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Medicinal Chemistry

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https://read.qxmd.com/read/30760191/chemistry-alpha-glucosidase-and-radical-scavenging-properties-of-uranyl-vi-hydrazide-complexes
#1
Parveen Akhter, Uzma Ashiq, Rifat Ara Jamal, Zara Shaikh, Mohammad Mahroof-Tahir, Mehreen Lateef, Rooma Badar
BACKGROUND: Antioxidant, anti-inflammatory, antiviral and antitumoral activities among others are essential characteristics in the development of novel therapeutic compounds. Acid hydrazides can form complexation with certain metal ions that positively enhances these biological characteristics. OBJECTIVE: Five new complexes of uranium with hydrazide ligands were synthesized at room temperature. METHOD: The characterization was done by spectroscopic methods (ESI-Mass, IR, 1H-NMR, 13C-NMR), CHN analysis and conductivity measurements...
February 12, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30747078/cytotoxicity-pro-apoptotic-activity-and-in-silico-studies-of-dithiocarbamates-and-their-structure-based-design-and-sar-studies
#2
Syeda Shamila Hamdani, Bilal Ahmad Khan, Shahid Hameed, Faisal Rashid, Sumera Zaib, Khalil Ahmed, Ehsan Ullah Mughal, Jamshed Iqbal
BACKGROUND: Cancer is a far reaching and lethal but cureable disease. Reasearchers have investigated numerous anticancer agents with only few commercialy available effective drugs which are very costly. OBJECTIVE: Herein we report the synthesis , characterization and anti cancer assays of a series of novel dithiocarbamates derivatives. METHOD: All compounds were synthesized from different secondary amines and substituted benzyl chlorides in single step...
February 11, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30747076/antiglycation-activity-of-triazole-schiff-s-bases-against-fructose-mediated-glycation-in-vitro-and-in-silico-study
#3
Muniza Shaikh, Salman Siddiqui, Humaira Zafar, Uzma Naqeeb, Fakiha Subzwari, Rehan Imad, Khalid Mohammed Khan, M Iqbal Choudhary
BACKGROUND: Advanced glycation end products (AGEs) are known to be involved in pathophysiology of diabetic complications, neurodegenerative diseases, and aging. Preventing the formation of AGEs can be helpful in the management of these diseases. OBJECTIVE: Two classes of previously synthesized traizole Schiff's bases (4H-1,2,4-triazole-4-Schiff's bases 1-14, and 4H-1,2,4-triazole-3-Schiff's bases 15-23) were evaluated for their in vitro antiglyaction activity. METHODS: In vitro fructose-mediated human serum albumin (HSA) glycation assay was employed to assess the antiglycation activity of triazole Schiff's bases...
February 11, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30747077/antibacterial-evaluation-of-novel-substituted-cycloheptaindoles-in-staphylococcus-and-enterococcus-strains
#4
A Hilgeroth, K Yasrebi, S Suzen, T Hertlein, K Ohlsen, M Lalk
BACKGROUND: Due to emerging resistances against antibiotics there is a strong need to find novel antibacterial agents with a novel structure to prevent early resistance developments. OBJECTIVE: Bisindole compounds with antibacterial activities which formally result from the reaction of an aldehyde with indole motivated to investigate the reaction of a dialdehyde and indole to give novel structures with potential antibacterial activities. METHOD: Compounds were yielded by chemical synthesis and purified using column chromatography...
February 8, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30734682/the-effects-of-trifluoromethylated-derivatives-on-prostaglandin-e2-and-thromboxane-a2-production-in-human-leukemic-u937-macrophages
#5
Ivana Beara, Tatjana Majkić, Stefania Fioravanti, Laura Trulli, Neda Mimica-Dukić, Lucio Pellacani, Luciano Saso
BACKGROUND: Convenient approach to modulation of the inflammation is influence on production of inflammatory mediators - eicosanoids, generated in arachidonic acid (AA) metabolism. Common therapeutic activity of non-steroidal anti-inflammatory drugs (NSAID), such as aspirin, includes inhibition of two crucial enzymes of AA metabolism - cyclooxygenase-1 and -2 (COX-1/2), with certain risk for gastrointestinal and renal intolerance. Ever since enrolment of COX-2, particularly overabundance of its main products prostaglandin E2 (PGE2) and thromboxane A2 (TXA2) in numerous pathological processes was recognized, it became significant therapeutic target...
