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Medicinal Chemistry

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https://www.readbyqxmd.com/read/28215170/derivatives-of-6-nitrobenzimidazole-inhibit-fructose-mediated-protein-glycation-and-intracellular-reactive-oxygen-species-production
#1
Humera Jahan, Muhammad Iqbal Choudhary, Zarbad Shah, Khalid M Khan, Atta-Ur-Rahman
BACKGROUND: Benzimidazoles are important pharmacophores in drug discovery. Several of them are currently used drugs, such as flubendazole, omeprazole, and astemizole for the treatment of anthelmintic, antiulcerative, and antihistaminic diseases, respectively. OBJECTIVES: The aim of the current study was to study the antiglycation activity of nitrobenzimidazole derivatives against fructose-mediated human serum albumin (HSA) glycation. The study was also aimed to investigate effects of newly identified antiglycation inhibitors on AGEs-induced intracellular reactive oxygen species production, and associated impaired proliferation of the hepatocytes...
February 16, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28215169/bioactive-constituents-from-an-endophytic-fungus-penicillium-polonicum-nfw9-associated-with-taxus-fauna
#2
Nighat Fatima, Tawanun Sripisut, Ui Joung Youn, Safia Ahmed, Ihsan Ul-Haq, Ulyana Muñoz-Acuña, Charles J Simmons, Muneer Ahmed Qazi, Muniba Jadoon, Ghee Teng Tan, Esperanza J Carcache de Blanco, Leng Chee Chang
BACKGROUND: Endophytic fungi are being recognized as vital and untapped sources of a variety of structurally novel and unique bioactive secondary metabolites in the field of natural products drug discovery. Herein, this study reports the isolation and characterization of secondary metabolites from an endophytic fungus Penicillium polonicum (NFW9) associated with Taxus fuana. METHODS: Extracts of the endophytic fungus cultured on potato dextrose agar were purified using several chromatographic techniques...
February 16, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185540/medicinal-chemistry-approaches-of-controlling-gastrointestinal-side-effects-of-non-steroidal-anti-inflammatory-drugs-endogenous-protective-mechanisms-and-drug-design
#3
Paraskevi Tziona, Panagiotis Theodosis-Nobelos, Eleni A Rekka
BACKGROUND: Non steroidal anti-inflammatory drugs are of the oldest and most widely used medicines. However, their untoward effects, especially gastrointestinal toxicity, remain the main obstacle to their application. Because of their mechanism of action, cycloxygenase (COX) inhibition, in combination with the weekly acidic character of most of them, major protective mechanisms of the gastrointestinal system are suppressed and deregulated. OBJECTIVE: In this review, several compounds designed to retain anti-inflammatory activity, but devoid of gastrointestinal side effects, are presented...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185539/prospects-of-gene-therapy-for-pulmonary-diseases-progress-and-limitations
#4
Garyfalia Karponi, Nikolaos Zogas, Kalliopi Domvri, Paul Zarogoulidis, Georgia Trakada, Stefanos Roumeliotis, Wolfgang Hohenforst-Schmidt, Kaid Darwiche, Lutz Freitag, Konstantinos Zarogoulidis
BACKGROUND: Despite the proof of principle that gene therapy can cure various monogenic diseases, limited clinical progress has been noted for gene therapy of the respiratory system. Certain anatomic features of the lungs, along with the suboptimal gene delivery vehicles utilized up to now, have significantly delayed successful clinical practice. Thus, the need for additional improvements towards safety and efficacy of the procedure is indispensable. OBJECTIVE: The objective of this work was to review the progress and limitations of gene therapy in the treatment of lung disease with a focus on monogenic disease, chronic obstructive pulmonary disease and asthma and to present studies that provide a proof of principle that it works in different model systems and in patients...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185538/synthesis-and-biological-evaluation-of-hybrid-1-5-and-2-5-disubstituted-indoles-as-potentially-new-antitubercular-agents
#5
Ana Soares, Mónica S Estevão, M Manuel B Marques, Vasily Kovalishyn, Diogo A R S Latino, João Aires-de-Sousa, Jorge Ramos, Miguel Viveiros, Filomena Martins
