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Medicinal Chemistry

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https://www.readbyqxmd.com/read/28427245/the-impact-of-dids-induced-inhibition-of-voltage-dependent-anion-channels-vdac-on-cellular-response-of-lymphoblastoid-cells-to-ionizing-radiation
#1
Magdalena Skonieczna, Artur Cieślar-Pobuda, Yuriy Saenko, Marek Foksiński, Ryszard Oliński, Joanna Rzeszowska-Wolny, Emilia Wiechec
No abstract text is available yet for this article.
April 21, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28425870/ipreny-pseaac-identify-c-terminal-cysteine-prenylation-sites-in-proteins-by-incorporating-two-tiers-of-sequence-couplings-into-pseaac
#2
Yan Xu, Zu Wang, Chunhui Li, Kuo-Chen Chou
PURPOSE: Occurring at the cysteine residue in the C-terminal of a protein, prenylation is a special kind of post-translational modification (PTM), which may play a key role for statin in altering immune function. Therefore, knowledge of the prenylation sites in proteins is important for drug development as well as for in-depth understanding the biological process concerned. Given a query protein whose C-terminal contains some cysteine residues, which one can be of prenylation or none of them can be prenylated? METHODS: To address this problem, we have developed a new predictor, called "iPreny-PseAAC", by incorporating two tiers of sequence pair coupling effects into the general form of PseAAC (pseudo amino acid composition)...
April 19, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28359234/identification-of-novel-5-6-dimethoxyindan-1-one-derivatives-as-antiviral-agents
#3
Siddappa A Patil, Vikrant Patil, Renukadevi Patil, Kenneth Beaman, Shivaputra A Patil
BACKGROUND: Discovery of novel antiviral agents is essential because viral infection continues to threaten human life globally. Various heterocyclic small molecules have been developed as antiviral agents. The 5,6-dimethoxy indan-1-one nucleus is of considerable interest as this ring is the key constituent in a range of bioactive compounds, both naturally occurring and synthetic, and often of considerable complexity. OBJECTIVE: The main purpose of this research was to discover and develop small molecule heterocycles as broad-spectrum of antiviral agents...
March 29, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28290251/dinuclear-cyclam-complex-as-a-non-cytotoxic-anti-hyperurecemic-lead-in-vitro-to-in-vivo-studies
#4
Humaira Zafar, Najlae Hamdi, Mohammed Lachkar, Brahim El Bali, Ajmal Khan, Muhammad Iqbal Choudhary
BACKGROUND: Uric acid is the end product of purine metabolism in humans and its increased level in serum leads to hyperuricemia. Among the different regulatory factors to control the level of uric acid in humans, xanthine oxidase (XO) is a well-established pharmacological target, as it is directly involved in uric acid production. METHODS: The aim of the study was to present a systematic approach to analyze the xanthine oxidase inhibition studies from in vitro leading to in vivo...
March 8, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28290250/synthesis-and-ativiral-activity-of-5-benzylthio-4-carbamyl-1-2-3-triazoles-against-human-cytomegalovirus-cmv-and-varicella-zoster-virus-vzv
#5
Yi-Ning Wen, Zhi-Feng Zhang, Ning-Ning Liu, Graciela Andrei, Robert Snoeck, Yu-Hong Xiang, Dominique Schols, Xue Chen, Zhuo-Yong Zhang, Qing-Shan Zhang, Qin-Pei Wu
BACKGROUND: All of clinic drugs for herpesvirus infections exhibit high toxicity and suffer from significant drug-resistantance. There is a great need for the development of new, effective, and safe anti-herpesvirus agents with different mechanisms of action. METHODS: A series of novel 5-(benzylthio)-1H-1,2,3- triazole-4-carboxamides were efficiently synthesized and EC50 values against human cytomegalovirus (HCMV), varicella-zoster virus (VZV) and herpes simplex virus (HSV) were evaluated in vitro...