February 8, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30734681/structure-activity-relationship-of-4-amino-2-thiopyrimidine-derivatives-as-platelet-aggregation-inhibitors
#6
Barbara Cacciari, Pamela Crepaldi, Chun Yan Cheng, Elena Bossi, Giampiero Spalluto, Stephanie Federico, Kenneth A Jacobson, Marco Cattaneo
BACKGROUND: Platelet aggregation plays a pathogenic role in the development of arterial thrombi, which are responsible for common diseases caused by thrombotic arterial occlusion, such as myocardial infarction and stroke. Much efforts is directed toward developing platelet aggregation inhibitors that act through several mechanisms: the main antiplatelet family of COX-inhibitors, phosphodiesterase inhibitors, and thrombin inhibitors. Recently, the important role in the platelet aggregation of adenosine diphosphate (ADP)-activated P2Y12 and P2Y1 receptors, G-protein coupled receptors of the P2 purinergic family, has emerged, and their inhibitors are explored as potential therapeutic antithrombotics...
February 8, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727909/design-synthesis-and-anti-bacterial-activity-of-novel-deoxycholic-acid-amino-alcohol-conjugates
#7
Satyendra Mishra, Sejal Patel
BACKGROUND: Numerous of synthetic bile acid derivatives have been recognized for its various biological activities. Among these, bile acid amides have emerged as an attractive antibacterial agent. We herein illustrate the synthesis and antibacterial evaluation of deoxycholic acid-amino alcohols conjugates. OBJECTIVE: Design and Synthesis of novel deoxycholic acid-amino alcohol conjugates to investigate their antibacterial activity against E. coli and S. aureus Method: Novel deoxycholic acid-amino alcohol conjugates were synthesized, from conjugation of deoxycholic acid-NHS ester with amino alcohols...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727908/target-based-virtual-screening-of-new-leads-inhibitor-against-bacterial-cell-division-protein-ftsz-for-the-discovery-of-antibacterial-agents
#8
Ratish Chandra Mishra, Rosy Kumari, Shivani Yadav, Jaya Parkash Yadav
BACKGROUND: Staphylococus epidermidis coagulase negative and gram positive streptococci have emerge as major nosocomial pathogens associated with infection of implanted medical devices and dandruff in human scalp. S. epidermidis filamenting temperature-sensitive mutant Z (FtsZ) gene encoded FtsZ protein that assembles at future bacterial cell division site that form Z-ring structure. FtsZ is a tubulin homologue protein with low sequence similarity; this makes it possible to inhibit bacterial FtsZ protein without affecting the eukaryote cell division...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727907/polyethylene-glycol-acts-as-a-mechanistic-stabilizer-of-l-asparaginase-a-computational-probing
#9
R Sindhu, H Pradeep, H K Manonmani
L-asparaginase (L-ASN) is an anti-cancer enzyme therapeutic drug that exerts cytotoxicity via inhibition of protein synthesis through depletion of L-asparagine in the tumour microenvironment. The therapeutic performance of the native drug is partial due to the associated instability, reduced half-life and immunogenic complications. In this study, we report the modification of recombinant L-asparaginase with PEG and an integrated computational strategy to probe the PEGylation in the protein to understand the biological stability/activity imparted by PEG...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727906/structure-activity-relationship-study-on-therapeutically-relevant-egfr-double-mutant-inhibitors
#10
Shehnaz Fatima, Subhash Mohan Agarwal
BACKGROUND: EGFR is a clinically approved drug target in cancer. The first generation tyrosine kinase inhibitors targeting L858R mutated EGFR are routinely used to treat non-small cell lung cancer (NSCLC). However, the presence of a secondary mutation (T790M) tenders these inhibitors ineffective and thus results in the relapse of the disease. OBJECTIVE: New reversible inhibitors are required, which act against T790M/L858R (TMLR) double mutants and overcome resistance...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727905/synthesis-design-and-antiplasmodial-evaluation-of-sulfoximine-triazole-hybrids-as-potential-antimalarial-prototypes
#11
Tommy Fredrick Mabasa, Awe Babatunde, Dustin Laming, Henok Hadgu Kinfe
BACKGROUND: Malaria, caused by the deadly Plasmodium falciparum strain, claims the lives of millions of people annually. The emergence of drug-resistant strains of P. falciparum to the artemisinin-based combination therapy (ACT), the last line of defense against malaria, is worrisome and urges for the development of new chemo-types with new mode of actions. In the search of new antimalarial agents, hybrids of triazoles and other known antimalarial drugs have been reported to possess better activity than either of the parent compounds administered individually...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30727904/synthesis-antimicrobial-evaluation-and-molecular-docking-of-some-potential-2-6-disubstituted-1h-benzimidazoles-non-classical-antifolates
#12
Sunil Harer, Manish Bhatia, Vikram Kawade
BACKGROUND: Dihydrofolate reductase is one of the important enzymes for thymidylate and purine synthesis in micro-organisms. A large number of drugs have been designed to inhibit microbial DHFR but over the period of time some drugs have developed resistance and cross reactivity towards the enzyme. Over the past few decades, benzimidazoles, triazoles and their derivatives have been grabbing the attention of the synthetic chemists for their wide gamut of antibacterial and antifungal activities targeting microbial protein DHFR...
