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Medicinal Chemistry

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https://www.readbyqxmd.com/read/28875862/an-update-on-the-role-of-matrix-metalloproteinases-in-the-pathogenesis-of-multiple-sclerosis
#1
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
https://www.readbyqxmd.com/read/28875861/therapeutic-monoclonal-antibodies-and-multiple-sclerosis-the-essentials
#2
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
https://www.readbyqxmd.com/read/28875860/scaffold-hopping-strategy-for-the-design-synthesis-and-biological-activity-evaluation-of-novel-hexacyclic-scutellarein-derivatives-with-a-1-3-oxazine-ring-fused-at-a-ring
#3
Yue Zhong, Yu-Ting Lu, Ying Sun, Nian-Guang Li, Ting Gu, Wen-Yu Wu, Shao-Peng Yu, Zhi-Hao Shi
BACKGROUND: Discovery of novel agents with anticoagulant and antioxidant activity is very important to treat cerebrovascular disease. Lead compound LR3d discovered in our laboratory exhibited stronger anticoagulant ability and good antioxidant activity, compared with scutellarein (2), which is the major in vivo active metabolite of the natural product scutellarin (1). OBJECTIVE: Design and synthesis novel scutellarein derivatives with improved anticoagulant and antioxidant activity...
September 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28875859/myelin-oligodendrocyte-glycoprotein-and-multiple-sclerosis
#4
Maria-Eleni Androutsou, Anthi Tapeinou, Alexios Vlamis-Gardikas, Theodore Tselios
BACKGROUND: Myelin oligodendrocyte glycoprotein (MOG) is located on the external surface of myelin, a membranous component of the central nervous system (CNS) that forms the insulating lipid layer around neurons. The major MOG splicing variant (a1 transcript) encodes a transmembrane protein with an extracellular domain of an Ig variable (IgV) fold. MOG IgV domains from the same or different cells dimerize and contribute to the organization and maintenance of the myelin sheath in neurons...
September 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28875858/managing-neuropathic-pain-in-multiple-sclerosis-pharmacological-interventions
#5
Samuel S Duffy, Justin G Lees, Chamini J Perera, Gila Moalem-Taylor
BACKGROUND: Multiple sclerosis (MS) is a chronic inflammatory demyelinating disease of the central nervous system (CNS). Of the plethora of motor and sensory disturbances experienced by sufferers, neuropathic pain is a highly prevalent and debilitating symptom, and at present remains extremely difficult to treat. Common forms of neuropathic pain seen in MS patients include central neuropathic pain, Lhermitte's phenomenon and trigeminal neuralgia, which are all speculated to arise from specific patterns of lesion formation...
September 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28875857/is-there-a-link-between-vitamin-b-and-multiple-sclerosis
#6
Natalie Nemazannikova, Kathleen Mikkelsen, Lily Stojanovska, Gregory L Blatch, Vasso Apostolopoulos
BACKGROUND: Damage to the myelin sheath (demyelination) is one of the main manifestations of multiple sclerosis (MS). Interestingly, both MS and vitamin B deficiency results in severe myelin degeneration that leads to loss in neuronal signal transmission. OBJECTIVE: Deficiency in vitamin B complex vary, although common symptoms include fatigue, increased oxidative stress, inflammation and demyelination. In particular, vitamin B12 (cobalamin) has had increased attention for its role in the methylation process, involvement in myelination and re-myelination, and reversal of MS symptoms...
September 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28875856/identification-of-1-aryl-1h-1-2-3-triazoles-as-potential-new-antiretroviral-agents
#7
Daniel T G Gonzaga, Thiago M L Souza, Viviane M M Andrade, Vitor F Ferreira, Fernando de C da Silva
BACKGROUND: Low molecular weight 1-Aryl-1H-1,2,3-triazoles are endowed with various types of biological activity, such as against cancer, HIV and bacteria. Despite the existence of six different classes of antiretroviral drugs in clinical use, HIV/AIDS continue to be an on growing public health problem. OBJECTIVE: In the present study, we synthesized and evaluated thirty 1-Aryl-1H-1,2,3-triazoles against HIV replication. METHOD: The compounds were prepared by Huisgen 1,3-dipolar cycloaddition protocol catalyzed by Cu(I) between aryl azides and propargylic alcohol followed by further esterification and etherification from a nucleophilic substitution with acid chlorides or alkyl bromides in good yields...
