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Medicinal Chemistry

Abha Sharma, Keert Jain, Swaran J S Flora
BACKGROUND: Tuberculosis (TB) is a deadly infectious disease caused by the pathogen Mycobacterium tuberculosis (M.tb). Approximately, 1.8 and 1.3 billion people are infected and die, respectively from TB each year as estimated by World Health Organization. Due to increase in the incidence of drug-resistant strains of M.tb, there is an urgent need to accelerate research which focuses on the development of new drugs with novel mechanism of action that can treat both drug-sensitive and resistant TB infections...
November 2, 2017: Medicinal Chemistry
Sobhi M Gomha, Magda A Abdallah, Ikhlass M Abbas, Mariam S H Kazem
BACKGROUND: Chalcones, 2-pyrazolines and thiazoles have been reported to possess various pharmacological activities. OBJECTIVES: Synthesis of new chalcones and utilizing them as a building block for constructing a series of thiazole derivatives and evaluate some of them as anticancer agents. METHODS: The new compounds were synthesized via stirring at room temperature or thermal heating. Cytotoxic evaluation of the new synthesized compounds was tested using the method of Skehan et al...
October 20, 2017: Medicinal Chemistry
Maya Z Gibson, Minh A Nguyen, Sarah K Zingales
BACKGROUND: Chalcones, natural products produced by plants as a natural defense mechanisms against various pathogens, are molecules with structures that include two aromatic rings joined by an α, β unsaturated carbonyl system. Previous research has demonstrated that chalcones exhibit a wide variety of biological activities, including anticancer, antifungal, and antibiotic properties. OBJECTIVE: Our goal is to synthesize novel heterocyclic-containing chalcones and have their biological activities evaluated...
October 20, 2017: Medicinal Chemistry
Humera Jahan, Muhammad Iqbal Choudhary, Amber Atta, Khalid Mohammad Khan, Atta-Ur- Rahman
BACKGROUND: Anthranilic acid derivatives are important pharmacophores in drug discovery. Several of them are currently used drugs, such as mefenamic acid and meclofenamates, possess analgesic, anti-inflammatory, and antipyretic activities. Some anthranilic acid-based scaffolds have also been reported for the management of metabolic disorders. OBJECTIVES: The aim of the current study was to investigate the antiglycation potential of anilino benzoic acid derivatives against fructose- human serum albumin (HSA) glycation...
October 20, 2017: Medicinal Chemistry
Mariusz Mojzych, Pawel Tarasiuk, Zbigniew Karczmarzyk, Malgorzata Juszczak, Wojciech Rzeski, Andrzej Fruziński, Artur Wozny
A convenient approach toward polycyclic frameworks containing fused 1,2,4-triazoles is described. The synthesis consists of alkylation of N1-unsubstituted pyrazolo[4,3-e][1,2,4]triazine, followed by nucleophilic substitution of methylsulfonyl group with hydrazine and reaction of 5-hydrazino-pyrazolo[4,3-e][1,2,4]triazines with organic acids. The final step of the construction of fused triazolo derivatives includes synthesis of appropriate hydrazide derivatives that undergo an intramolecular cyclization to form linear form of pyrazolo[4,3-e]triazolo[4,5-b][1,2,4]triazine derivatives...
October 20, 2017: Medicinal Chemistry
Jin Zhou, Jinzheng Wang, Chao Chen, Haoliang Yuan, Xiaoan Wen, Hongbin Sun
BACKGROUND: USP7 (ubiquitin specific protease 7, also known as HAUSP) is one of the deubiquitinating enzymes (DUB) that reverse ubiquitination and spare substrate proteins from degradation. METHODS: After a brief introduction of ubiquitin-proteasome system (UPS) and human DUB, this review focuses on the structural and functional complexity of USP7 in tumor development and progression. Afterwards, USP7's physiological regulatory mechanisms and manipulation strategies are elaborated...
October 20, 2017: Medicinal Chemistry
Rita Morigi, Beatrice Vitali, Cecilia Prata, Rogers A A Palomino, Alessandra Graziadio, Alessandra Locatelli, Mirella Rambaldi, Alberto Leoni
BACKGROUND: Fused five-membered heterocyclic rings containing bridgehead nitrogen atom are particularly versatile in the field of medicinal chemistry because of their different biological activities. Among them, the imidazo[2,1-b]thiazole is an attractive fused heterocyclic core that has been extensively studied. OBJECTIVE: The aim of the current study was to study the therapeutic applications of imidazo[2,1-b]thiazole derivatives as antimicrobial agents for the treatment of genitourinary infections...