March 7, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28290249/in-vitro-and-in-silico-studies-of-mangiferin-from-aphloia-theiformis-on-key-enzymes-linked-to-diabetes-type-2-and-associated-complications
#6
Marie C N Picot, Gokhan Zengin, Adriano Mollica, Azzurra Stefanucci, Simone Carradori, Mohamad F Mahomoodally
BACKGROUND: Mangiferin, was identified in the crude methanol extract, ethyl acetate, and n-butanol fractions of Aphloia theiformis (Vahl.) Benn. OBJECTIVE: To study the plausible binding modes of mangiferin to key enzymes linked to diabetes type 2 (DT2), obesity, hypertension, Alzheimer's disease, and urolithiasis using molecular docking. METHOD: Crystallographic structures of α-amylase, α-glucosidase, glycogen phosphorylase (GP), pancreatic lipase, cholesterol esterase (CEase), angiotensin-I-converting enzyme (ACE), acetyl cholinesterase (AChE), and urease available on the Protein Databank database were docked to mangiferin using Gold 6...
March 7, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28266280/additive-effect-of-mcp-in-combination-with-cefotaxime-against-staphylococcus-aureus
#7
Roula M Abdel-Massih, Elias Baydoun, Salah El-Khatib, Elias Dahdouh
BACKGROUND: Pectin is a heterogeneous polysaccharide present in plants and citrus fruits. It exhibits different beneficial biological activities. Conflicting reports exist about the antimicrobial effect of pectin and its derivatives. OBJECTIVE: In this study, we investigate the antimicrobial effect of Modified Citrus Pectin (MCP) against Staphylococcus aureus, a pathogen showing increasing rates of antimicrobial resistance worldwide. METHODS: Forty-three clinical isolates of S...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28266279/synthesis-characterization-and-cholinesterase-inhibition-studies-of-new-arylidene-aminothiazolylethanone-derivatives
#8
Jamshed Iqbal, Ghulam Shabir, Fayaz A Larik, Shafi Ullah Khan, Aamer Saeed, Muhammad S Shah, Pervaiz A Channar
BACKGROUND: Alzheimer's disease is caused by the destruction or loss of cholinergic cells that produce or use ACh in the brain, thereby reducing the availability of enzyme to other cells. The major treatment strategy for AD is to decrease the level of cholinesterase in the brain. OBJECTIVE: The aim of this study was to describe the effect of novel series of thiazole derivatives i.e. arylidene aminothiazolylethanones (3a-h) as cholinesterase inhibitors (CEIs). METHODS: A novel series of thiazole derivatives i...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28266278/synthesis-and-preliminary-cytotoxicity-studies-of-1-1-4-5-dihydrooxazol-2-yl-1h-indazol-3-yl-3-phenylurea-and-3-phenylthiourea-derivatives
#9
Anita Kornicka, Franciszek Sączewski, Patrick J Bednarski, Martyna Korcz, Piotr Szumlas, Ewa Romejko, Aneta Sakowicz, Łukasz Sitek, Monika Wojciechowska
BACKGROUND: N-substituted 3-amino-1H-indazoles represent an interesting class of biologically active compounds. Among them, derivatives containing phenylurea moiety are of particular interest. Such compounds have been found to possess inhibitory activity against cancer cell growth. Additionally, various oxazoline-containing compounds have also been designed as potential anticancer agents. OBJECTIVE: The aim of this work was to obtain a new class of N-substituted 3-amino-1H-indazole derivatives with cytotoxic activity towards cancer cells...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28266277/bergenin-from-peltophorum-dubium-isolation-characterization-and-antioxidant-activities-in-non-biological-systems-and-erythrocytes
#10
Guilherme A L de Oliveira, George L da Silva Oliveira, Lucas A D Nicolau, Ana C Mafud, Larissa F Batista, Yvonne P Mascarenhas, Luan K.M. de Sousa, Jorge M David, Larissa S Pinto, Clayton Q Alves, Jand V R Medeiros
BACKGROUND: Bergenin, a compound derived from gallic acid, is a secondary metabolite of the plant Peltophorum dubium (Spreng.) Taub. OBJECTIVE: In this study, we aimed to characterize the ability of bergenin to eliminate the radicals in non-biological systems. METHODS: We evaluated bergenin is ability to protect erythrocytes from oxidative damage in a biological system. We have elucidated bergenin structure using nuclear magnetic resonance, X-ray diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#11
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28215170/derivatives-of-6-nitrobenzimidazole-inhibit-fructose-mediated-protein-glycation-and-intracellular-reactive-oxygen-species-production
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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