone erosion in destructive arthritis. Studies have showed the key role played by osteoclasts and receptor activator of nuclear factor kappaB ligand (RANKL) signaling in bone erosion. Cathepsins and tartrate resistant acid phosphatase (TRAP) are considered key enzymatic factors contributing to bone erosion...
March 15, 2017: Mini Reviews in Medicinal Chemistry
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