BACKGROUND: Tuberculosis (TB) is the second leading cause of mortality worldwide being a highly contagious and insidious illness caused by Mycobacterium tuberculosis, Mtb. Additionally, the emergence of multidrug-resistant and extensively drug-resistant strains of Mtb, together with significant levels of co-infection with HIV and TB (HIV/TB) makes the search for new antitubercular drugs urgent and challenging. METHODS: This work was based on the hypothesis that an active compound could be obtained if substituents present in some other active compounds were attached on a core of an important structure, in this case the indole scaffold, thus generating a hybrid compound...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185537/a-concise-update-on-the-relevance-of-secretory-phospholipase-a2-group-iia-and-its-inhibitors-to-cancer
#6
Juan Chen, Long Ye, Yu Sun, Yoshikazhu Takada
Secretory phospholipase A2 group IIA (sPLA2-IIA) is an enzyme that hydrolyzes the sn-2 ester bond in glyceroacyl phospholipids present in lipoproteins and cell membranes. As many immunohistochemical studies reveal that the high expression of sPLA2-IIA in the tumorous tissue or plasma of cancer patients, though low expression in other cases, the enzyme is considered highly relevant with cancer development. Effort has been made to establish the mechanism of how sPLA2-IIA is involved in various cancers in order to understand its pathogenic role and to utilize it as a target for cancer diagnosis and therapy...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185536/a-new-anti-aging-lysophosphatidic-acid-from-arabidopsis-thaliana
#7
Yujuan Sun, Yanhui Wang, Guangfa Wang, Lan Xiang, Jianhua Qi
BACKGROUND: Aging is a risk factor of age-related diseases. With the increasing number of patients, serious consequences, and heavy economic burden, demands for drugs used to treat age-related diseases have increased. As such, anti-aging substances should be isolated to develop drugs for the prevention and treatment of age-related diseases. METHODS: In this study, a methanol extract of immature Arabidopsis thaliana seeds with coat was separated by using a K6001 yeast bioassay system...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185535/a-simple-method-to-predict-blood-brain-barrier-permeability-of-drug-like-compounds-using-classification-trees
#8
Juan A Castillo-Garit, Gerardo M Casañola-Martin, Huong Le-Thi-Thu, Hai Pham-The, Stephen J Barigye
BACKGROUND: To know the ability of a compound to penetrate the blood-brain barrier (BBB) is a challenging task; despite the numerous efforts realized to predict/measure BBB passage, they still have several drawbacks. METHODS: The prediction of the permeability through the BBB is carried out using classification trees. A large data set of 497 compounds (recently published) is selected to develop the tree model. RESULTS: The best model shows an accuracy higher than 87...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28185534/effect-of-inhibition-of-intestinal-cholesterol-absorption-on-the-prevention-of-cholesterol-gallstone-formation
#9
Piero Portincasa, David Q-H Wang
BACKGROUND: Cholesterol cholelithiasis is a multifactorial hepatobiliary disease. METHODS: Interactions between genetic and environmental factors play a critical role in biliary cholesterol homeostasis and its imbalance enhances cholelithogenesis. RESULTS: In patients developing symptoms or complications of gallstone disease, laparoscopic cholecystectomy is recommended for treatment of gallstones. In a subgroup of patients with small, radiolucent pure cholesterol gallstones, the hydrophilic bile acid, ursodeoxycholic acid (UDCA) is still considered only pharmacological therapy able to induce oral litholysis...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28124614/synthesis-of-adamantane-aminoethers-with-antitubercular-potential
#10
Angeliki-Sofia Foscolos, Ioannis Papanastasiou, Andrew Tsotinis, Nicolas Kolocouris, George B Foscolos, Anthony Vocat, Stewart T Cole
BACKGROUND: Intrigued by the fact that aminoadamantane derivatives, bearing the active 1,2-ethylenediamine moiety, are promising antitubercular agents, we report herein on the synthesis and the antitubercular evaluation of N,N'-substituded-4,4'-[adamantane-2,2-diyl]bis(phenoxyalkyl amines) 1a-g, 1,1'-{4,4'-[adamantane-1,3-diyl]bis(phenoxyalkyl)} amines 2a-f, N,N'-substituded-[4-(1-adamantane)phenoxy] alkylamines) 3a-d and 2-[4-(dimethylaminoalkoxy)phenyl]adamantan-2-ol 4a,b, Methods: A substituted diarylmethane moiety was introduced on the adamantane skeleton of the new derivatives...