September 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28745232/in-vitro-%C3%AE-glucosidase-inhibition-by-non-sugar-based-triazoles-of-dibenzoazepine-their-structure-activity-relationship-and-molecular-docking
#8
Maria A Khan, Kulsoom Javaid, Abdul Wadood, Alam Jamal, Farhana Batool, Saba Fazal-Ur-Rehman, Fatima Z Basha, M Iqbal Choudhary
BACKGROUND: α-Glucosidase inhibitors (AGIs) have been reported for their clinical potential against postprandial hyperglycemia, which is responsible for risks associated with diabetes mellitus 2 and cardiovascular diseases (CVDs). Besides, a number of compounds have been reported as potent AGIs, several side effects are associated with them. METHODS: The aim of present work is to explore new and potent molecules as AGIs. Therefore, a library of dibenzoazepine linked triazoles (1-15) was studied for their in vitro α-glucosidase inhibitory activity...
July 26, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28745231/synthesis-and-antimalarial-activity-of-new-enantiopure-aminoalcoholpyrrolo-1-2-a-quinoxalines
#9
Alexia Jonet, Jean Guillon, Catherine Mullié, Anita Cohen, Guillaume Bentzinger, Jérémy Schneider, Nicolas Taudon, Sebastien Hutter, Nadine Azas, Stephane Moreau, Solene Savrimoutou, Patrice Agnamey, Alexandra Dassonville-Klimpt, Pascal Sonnet
Backgroung: We prepared a novel series of enantiopure mefloquine analogues with pyrrolo[1,2-a]quinoxaline core in order to fight Plasmodium falciparum resistant strain. OBJECTIVES: To observe the influence of pyrrolo[1,2-a]quinoxaline core versus quinoline core on the antimalarial activity. METHOD: Four enantiopure aminoalcoholpyrrolo[1,2-a]quinoxalines 2 were synthetized via Sharpless asymmetric dihydroxylation reaction in eight steps. Their antimalarial activity was evaluated on two Plasmodium falciparum strains 3D7 and W2 with a SYBR Green I fluorescence-based method and their cytotoxicity was measured on four cell lines HepG2, THP-1, CHO and HFF...
July 26, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28676003/synthesis-structural-characterization-and-antinociceptive-activities-of-new-arylated-quinolines-via-suzuki-miyaura-cross-coupling-reaction
#10
Malik Aman Ullah, Muhammad Adeel, Muhammad N Tahir, Abdur Rauf, Muhammad Akram, Taibi Ben Hadda, Yahia N Mabkhot, Naveed Muhammad, Fehmida Naseer, Mohammad S Mubarak
Backgorund: The quinoline ring system is one of the most commonly encountered heterocycles in medicinal chemistry, due to the pharmaceutical and medicinal uses of derivatives containing this ring. These quinoline-based compounds have remarkable biological activity, as they are employed as antimalarial, antibacterial, antifungal, and antitumor agents. The quinoline nucleus can be synthesized by various traditional methods such as the Skraup reaction, Friedlaender synthesis, Combes quinoline synthesis, Larock quinoline synthesis, among others...
July 4, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28676004/evaluation-of-1-3-benzoxathiol-2-one-derivatives-as-potential-antifungal-agents
#11
Luciana Terra, Eliza de L Chazin, Paola de S Sanches, Max Saito, Marcus V N de Souza, Claudia R B Gomes, James L Wardell, Solange M S V Wardell, Plínio C Sathler, Gabriela C C Silva, Viviane O Lione, Marcos Kalil, Ana Joffily, Helena C Castro, Thatyana R A Vasconcelos
BACKGROUND: Over the last few years, fungal infections have emerged as a worrisome global public health problem. Candidiasis is a disease caused by Candida species and has been a problem worldwide mainly for immunosuppressed patients. Lately, the resistant strains and side effects have been reported as important issues for treating Candidiasis, which have to be solved by identifying new drugs. OBJECTIVE: The goal of this work was to synthesize a series of 1,3-benzoxathiol-2-one derivatives, XY-benzo[d][1,3]oxathiol-2-ones, and evaluate their antifungal activity against five Candida species...
