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Mini Reviews in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28714399/design-synthesis-and-antibacterial-evaluation-of-compounds-based-on-new-benzoxepine-oxime-1-2-3-triazole-hybrid
#1
Naveen Kuntala, Jhonsee Rani Telu, Venkanna Banothu, Sridhar Balasubramanian, Jaya Shree Anireddy, Sarbani Pal
A library of small molecules based on the new benzoxepine-oxime-1,2,3-triazole hybrid was initially designed as potential antibacterial agents. These compounds were synthesized using a Cu-catalyzed azide-alkyne cycloaddition (CuAAC) as a key step to construct the desired 1,2,3-triazole ring. Thus the click reaction between the appropriate alkyne containing the benzoxepine-oxime framework with aryl azides afforded the target compounds in good yields. To assess their antibacterial properties all the synthesized compounds were tested against four strains of bacterial microorganisms including one Gram-positive and three Gram-negative species...
July 17, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28714398/nutlin-3-a-p53-mdm2-antagonist-for-nasopharyngeal-carcinoma-treatment
#2
Voon Yee-Lin, Wong Pooi-Fong, Alan Khoo Soo-Beng
Nasopharyngeal carcinoma (NPC) is a form of head and neck cancer of multifactorial etiologies that is highly prevalent among men in the populations of Southern China and Southeast Asia. NPC has claimed many thousands of lives worldwide; but the low awareness of NPC remains a hindrance in early diagnosis and prevention of the disease. NPC is highly responsive to radiotherapy and chemotherapy, but radiocurable NPC is still dependent on concurrent treatment of megavoltage radiotherapy with chemotherapy. Despite a significant reduction in loco-regional and distant metastases, radiotherapy alone has failed to provide a significant improvement in the overall survival rate of NPC, compared to chemotherapy...
July 17, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28714400/cholinesterase-inhibitory-activity-of-some-semi-rigid-spiro-heterocycles-pom-analyses-and-crystalline-structure-of-pharmacophore-site
#3
Taibi Ben Hadda, Oualid Talhi, Artur S M Silva, Fatma Sezer Senol, Ilkay Erdogan Orhan, Abdur Rauf, Yahia N Mabkhot, Khaldoun Bachari, Ismail Warad, Thoraya A Farghaly, Ismail I Althagafi, Mohammad S Mubarak
Cholinesterase family consists of two sister enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which hydrolyze acetylcholine. Since deficit of acetylcholine has been evidenced in the patients of Alzheimer's disease (AD), cholinesterase inhibitors are currently the most prescribed drug class for the treatment of AD. In the present study, five compounds (2-6) with spiro skeleton have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 25 mg/mL...
July 13, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28699496/up-scaling-strategies-to-improve-the-industrial-production-of-bacitracin-at-largescale
#4
Chandra Kant Sharma, Monika Sharma
Bacitracin was discovered and named after a 7 year old American girl, Margaret Tracey in 1943 as Bacillus was isolated from her wounds. Bacillus licheniformis is usually present in soil and bird feathers. This bacterium is most commonly present around back plumage and chest of birds. There are different types of bacitracin but the one most potent is Bacitracin A. Bacitracin induced proteins are localized in bacterial membrane. Production of antibiotic initially stopped, resumed by induction of bacitracin induced protein but after few mitotic divisions microbes reverted to their vulnerable state...
July 11, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28699495/dietary-phytochemicals-and-endrocrine-related-activities-an-update
#5
Antonella Smeriglio, Marcella Denaro, Domenico Trombetta
Phytochemicals are non-nutrient bioactive compounds that occur in plant and food which possess the capacity to modulate one or more metabolic processes or pathways in the body, resulting to health benefits and promotion of well-being. At this regard, the interest of the scientific community continues to grow, powered by progressive research efforts to identify properties and potential applications of bioactive substances, and coupled with public interest and consumer demand. However, the natural derivation of these compounds is not a feature of harmlessness, over that of therapeutic efficacy, to which is also added the absence of post-marketing monitoring that does not allow to evaluate the occurrence of adverse effects related to the use of their related products...