January 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28124613/harmaline-and-its-derivatives-against-the-infectious-multi-drug-resistant-escherichia-coli
#11
Hina Siddiqui, Sehar Tasneem, Saba Farooq, Amtul Sami, Atta-Ur-Rahman, Muhammad Iqbal Choudhary
Background Multidrug resistance (MDR) is a major challenge in the treatment of infectious diseases. The MDR in urinary tract infection causing bacteria, such as Escherichia coli, has made treatment of UTI very difficult. Objective The aims of the current study were to synthesize a library of harmaline derivatives, and to evaluate their activity against various strains of multi-drug resistance (MDR) E. coli. Method Harmaline derivatives were synthesized by the reaction of harmaline (1) with various acid halides and anhydrides...
January 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28067167/6-benzothiazolyl-ureas-thioureas-and-guanidines-are-potent-inhibitors-of-abad-17%C3%AE-hsd10-and-potential-drugs-for-alzheimer-s-disease-treatment-design-synthesis-and-in-vitro-evaluation
#12
Ondrej Benek, Lukas Hroch, Laura Aitken, Rafael Dolezal, Patrick Guest, Marketa Benkova, Ondrej Soukup, Karel Musil, Kamil Kuca, Terry K Smith, Frank Gunn-Moore, Kamil Musilek
BACKGROUND: The mitochondrial enzyme amyloid beta-binding alcohol dehydrogenase (ABAD) also known as 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) has been connected with the pathogenesis of Alzheimer's disease (AD). ABAD/ 17β-HSD10 is a binding site for the amyloid-beta peptide (Aβ) inside the mitochondrial matrix where it exacerbates Aβ toxicity. Interaction between these two proteins triggers a series of events leading to mitochondrial dysfunction as seen in AD. METHODS: As ABAD's enzymatic activity is required for mediating Aβ toxicity, its inhibition presents a promising strategy for AD treatment...
January 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031019/naphthyridines-with-antiviral-activity-a-review
#13
Inder Pal Singh, Sanjay Kumar, Shiv Gupta
BACKGROUND: Naphthyridine scaffold is an important pharmacophore in compounds which have shown various biological activities like antiviral, antimicrobial, anticancer, anti-inflammatory and analgesic etc. This scaffold is also reported to exhibit activity against HIV, HCMV, HSV, HPV and HCV. Antiviral activity displayed by many naphthyridine analogs is in nM range. Only few review articles are available in literature which describe about various biological activities of naphthyridines, but there is no comprehensive compilation particularly for antiviral activities...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031018/titanocenes-as-anticancer-agents-recent-insights
#14
Hana Skoupilova, Roman Hrstka, Martin Bartosik
BACKGROUND: Enormous success of antitumor agent cisplatin initiated interest in other organometallic complexes. A subclass of organometallic compounds termed metallocenes, characterized by a transition metal central atom (M) bound to cyclopentadienide (Cp-/[C5H5]-) ligands with the basic formula Cp2M, has gained increasing interest as promising anticancer agents. OBJECTIVES: This review is aimed at a progress in the development of organometallic titanium-based compounds focusing primarily on the evaluation of their cytotoxic activity and mechanism of action in relation to potential utilization as anticancer drugs...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031017/nitric-oxide-signaling-and-the-cross-talk-with-prostanoids-pathways-in-vascular-system
#15
Bruno R Silva, Tiago D Paula, Michele Paulo, Lusiane M Bendhack
BACKGROUND: This review provides an overview of the cellular signaling of nitric oxide (NO) and prostanoids in vascular cells and the possible cross talk between their pathways, mainly in hypertension, since the imbalance of these two systems has been attributed to development of some cardiovascular diseases. It also deals with the modulation of vasodilation induced by NO donors. NO is a well-known second messenger involved in many cellular functions. CONCLUSION: In the vascular system, the NO produced by endothelial NO-synthase (eNOS) or released by NO donors acts in vascular smooth muscle cells, the binding of NO to Fe2+-heme of soluble guanylyl-cyclase (sGC) activates sGC and the production of cyclic guanosine-3-5-monophosphate (cGMP)...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28000551/antimicrobial-evaluation-of-5-substituted-aryl-1h-tetrazoles
#16
Liana Feinn, Joshua Dudley, Adiel Coca, Elizabeth Lewis Roberts
BACKGROUND: Tetrazole derivatives such as 1-substituted dinitrobenzyl tetrazoles and their oxa and selanyl analogs have previously been studied against drug-susceptible and multidrug-resistant mycobacteria. In addition, other tetrazole derivatives have been shown to inhibit CTX-M class A b-lactamases. OBJECTIVE: To study the antibacterial activity of 5-substituted aryl 1H-tetrazole derivatives. METHODS: The antibacterial activity of several known 5-substituted aryl 1H-tetrazole derivatives was evaluated against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa...