October 10, 2017: Medicinal Chemistry
Lenka Applova, Elma Veljovic, Samija Muratovic, Jana Karlickova, Katerina Macakova, Davorka Završnik, Luciano Saso, Kemal Duric, Premysl Mladenka
BACKGROUND: Currently used oral antiplatelet drugs are both limited and associated with risk of treatment failure/resistance. Research in this area is hence highly desired. A series of xanthene-3-ones derivatives, we had synthesized, showed us that these derivatives had antiplatelet activity. As far as we know, no research on the effects of xanthen-3-ones in this area has been done. OBJECTIVE: The aim was to study the antiplatelet potential of a series of synthesised 9-phenyl-xanthene-3-ones and to find the ideal structural feature(s) for antiplatelet potential and determine the mechanism of action...
October 10, 2017: Medicinal Chemistry
Jiulin Huang, Si-Ying Xiang, Min Lv, Liu-Meng Yang, Yuanyuan Zhang, Yong-Tang Zheng, Hui Xu
BACKGROUND: The human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) has always been the global health threat and the leading cause of deaths. However, due to the emergence of drug-resistant HIV, an inevitable consequence of increasing use of antiretroviral drugs posed a major threat to antiretroviral therapy success. OBJECTIVE: The discovery of anti-HIV-1 agents will be used for the effective treatment of HIV/AIDS. METHOD: In continuation of our program aimed to discover anti-HIV-1 agents, twelve matrine derivatives, such as 14-formyl-15-aryloxy/methoxymatrines (3a-j) and 14-aryloxymethylidenylmatrines (3k,l), were semi-prepared from matrine, and evaluated against HIV-1ⅢB replication in acutely infected C8166 cells in vitro...
October 2, 2017: Medicinal Chemistry
Hakan Sezgin Sayiner, Afaf A S Abdalrahm, Murat A Başaran, Vasyl Kovalishyn, Fatma Kandemirli
BACKGROUND: Acinetobacter is a Gram-negative, catalase-positive, oxidase-negative, non-motile, and no fermenting. OBJECTIVE: In this study, some of the electronic and molecular properties, such as the highest occupied molecular orbital energy (EHOMO), lowest unoccupied molecular orbital energy (ELUMO), the energy gap between EHOMO and ELUMO, Mulliken atomic charges, bond lengths, of molecules having impact on antibacterial activity against A. Baumannii were studied...
October 2, 2017: Medicinal Chemistry
Andrew J Byrne, Sandra A Bright, Darren Fayne, James P McKeown, Thomas McCabe, Brendan Twamley, Clive Williams, Mary J Meegan
BACKGROUND: Cancers of the lymphatic cells (lymphomas) account for approximately 12% of malignant diseases worldwide. The nitrostyrene scaffold is identified as a lead target structure for development of particularly effective compounds targeting Burkitt's lymphoma (BL). OBJECTIVES: The aims of the curent study were to synthesise a panel of nitrostyrene compounds and to evaluate their activity in Burkitt's lymphoma (BL). METHODS: A panel of structurally varied compounds were designed and synthesised using Henry Knoevenagel condensation reactions...
October 2, 2017: Medicinal Chemistry
Armando L Morera-Fumero, Pedro Abreu-Gonzalez, Manuel Henry-Benitez, Lourdes Fernandez-Lopez, Estefania Diaz-Mesa, Maria Del Rosario Cejas-Mendez, Fernando Guillen-Pino
BACKGROUND: Seasonal and circadian changes are two factors described to affect blood levels of some biological molecules. The Total Antioxidant Capacity (TAC) is one global measure of the antioxidant capacity of a system. There is no agreement about the existence of day/night changes in TAC levels as well as there is no information about seasonal changes in TAC levels. OBJECTIVE: The aims of this research are studying if there are summer/winter changes in TAC concentrations or if TAC concentrations have day/night changes...
October 2, 2017: Medicinal Chemistry
Olivier Van der Poorten, Mouhamad Jida, Dirk Tourwé, Steven Ballet
BACKGROUND: Benzazepines received great attention in the field of medicinal chemistry since this scaffold has been recognized to belong to the important family of privileged templates. More specifically, the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) is used as a core structure in a variety of constrained therapeutic peptide (turn) mimetics. Most of the synthetic approaches towards this template have focused on cyclizations which form the central 7-membered azepine ring. OBJECTIVE: Previous investigations in our group allowed an expansion of the substitution patterns in the 4-amino-benzazepin-3-one scaffold by introduction of methyl substituents at positions 4 and 5 of the azepinone ring system, but also to 1-aryl substituted compounds...