February 6, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30686264/synthesis-anticancer-evaluation-and-synergistic-effects-with-cisplatin-of-novel-palladium-complexes-dna-bsa-interactions-and-molecular-docking-study
#13
Nenad Joksimović, Nenad Janković, Jelena Petronijević, Dejan Baskić, Suzana Popovic, Danijela Todorović, Milan Zarić, Olivera Klisurić, Milan Vraneš, Aleksandar Tot, Zorica Bugarčić
BACKGROUND: In order to discover new agents for chemotherapy with improved properties related to existing and bearing in mind the fact that some Pd complexes possess better antitumor activity and exhibit less kidney toxicity comparing to cisplatin, series of novel square-planar palladium(II) complexes [Pd (L)2] (3a-f) with O,O bidentate ligands [L = ethyl 2-hydroxy-alkyl(aryl)-4-oxo-2-butenoate] were synthesized. METHODS: All complexes were characterized by spectral (UV-Vis, IR, NMR, ESI-MS) and X-ray analysis and examined for their cytotoxic effect on human cancer cell lines HeLa and MDA-MB 231 and normal fibroblasts (MRC-5)...
January 27, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30686263/synthesis-of-new-hydrazone-derivatives-and-evaluation-of-their-efficacy-as-proliferation-inhibitors-in-human-cancer-cells
#14
Piotr Świątek, Jolanta Saczko, Nina Rembiałkowska, Julita Kulbacka
BACKGROUND: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities. OBJECTIVE: In this study, we designed new derivative compounds from groups of hydrazones. METHOD: The group of new derivatives was evaluated by the viability assay in human cancer and normal cells. RESULTS: The dimethylpyridine hydrazones showed potent inhibition of cell proliferation of breast, colon cancer cells, human melanoma and glioblastoma...
January 27, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30569870/synthesis-plasmodium-falciparum-inhibitory-activity-cytotoxicity-and-solubility-of-n2-n4-disubstituted-quinazoline-2-4-diamines
#15
Nattakarn Pobsuk, Praphasri Suphakun, Supa Hannongbua, Chanin Nantasenamat, Kiattawee Choowongkomon, M Paul Gleeson
BACKGROUND: Despite the development of extensive control strategies and treatment options, approximately 200 million malaria cases, leading to approximately 450,000 deaths, were reported in 2015. Due to issue of disease resistance, additional drug development efforts are needed to produce new, more effective treatments. Quinazoline-2,4-diamines were identified as anti-parasitic compounds over three decades ago and have remained of interest to date in industry and academia. OBJECTIVE: An anti-malarial SAR evaluation of previously unreported N2,N4-disubstituted quinazoline-2,4-diamines have been undertaken in this study...
December 18, 2018: Medicinal Chemistry
https://read.qxmd.com/read/30569869/the-multiple-applications-and-possible-mechanisms-of-the-hyperbaric-oxygenation-therapy
#16
Wan Chen, Xingmei Liang, Zhihuan Nong, Yaoxuan Li, Xiaorong Pan, Chunxia Chen, Luying Huang
Hyperbaric Oxygenation Therapy (HBOT) is used as adjunctive method for multiple diseases. The method meets the routine treating and is non-invasive, as well as provides 100% pure oxygen (O2) which is at above-normal atmospheric pressure in a specialized chamber. It is well known that in the condition of O2 deficiency, it will induce a series of adverse events. In order to prevent the injury induced by anoxia, the capability of offering pressurized O2 by HBOT seems involuntary and significant. In recent years, HBOT displays particular therapeutic efficacy in some degree, and it is thought to be beneficial to the conditions of angiogenesis, tissue ischemia and hypoxia, nerve system disease, diabetic complications, malignancies, Carbon monoxide (CO) poisoning and chronic radiation-induced injury...