December 20, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27991400/isolation-of-chemical-constituents-of-centaurea-virgata-lam-and-xanthine-oxidase-inhibitory-activity-of-the-plant-extract-and-compounds
#17
Burcu S Tuzun, Zsuzsanna Hajdu, Orsolya Orban-Gyapai, Zoltan P Zomborszki, Nikoletta Jedlinszki, Peter Forgo, Bijen Kıvcak, Judit Hohmann
BACKGROUND: Centaurea virgata Lam. is a species widely used in the traditional medicine in Turkey for the treatment of diabetes, allergy and gastric ulcers. The rationale of its use in the therapy has not been studied previously, therefore the present work aimed at the chemical-pharmacological evaluation of the plant. OBJECTIVE: The xanthine oxidase (XO) inhibitory activity of the MeOH extract and its subextracts (n-hexane, CHCl3 and remaining MeOH-H2O) prepared from C...
December 19, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27978787/synthesis-and-antiproliferative-activity-of-new-pyrazolo-3-4-c-pyridines
#18
Efthymios-Spyridon Gavriil, Nikolaos Lougiakis, Nicole Pouli, Panagiotis Marakos, Alexios-Leandros Skaltsounis, Sangkil Nam, Richard Jove, David Horne, Katerina Gioti, Harris Pratsinis, Dimitris Kletsas, Roxane Tenta
BACKGROUND: Several pyrazolopyridines possess promising pharmacological activities, mainly attributed to their antagonistic nature towards the natural purines in many biological processes. Cytotoxicity and anticancer potential of this class of compounds is mainly related to induction of apoptotic cell death and inhibition of protein kinases. OBJECTIVES: This prompted us to design, synthesize and study the antiproliferative activity of a number of new 3,7-disubstituted pyrazolo[3,4-c] pyridines...
December 13, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27924728/synthesis-and-immunosuppressive-activity-of-new-mycophenolic-acid-derivatives
#19
Karina Pereira Barbieri, Lucas Dos Reis Ercolin, Thierry Louat, Marisa Campos Polesi, Chung Man Chin, Iracilda Carlos Zeppone, Jean Leandro Dos Santos
BACKGROUND: Immunosuppressive drugs are widely used to prevent and treat allograft rejection and autoimmune diseases. Mycophenolic acid (MPA) and its derivatives are currently one of the most prescribed immunosuppressive drugs; however, metabolic drawbacks and variable inter- and intrapatient responses limit its use. OBJECTIVE: In order to find out new safe and effective immunosuppressive compounds we report here the synthesis and pharmacological evaluation of hybrid MPA derivatives containing the thalidomide/phthalimide subunits...
December 7, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27917709/synthesis-of-some-steroidal-derivatives-with-side-chain-of-20-and-22-hydrazone-aromatic-heterocycles-and-their-antiproliferative-acitivity
#20
Chunfang Gan, Liang Liu, Jianguo Cui, Zhiping Liu, Haixin Shi, Qifu Lin, Haibing Sheng, Chunhui Yang, Yanmin Huang
BACKGROUND: The modification of steroidal structure is commonly used to change the biological activity of steroids in medicinal chemistry. Some steroids containing heterocycles exhibit distinct cytotoxicity against various cancer cell lines and have been gotten wide attention over the years by medicinal chemists for drug discovery. METHODS: Using pregnenolone and stigmasterol as starting materials, via different chemical reaction, two series of heterosteroids with side chain of 20- and 22-hydrazone aromatic cycles or heterocycles in their structures were synthesized and characterized by IR, NMR and HRMS...
December 5, 2016: Medicinal Chemistry
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