keyword
MENU ▼
Read by QxMD icon Read
search

Medicinal chemistry

keyword
https://www.readbyqxmd.com/read/28731336/triple-reuptake-inhibitors-as-potential-therapeutics-for-depression-and-other-disorders-design-paradigm-and-developmental-challenges
#1
Murugaiah A M Subbaiah
Although first-line antidepressants offer therapeutic benefit, about 35% of depressed patients are not adequately treated, creating a large unmet medical need. These medicines mostly enhance the synaptic levels of serotonin and/or norepinephrine. Evidence from preclinical and clinical studies implicate dopamine hypofunction in the pathophysiology of depression. Triple reuptake inhibitors (TRIs), which elevate dopamine in addition to serotonin and norepinephrine, may demonstrate greater efficacy, with the reversal of anhedonia and improved tolerability...
July 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28730956/review-on-bioorganometallic-chemistry-and-new-outcomes-in-the-synthesis-and-substitution-of-tetracarbonyl-pyrrolylimine-complexes-of-rhenium-with-organophosphorus-ligands
#2
Antoine Simonneau, Franck Le Bideau, Jean-Hugues Mirebeau, Jérôme Marrot, Gérard Jaouen
: After a short review dealing with bioorganometallic chemistry, the synthesis of tetracarbonyl (pyrrolylimine) complexes of rhenium bearing chirality on the pyrrolyl ligands was reported.The reactivity of these compounds towards the substitution of one carbonyl ligand with triphenyl phosphine, tricyclohexyl phosphine and trimethyl phosphite was studied. The rhenium becoming a stereogenic center in that transformation, the resulting tricarbonyl species were obtained as mixtures of diastereomers, with diastereomeric excesses varying from 8 to 84%, according to the reaction conditions and the relative steric hindrances of the pyrrolylimine and the organophosphorus ligands...
July 19, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28730213/magnetic-separation-its-application-in-mining-waste-purification-medicine-biochemistry-and-chemistry
#3
REVIEW
M Iranmanesh, J Hulliger
The use of strong magnetic field gradients and high magnetic fields generated by permanent magnets or superconducting coils has found applications in many fields such as mining, solid state chemistry, biochemistry and medical research. Lab scale or industrial implementations involve separation of macro- and nanoparticles, cells, proteins, and macromolecules down to small molecules and ions. Most promising are those attempts where the object to be separated is attached to a strong magnetic nanoparticle. Here, all kinds of specific affinity interactions are used to attach magnetic carrier particles to mainly objects of biological interest...
July 21, 2017: Chemical Society Reviews
https://www.readbyqxmd.com/read/28729656/endolysosomal-targeting-of-a-clinical-chlorin-photosensitiser-for-light-triggered-delivery-of-nano-sized-medicines
#4
Elnaz Yaghini, Ruggero Dondi, Kunal M Tewari, Marilena Loizidou, Ian M Eggleston, Alexander J MacRobert
A major problem with many promising nano-sized biotherapeutics including macromolecules is that owing to their size they are subject to cellular uptake via endocytosis, and become entrapped and then degraded within endolysosomes, which can significantly impair their therapeutic efficacy. Photochemical internalisation (PCI) is a technique for inducing cytosolic release of the entrapped agents that harnesses sub-lethal photodynamic therapy (PDT) using a photosensitiser that localises in endolysosomal membranes...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28728539/editorial-dna-damage-as-a-strategy-for-anticancer-chemotherapy
#5
EDITORIAL
Maria Bozko, Andrzej Bozko, Tim Scholta, Nisar P Malek, Przemyslaw Bozko
Amongst all currently used drugs in the field of cancer therapy, the most prominent group of agents which induce DNA, damage both directly or indirectly. Intuitively DNA should not be a perfect target for relatively unspecific small molecular weight drugs. However, the current understanding is that not damage per se but cellular response to DNA damage induced by antitumor agents is responsible for their specific targeted effect towards cancer cells in comparison to the normal cells. DNA damaging chemotherapeutics include compounds with diferent activities namely: directly or indirectly induce DNA strand breaks, covalently modify DNA bases, change the chromatin structure and topology by inhibiting chromatin-modifying enzymes...