December 18, 2018: Medicinal Chemistry
https://read.qxmd.com/read/30569868/structural-variability-in-the-rlr-mavs-pathway-and-sensitive-detection-of-viral-rnas
#17
Qiu-Xing Jiang
Cells need high-sensitivity detection of non-self molecules in order to fight against pathogens. These cellular sensors are thus of significant importance to medicinal purposes, especially for treating novel emerging pathogens. RIG-I-like receptors (RLRs) are intracellular sensors for viral RNAs (vRNAs). Their active forms activate mitochondrial antiviral signaling protein (MAVS) and trigger downstream immune responses against viral infection. Functional and structural studies of the RLR-MAVS signal pathway have revealed significant supramolecular variability in the past few years, which revealed different aspects of the functional signaling pathway...
December 18, 2018: Medicinal Chemistry
https://read.qxmd.com/read/30569867/synthesis-molecular-modelling-and-biological-studies-of-3-hydroxy-pyrane-4-one-and-3-hydroxy-pyridine-4-one-derivatives-as-hiv-1-integrase-inhibitors
#18
Hajar Sirous, Afshin Fassihi, Simone Brogi, Giuseppe Campiani, Frauke Christ, Zeger Debyser, Sandra Gemma, Stefania Butini, Giulia Chemi, Alessandro Grillo, Rezvan Zabihollahi, Mohammad R Aghasadeghi, Lotfollah Saghaie, Hamid R Memarian
BACKGROUND: Despite the progresses in the discovery of antiretroviral compounds for treating HIV-1 infection by targeting HIV integrase (IN), a promising and well-known drug target against HIV-1, there is a growing need to increase the armamentarium against HIV, for avoiding the drug resistance issue. OBJECTIVE: To develop novel HIV-1 IN inhibitors, a series of 3-hydroxy-pyrane-4-one (HP) and 3-hydroxy-pyridine-4-one (HPO) derivatives have been rationally designed and synthesized...
December 18, 2018: Medicinal Chemistry
https://read.qxmd.com/read/30569866/discovery-of-n-phenyl-4-1h-pyrrol-3-yl-pyrimidin-2-amine-derivatives-as-potent-mnk2-inhibitors-design-synthesis-sar-analysis-and-evaluation-of-in-vitro-anti-leukaemic-activity
#19
Ahmed M Abdelaziz, Sarah Diab, Saiful Islam, Sunita K C Basnet, Ben Noll, Peng Li, Laychiluh B Mekonnen, Jingfeng Lu, Hugo Albrecht, Robert W Milne, Cobus Gerber, Mingfeng Yu, Shudong Wang
BACKGROUND: Aberrant expression of eukaryotic translation initiation factor 4E (eIF4E) is common in many types of cancer including acute myeloid leukaemia (AML). Phosphorylation of eIF4E by MAPK-interacting kinases (Mnks) is essential for the eIF4E-mediated oncogenic activity. As such, the pharmacological inhibition of Mnks can be an effective strategy for the treatment of cancer. METHODS: A series of N-phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine derivatives was designed and synthesised...
December 18, 2018: Medicinal Chemistry
https://read.qxmd.com/read/30569872/the-inhibition-of-polysialyltranseferase-st8siaiv-through-heparin-binding-to-polysialyltransferase-domain-pstd
#20
Li-Xin Peng, Xue-Hui Liu, Bo Lu, Si-Ming Liao, Feng Zhou, Ji-Min Huang, Dong Chen, Frederic A Troy Ii, Guo-Ping Zhou, Ri-Bo Huang
BACKGROUND: The polysialic acid (polySia) is a unique carbohydrate polymer produced on the surface of neuronal cell adhesion molecule (NCAM) in a number of cancer cells, and strongly correlates with the migration and invasion of tumor cells and with aggressive, metastatic disease and poor clinical prognosis in the clinic. Its synthesis is catalyzed by two polysialyltransferases (polySTs), ST8SiaIV (PST) and ST8SiaII (STX). Selective inhibition of polySTs, therefore presents a therapeutic opportunity to inhibit tumor invasion and metastasis due to NCAM polysialylation...
December 17, 2018: Medicinal Chemistry
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