July 11, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685702/a-focus-on-pharmacological-management-of-catecholaminergic-polymorphic-ventricular-tachycardia
#6
Claudio Barbanti, Alice Maltret, Daniel Sidi
Catecholaminergic polymorphic ventricular tachycardia (CPVT) is a channelopathy characterized by adrenergic mediated ventricular arrhythmia. Untreated CPVT is a malignant syndrome with more than 50% of arrhythmic event and up to 25% of fatal or near-fatal cardiac event at 8 years follow-up. Prevention of sudden cardiac death starts with exclusion of competitive sports. Beta blockers (BB) are the cornerstone pharmacological therapy for prevention of cardiac event in CPVT patients. Dose of BB should be the highest tolerable, preferably nadolol...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685701/the-role-of-quinidine-in-the-pharmacological-therapy-of-ventricular-arrhythmias-quinidine
#7
Milica Bajcetic, Teodora Vidonja Uzelac, Aleksandra Kezic, Milica Bajcetic
BACKGROUND: Historically, quinidine was the first medicine used in the therapy of heart arrhythmias. Studies in the early 20th century identified quinidine, a diastereomer of the antimalarial quinine, as the most potent of the antiarrhythmic substances extracted from the cinchona plant. Quinidine is used by the 1920s, as an antiarrhythmic agent to maintain sinus rhythm after conversion from atrial flutter or atrial fibrillation and to prevent recurrence of ventricular tachycardia or ventricular fibrillation...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685700/substituted-benzamides-from-antiinflammatory-and-p38-kinase-inhibitors-to-antitubercular-activity-design-synthesis-and-screening
#8
Ravindra Kulkarni, Umakant Mitkari, G Achaiah, Stefan Laufer, D V R N Bikshapti, V M Chandrashekar, P B Gurav, S J Joshi, V D Chipade
A series of amides possessing phenoxy/benzyloxy/pyridinyl groups has been synthesized by benzoylation of respective amines in presence of base with moderate to encouraging yields. Upon confirmation of structure, compounds were subjected for p38 kinase inhibitory, anti-inflammatory, antimicrobial and antitubercular activities. Antiinflammatory activity was determined using carageenan induced rat paw edema model while p38 kinase inhibitory activity was studied using ELISA method and serial dilution method was employed to determine MICs...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685699/pharmacological-treatment-of-vagal-hyperactivity-a-rare-but-potentially-fatal-cause-of-sudden-cardiac-death
#9
Pier Paolo Bassareo, Daniele Cocco, Valentina Bassareo, Stefano Bandino, Giuseppe Mercuro
Vasovagal reaction, resulting in bradycardia and/or hypotension in response to a number of stimuli, is usually self limitant, but potentially life-threatening exceptions have been described. Pharmacological treatment of proven efficacy is still lacking and the administered compounds are often chosen on the basis of either case reports or outdated small studies with a short-term follow up. In refractory cases, pacemaker implantation may be considered, although no responder patients represent a severe challenge for clinicians...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685698/medical-therapy-for-long-qt-syndrome
#10
George Adamos, Nicoletta Iacovidou, Theodoros Xanthos
Long QT syndrome (LQTS) is an arrhythmogenic disorder characterized by repolarization abnormalities with a propensity to cause life threatening cardiac events. The first manifestation of the syndrome may be sudden death, therefore, early diagnosis and therapy is of great importance. LQTS can be both congenital and acquired. The latter is most commonly seen in hospitalized patients and such individuals have an easily recognizable and reversible precipitating factor (electrolyte disturbances, certain drugs etc...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685697/does-pharmacological-therapy-still-play-a-role-in-preventing-sudden-death-in-surgically-treated-tetralogy-of-fallot
#11
Gabriele Bronzetti, Maurizio Brighenti, Marco Bonvicini
Tetralogy of Fallot (TOF) is the most common cyanotic congenital heart disease, with a familial recurrence risk of 3%. Despite the performing of an optimal surgical repair, TOF patients may feature a poor medium and long-term survival rate: atrial re-entrant tachycardia will develop in more than 30% of patients and high-grade ventricular arrhythmias will be seen in about 10% of patients. These life-threatening arrhythmias and consequent sudden death continue to represent serious complications following TOF repair...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28552049/1-4-benzothiazines-a-biologically-attractive-scaffold
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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