July 3, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641529/irna-2methyl-identify-rna-2-o-methylation-sites-by-incorporating-sequence-coupled-effects-into-general-pseknc-and-ensemble-classifier
#12
Wang-Ren Qiu, Shi-Yu Jiang, Bi-Qian Sun, Xuan Xiao, Xiang Cheng, Kuo-Chen Chou
OBJECTIVE: Being a kind of post-transcriptional modification (PTCM) in RNA, the 2'-O-methylation modification occurs in the processes of life development and disease formation as well. Accordingly, from the angles of both basic research and drug development, we are facing a challenging problem: given an uncharacterized RNA sequence formed by many nucleotides of A (adenine), C (cytosine), G (guanine), and U (uracil), which one can be of 2-O-methylation modification, and which one cannot? Unfortunately, so far no computational method whatsoever has been developed to address such a problem...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641528/drug-design-synthesis-and-in-vitro-evaluation-of-substituted-benzofurans-as-hsp90-inhibitors
#13
Sundeep Kadasi, Thadeu E M M Costa, Neha Arukala, Mallika Toshakani, Chaitanya Duggineti, Sreekanth Thota, Sayan Dutta Gupta, Shiva Raj, Carmen Penido, Maria G Henriques, Nulgumnalli Manjunathaiah Raghavendra
BACKGROUND: Heat shock protein 90 is a molecular chaperone required for the stability and function of several client proteins that promote cancer cell growth and/or survival. Discovery of Hsp90 inhibitors has emerged as an attractive target of research in cancer therapeutics. Natural products like geldanamycin and radicicol are established Hsp90 inhibitors, but face limitations with toxicity and inactivity, by in vivo studies respectively. However, they lay the logical starting point for the design of novel synthetic or semi-synthetic congeners as Hsp90 inhibitors...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641527/design-synthesis-and-biological-evaluation-of-c-2-substituted-3h-thieno-2-3-d-pyrimidin-4-one-derivatives-as-novel-fgfr1-inhibitors
#14
Ping Guo, Faqing Ye, Zixin Xie, Huan Zhang, Zaikui Zhang, Chao Han, Donghua Cheng, Dan Lin, Yuan Zhang, Xuebao Wang, Xin Guo
BACKGROUND: Thienopyrimidinone is a newly designed, selective fibroblast growth factor receptor 1 (FGFR1) inhibitor with an excellent anticancer effect. OBJECTIVE: The goal of the present study was to design and synthesize better FGFR1 inhibitors through modifications of the lead compound thienopyrimidinone. METHODS: In the present study, a series of C-2 substituted derivatives of thienopyrimidinone, namely L1-L16, were synthesized, and their inhibitory effects on FGFR1 were evaluated...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641526/biology-oriented-synthesis-bios-of-piperine-derivatives-and-their-comparative-analgesic-and-antiinflammatory-activities
#15
Ammar Yasir, Saiqa Ishtiaq, Muhammad Jahangir, Muhammad Ajaib, Uzma Salar, Khalid Mohammed Khan
BACKGROUND: Serious side effects such as gastric intestinal ulcer, bleeding etc. are associated with most of the antiinflammatory and analgesic drugs. So there is a need to search novel, potent, and safer antiinflammatory and analgesic drug. METHOD: Based on "biology-oriented synthesis approach", piperine alkaloid was isolated from Piper nigrum L. and some derivatives of piperine having azomethine, sulfamoyl, propanoyl, acetamoyl and heterocyclic oxadiazole were synthesized...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641525/1-1%C3%AA-carbonyldiimidazole-cdi-mediated-facile-synthesis-structural-characterization-antimicrobial-activity-and-in-silico-studies-of-coumarin-3-carboxamide-derivatives
#16
Uzma Salar, Khalid Mohammed Khan, Muhammad Imran Fakhri, Shafqat Hussain, Saima Tauseef, Shagufta Ameer, Abdul Wadood, Huma Khan, Shahnaz Perveen
BACKGROUND: Despite of the availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. So, identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. METHOD: To explore the antimicrobial activity of coumarin-3-carboxamides for a range of bacterial and fungal strains, twenty eight derivatives were synthesized by the reaction of coumarin-3-carboxylic acid with a variety of aniline derivatives in the presence of 1,1ꞌ-carbonyldiimidazole (CDI)...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28629311/cell-cycle-arrest-and-apoptosis-induction-activity-of-nitidine-chloride-on-acute-myeloid-leukemia-cells
#17
Peng Li, Shuxin Yan, Xin Dong, Zhao Li, Yu Qiu, Chunyan Ji, Jingru Zhang, Min Ji, Wei Li, Hongchun Wang, Zhi Liu, Xing Li Wang, Jingjing Ye, Daoxin Ma
: Background: Acute myeloid leukemia (AML) is the most common hematological malignancy in adults, characterized by distorted proliferation and development of myeloid cells and their precursors in the bone marrow. Nitidine chloride, a naturally occurring alkaloid, has been identified to possess antitumor activity. However, the effects of nitidine chloride on acute myeloid leukemia cells and its underlying mechanisms have not been elucidated. Here we investigated the cellular and molecular mechanism of the anti-leukemic effects of nitidine chloride...