2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28723415/pharmacology-of-human-trace-amine-associated-receptors-therapeutic-opportunities-and-challenges
#6
REVIEW
Mark D Berry, Raul R Gainetdinov, Marius C Hoener, Mohammed Shahid
The discovery in 2001 of a G protein-coupled receptor family, subsequently termed trace amine-associated receptors (TAAR), triggered a resurgence of interest in so-called trace amines. Initial optimism quickly faded, however, as the TAAR family presented a series of challenges preventing the use of standard medicinal chemistry and pharmacology technologies. Consequently the development of basic tools for probing TAAR and translating findings from model systems to humans has been problematic. Despite these challenges the last 5 years have seen considerable advances, in particular with respect to TAAR1, which appears to function as an endogenous rheostat, maintaining central neurotransmission within defined physiological limits, in part through receptor heterodimerization yielding biased signaling outputs...
July 16, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28722469/recent-advances-in-gossypol-derivatives-and-analogs-a-chemistry-and-biology-view
#7
Yuzhi Lu, Jun Li, Chun-E Dong, Jian Huang, Hai-Bing Zhou, Wei Wang
Gossypol as a natural occurring polyphenol has been studied in a wide range of therapeutic contexts for a long time. The chemical modifications on gossypol were limited due to the unique chemical properties of polyphenols. The design and synthesis of gossypol derivatives and the exploration of their biological activities are the interest of the synthetic chemists, medicinal chemists and pharmacologists. Thus, the progress of diverse gossypol derivatives and analogs' synthesis, biological activities, mechanism elucidation and drug discovery based on gossypol scaffold is summarized...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28722154/application-of-headspace-solid-phase-microextraction-followed-by-gas-chromatography-coupled-with-mass-spectrometry-spme-gc-ms-to-determine-esters-of-carboxylic-acids-and-other-volatile-compounds-in-d-maculatus-and-d-ater-lipids
#8
Magdalena Cerkowniak, Mieczysława I Boguś, Emilia Włóka, Piotr Stepnowski, Marek Gołębiowski
A constant problem in veterinary medicine, human healthcare, agriculture, forestry or horticulture is the large number of pests, and the lack of effective methods to combat them which cause no harm to the rest of the environment. It is recommended and desired to reduce the use of chemicals and increase the use of agents based on the knowledge acquired in the field of biology, chemistry, and agrochemicals. To learn the defense mechanisms of insects we should consider not only the site of their physiological ability to protect against external factors (cuticle), but also check the possibility of chemical protection, formed by all compounds on the surface and in the body of insects...
July 19, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28720681/the-eubivas-project-within-and-between-subject-biological-variation-data-for-serum-creatinine-using-enzymatic-and-alkaline-picrate-methods-and-implications-for-monitoring
#9
Anna Carobene, Irene Marino, Abdurrahman Coŝkun, Mustafa Serteser, Ibrahim Unsal, Elena Guerra, William A Bartlett, Sverre Sandberg, Aasne Karine Aarsand, Marit Sverresdotter Sylte, Thomas Røraas, Una Ørvim Sølvik, Pilar Fernandez-Calle, Jorge Díaz-Garzón, Francesca Tosato, Mario Plebani, Niels Jonker, Gerhard Barla, Ferruccio Ceriotti
BACKGROUND: The European Federation of Clinical Chemistry and Laboratory Medicine (EFLM) European Biological Variation Study (EuBIVAS) has been established to deliver rigorously determined biological variation (BV) indices. EuBIVAS determined BV for serum creatinine using the enzymatic and alkaline picrate measurement methods. METHOD: In total, 91 healthy individuals (38 males, 53 females; age range, 21-69 years) were bled for 10 consecutive weeks at 6 European laboratories...