October 2, 2017: Medicinal Chemistry
Barbara Czaplińsk, Ewelina Spaczyńska, Robert Musioł
Background Fluorescent compounds had gained strong attention due to their wide and appealing applications. Microscopic techniques and visualization are good examples among others. Introduction of fluorescent dyes into microbiology opens the possibility to observe tissues, organisms or organelle with exceptional sensitivity and resolution. Probes for detection of biologically relevant metals as zinc, iron or copper seems to be particularly important for drug design and pharmaceutical sciences. Objective Quinoline derivatives are well known for their good metal affinity and wide spectrum of biological activity...
October 2, 2017: Medicinal Chemistry
Shicheng Hou, Henan Xu, Jianshu Hu, Jian Hou, Yan Wang, Zhe Jin, David C C Wan, Chun Hu
Background Osteoporosis (OP) is a common bone disease, most often diagnosed in post-menopausal women. The majority of OP treatments focused at manipulation of the patient's hormone levels, therefore, they are associated with significant adverse effects. Objective To design, synthesize and evaluate the β-catenin translocation capability and the alkaline phosphatase (ALP) activation activity of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives. Method The styrene derivatives were synthesized as raw materials, followed by oxidation and condensation reactions, 6-aryl-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one derivatives (1) were obtained...
October 2, 2017: Medicinal Chemistry
Katarzyna Pietrzak, Kamila Czarnecka, Elżbieta M Ikiciuk-Olasik, Paweł Szymański
As lifespan tendency is increasing, age-related diseases are becoming a burden to the society and health care system. Mostly incurable, constitute a subject of researchers' work. In this review the insight into the problem of Alzheimer Disease (AD) diagnostics will be given. The unquestionable diagnosis is possible only during a post-mortem examination. AD is known as one of the forms of dementia and its differentiation from mild cognitive impairments has to be improved. Despite a great diagnostic progress during last decades, medicine still needs more accurate tools for an early detection of this incurable disease...
October 2, 2017: Medicinal Chemistry
Alfonso López-Vázquez, Jesús Garcia-Bañuelos, Angélica González-Garibay, Pedro Urzúa-Lozano, Susana Del Toro-Arreola, Miriam R Bueno-Topete, Sergio Sánchez-Enríquez, José Muñoz-Valle, Luis Jave-Suárez, Juan Armendáriz-Borunda, Blanca E Bastidas-Ramirez
BACKGROUND: 3,3'-Diindolylmethane (DIM) is a condensation product of indole-3-carbinol, a glucosinolate naturally occurring in Brassica genus vegetables. The antiinflammatory properties of DIM through the inhibition of NF-κB, as well as its ameliorating effects on glucose tolerance and hyperglicemic states, have been described. A subclinical proinflammatory profile resultant from the interaction of adipocytes and macrophages have been reported in obesity, affecting the insulin signaling pathway, contributing to insulin resistance...
September 21, 2017: Medicinal Chemistry
Steve Simpson, Ingrid van der Mei, Bruce Taylor
Multiple sclerosis (MS) is a progressive, demyelinating condition of the central nervous system, manifesting in loss or alterations in function of sensory, motor and cognitive function. Of the various environmental and behavioural risk factors identified as playing a role in MS onset and progression, perhaps none has been as consistent as vitamin D. OBJECTIVE: In this review, we will endeavour to present a general background on the role of vitamin D in human health and particularly in MS, as well as the substantial epidemiological evidence in support of vitamin D's role in MS...
September 21, 2017: Medicinal Chemistry
Marina Boziki, Nikolaos Grigoriadis
BACKGROUND: Matrix metalloproteinases (MMPs) are zinc-containing endopeptidases, proteins essential to the degradation of various tissue extracellular matrix proteins. Under normal conditions MMPs participate in several physiological processes, both in the developing organism and the adult. Multiple sclerosis (MS) is an inflammatory demyelinating disease of the central nervous system (CNS), affecting primarily young adults. Inflammatory infiltrations of the CNS parenchyma by autoreactive immune cells, that mediate myelin degradation in the form of the demyelination "plaque", are the pathological hallmark of the disease...
September 6, 2017: Medicinal Chemistry
Ioannis Heliopoulos, Athanasia Patousi
BACKGROUND: Monoclonal antibodies (mAbs) are now established as targeted therapies for malignancies, transplant rejection, autoimmune and infectious diseases. Two monoclonal antibodies are available for treatment and other antibodies are currently being tested in multiple sclerosis (MS) patients. OBJECTIVES: The purpose of the present review paper is to outline the antibody engineering technologies, the immunologic and pharmacologic concepts of mΑbs and the current status of treatment in MS with emphasis on clinical efficacy and safety...
September 6, 2017: Medicinal Chemistry
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