June 19, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28606042/isolation-of-chlorogenic-acid-from-soil-borne-fungi-screlotium-rolfsii-their-reversal-of-multidrug-resistance-and-anti-proliferative-in-mouse-lymphoma-cells
#18
Bashir Ahmad, Muhammad Rizwan, Abdur Rauf, Muslim Raza, Shumaila Bashir, Joseph Molnáre, Ákos Csonka, Diána Szabó, Mohammad S Mubarak, Mah Noor, Bina S Siddiqui
BACKGROUND: Fungi performing a wide range of function in soil by secreting low molecular weight compound known as secondary metabolites. S. rolfsii is a soil borne phytopathogenic fungi was used for the production of bioactive compounds. OBJECTIVE: The present study belongs to evaluate the anticancer potentials of a secondary metabolites isolated from S. rolfsii, their multidrug resistance (MDR), and molecular docking study. METHOD: (1S,3R,4R,5R,E)-3-(3-(3,4-Dihydroxyphenyl)acryloyloxy)-1,4,5 trihydroxycyclohexanecarboxylic acid (1), or best known as chlorogenic acid, was isolated from the ethyl acetate fraction of crude secondary metabolites produced by the soil borne Fungus Screlotium rolfsii...
June 12, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28571532/rapid-access-to-oxazine-fused-furocoumarins-and-in-vivo-and-in-silico-studies-of-theirs-biological-activity
#19
Alla V Lipeeva, Dmitry S Baev, Margarita P Dolgikh, Tatijana G Tolstikova, Elvira E Shults
BACKGROUND: The synthesis of 1,2-oxazine-fused linear furocoumarins was performed involving the transition metal catalysis reaction of plant coumarin oreoselone derivatives. OBJECTIVE AND METHODS: The Pd-catalyzed desulfonative cross-coupling reactions of 2-(tosyl)oreoselone with terminal alkynes and the successive treatment of the obtained 2-(arylethynyl)furocoumarins with an excess of hydroxylamine gave the expected (Z,E)-3-(hydroxyimino)-2-(arylethynyl)furocoumarins with an (Z:E) ratio of about 1:0...
May 31, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28545385/effect-on-acetylcholinesterase-and-anti-oxidant-activity-of-synthetic-chalcones-having-a-good-predicted-pharmacokinetic-profile
#20
Renata Parruca Sakata, Micheli Figueiro, Daniel Fabio Kawano, Wanda Pereira Almeida
BACKGROUND: Acetylcholinesterase (AChE) is an important target in the development of drug to treat Alzheimer´s disease (AD). In this work, we investigated the effect of twenty-two synthesized chalcones on AChE activity. OBJECTIVE: This work is aimed to synthesize and evaluate the effect of chalcones on the AChE activity, as well as anti-oxidant activity and predict their pharmacokinetic profile. METHODS: Chalcones were synthesized through a Claisen-Schmidt condensation and their inhibitory effect on the AChE was evaluated by Elmann's colorimetric method...
May 25, 2017: Medicinal Chemistry
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