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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28552049/1-4-benzothiazines-a-biologically-attractive-scaffold
#1
Amit Rai, Ashok K Singh, Vinit Raj, Sudipta Saha
1,4-benzothiazine (1,4-B), a pharmacophore of anti-psychotic drug phenothiazines, is a vital class of heterocyclic compounds implicating versatile biological activities. Among offering several interesting biological activities, 1,4-benzothiazines (1,4-Bs) have a tremendous ability to regulate diverse range of cellular pathways that can be explored for selective anticancer activity. Synthetic chemists have discovered numerous routes for the syntheses of various 1,4-B analogues that show excellent activities through multiple mechanisms...
May 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28552048/artificial-virus-as-trump-card-to-resolve-exigencies-in-targeted-gene-delivery
#2
K C Ajithkumar, K Pramod
Viruses are potent pathogens that can effectively deliver the genetic material to susceptible host cells. This capability is beneficially utilized for successfully deliver the genetic material. However, the therapeutic use of viruses for gene delivery is controversial because, the potentially replicable genomes recombine or integrates with the cell DNA resulted with immunogenicity, ranging from inflammation to death. Thus, the need for potentially effective nonviral gene therapy vehicles arises and the non-viral vectors, protein only particles and virus like particles (VLP) can be engineered which contain all the required functional modules in single chain molecules...
May 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28618985/dendrimers-general-aspects-applications-and-structural-exploitations-as-prodrug-drug-delivery-vehicles-in-current-medicine
#3
Merina Mariyam, Kajal Ghosal, Anne George, Sabu Thomas, Nandakumar Kalarikkal, Mahima S Latha
Dendrimers are hyper branched macro molecules with well-defined structure and high degree of functionality on the surface. The dendrimer architecture allows control over properties such as shape, size, density, polarity, reactivity, solubility etc. This can be manipulated to design molecules with desired properties in biomedical applications. Recent advancement in correlating structure to biodegradability and invivo performance opens up new avenue for these molecules in biological applications like drug delivery and tissue engineering...
May 11, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28494732/pharmacokinetics-of-botanical-drugs-and-plant-extracts
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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