July 18, 2017: Clinical Chemistry
https://www.readbyqxmd.com/read/28720470/molecular-docking-prediction-and-in-vitro-studies-elucidate-anti-cancer-activity-of-phytoestrogens
#10
Shreelekha Dutta, Prashant S Kharkar, Niteshkumar U Sahu, Aparna Khanna
AIM: The study is aimed at evaluating the chemosensitization and apoptotic effect of aglycone rich extracts of dietary phytoestrogens (derived from soybean and flaxseed) on estrogen receptor positive, MCF-7 and estrogen receptor negative, MDA-MB-231 cells. The extracts show potent activity on both the cell lines, hence, in silico studies have been carried out to find the possible reason for their activity. MAIN METHODS: MTT assay was carried to assess chemosensitization effect and activated caspase-3/7 activity was studied using flow-cytometry and western blotting...
July 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28720325/therapeutic-peptides-historical-perspectives-current-development-trends-and-future-directions
#11
Jolene L Lau, Michael K Dunn
Peptide therapeutics have played a notable role in medical practice since the advent of insulin therapy in the 1920s. Over 60 peptide drugs are approved in the United States and other major markets, and peptides continue to enter clinical development at a steady pace. Peptide drug discovery has diversified beyond its traditional focus on endogenous human peptides to include a broader range of structures identified from other natural sources or through medicinal chemistry efforts. We maintain a comprehensive dataset on peptides that have entered human clinical studies that includes over 150 peptides in active development today...
July 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28716664/advances-and-challenges-in-the-search-for-d2-and-d3-dopamine-receptor-selective-compounds
#12
REVIEW
Amy E Moritz, R Benjamin Free, David R Sibley
Compounds that target D2-like dopamine receptors (DRs) are currently used as therapeutics for several neuropsychiatric disorders including schizophrenia (antagonists) and Parkinson's disease (agonists). However, as the D2R and D3R subtypes are highly homologous, creating compounds with sufficient subtype-selectivity as well as drug-like properties for therapeutic use has proved challenging. This review summarizes the progress that has been made in developing D2R- or D3R-selective antagonists and agonists, and also describes the experimental conditions that need to be considered when determining the selectivity of a given compound, as apparent selectivity can vary widely depending on assay conditions...
July 14, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28715203/a-bioinorganic-approach-to-fragment-based-drug-discovery-targeting-metalloenzymes
#13
Seth M Cohen
Metal-dependent enzymes (i.e., metalloenzymes) make up a large fraction of all enzymes and are critically important in a wide range of biological processes, including DNA modification, protein homeostasis, antibiotic resistance, and many others. Consequently, metalloenzymes represent a vast and largely untapped space for drug development. The discovery of effective therapeutics that target metalloenzymes lies squarely at the interface of bioinorganic and medicinal chemistry and requires expertise, methods, and strategies from both fields to mount an effective campaign...
July 17, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28715190/chemical-topic-modeling-exploring-molecular-datasets-using-a-common-text-mining-approach
#14
Nadine Schneider, Nikolas Fechner, Gregory A Landrum, Nikolaus Stiefl
Big data is one of the key transformative factors which are increasingly influencing all aspects of modern life. Although this transformation brings vast opportunities it also generates novel challenges, not the least of which is organizing and searching this data deluge. The field of medicinal chemistry is not different: more and more data are being generated, for instance by technologies such as DNA encoded libraries, peptide libraries, text mining of large literature corpora, and new in silico enumeration methods...
July 17, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28715083/macroevolution-a-new-method-for-the-rapid-generation-of-novel-scaffold-diverse-macrocyclic-libraries
#15
Kunz Oliver, Jörn Saupe, Haustedt Ole Lars, Sven Jakupovic, Christian Mang
Macrocycles are a structural class bearing great promise for future challenges in medicinal chemistry. Nevertheless there are few flexible approaches for the rapid generation of structurally diverse macrocyclic compound collections. We have developed an efficient method for the generation of novel macrocyclic peptide-based scaffolds. The process, called MacroEvoLution is based on a cyclization screening approach which gives reliable access to novel macrocyclic architectures. Classification of building blocks into specific pools ensures that scaffolds with orthogonally addressable functionalities are generated which can easily be used for the generation of structurally diverse compound libraries...
July 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28714500/exploring-the-immunomodulatory-and-anticancer-properties-of-zerumbone
#16
REVIEW
Md Areeful Haque, Ibrahim Jantan, Laiba Arshad, Syed Nasir Abbas Bukhari
Plant-derived immunomodulators and anti-cancer agents have attracted a lot of interest from natural product scientists for their efficacy and safety and their significant contribution towards understanding targeted drug action and drug delivery mechanisms. Zerumbone, the main constituent of Zingiber zerumbet rhizomes, has been investigated for its wide-spectrum role in treating multitargeted diseases. The rhizomes have been used as food flavoring agents in various cuisines and in herbal medicine. Many in vivo and in vitro studies have provided evidence of zerumbone as a potent immunomodulator as well as a potential anti-cancer agent...
July 17, 2017: Food & Function
https://www.readbyqxmd.com/read/28712298/the-fragment-network-a-chemistry-recommendation-engine-built-using-a-graph-database
#17
Richard J Hall, Christopher W Murray, Marcel L Verdonk
The hit validation stage of a fragment-based drug discovery campaign involves probing the SAR around one or more fragment hits. This often requires a search for similar compounds in a corporate collection or from commercial suppliers. The Fragment Network is a graph database that allows a user to efficiently search chemical space around a compound of interest. The result set is chemically intuitive, naturally grouped by substitution pattern and meaningfully sorted according to the number of observations of each transformation in medicinal chemistry databases...
July 15, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28711702/development-of-a-series-of-novel-4-anlinoquinazoline-derivatives-possessing-quinazoline-skeleton-design-synthesis-egfr-kinase-inhibitory-efficacy-and-evaluation-of-anticancer-activities-in%C3%A2-vitro
#18
Jin Chang, Hongyu Ren, Mingxia Zhao, Yan Chong, Wenwen Zhao, Yong He, Yunling Zhao, Huabei Zhang, Chuanmin Qi
4-anilinoquinazoline-based derivatives represent an attractive scaffold for small molecular EGFR-TKIs in the field of medicinal chemistry. A series of novel heterocyclic substituted derivatives have been designed, synthesized and evaluated their antitumor bioactivities as potential EGFR-TKIs. Most of the new compounds exhibited certain efficient inhibition potency for proliferation of a panel of five human cancer cells with IC50 values at the low micromolar level, and some of them possessed good broad-spectrum inhibition activities, compared to Gefitinib...
July 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28708383/unlocking-reactivity-of-trpb-a-general-biocatalytic-platform-for-synthesis-of-tryptophan-analogs
#19
David K Romney, Javier Murciano-Calles, Jöri Elias Wehrmüller, Frances H Arnold
Derivatives of the amino acid tryptophan (Trp) serve as precursors for the chemical and biological synthesis of complex molecules with a wide range of biological properties. Trp analogs are also valuable as building blocks for medicinal chemistry and as tools for chemical biology. While the enantioselective synthesis of Trp analogs is often lengthy and requires the use of protecting groups, enzymes have the potential to synthesize such products in fewer steps and with the pristine chemo- and stereoselectivity that is a hallmark of biocatalysis...
July 14, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28707591/new-generation-non-ssri-antidepressants-therapeutic-drug-monitoring-and-pharmacological
#20
Roberto Mandrioli, Michele Protti, Laura Mercolini
BACKGROUND: New-generation antidepressants (NGAs) are the latest additions to the clinician's arsenal in the fight against depression. After the introduction of selective serotonin reuptake inhibitors (SSRIs), a plethora of other groups followed, identified by their main mechanisms of activity: serotonin and norepinephrine reuptake inhibitors (SNRI); serotonin modulators and stimulators (SMS); serotonin antagonists and reuptake inhibitors (SARI); noradrenergic and selective serotonergic antidepressants (NaSSA); norepinephrine reuptake inhibitors (NeRI); serotonin, norepinephrine and dopamine reuptake inhibitors (SNDRI) or triple reuptake inhibitors (TRI); and melatonin and serotonin agonists (MaSA)...
July 12, 2017: Current Medicinal Chemistry
keyword
keyword
20947
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"