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Medicinal Chemistry

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https://www.readbyqxmd.com/read/29336266/design-synthesis-evaluation-and-computational-studies-of-nipecotic-acid-acetonaphthone-hybrids-as-potential-antiepileptic-agents
#1
Ankit Seth, Piyoosh A Sharma, Avanish Tripathi, Priyanka K Choubey, Pavan Srivastava, Prabhash N Tripathi, Sushant Kumar Shrivastava
BACKGROUND: Nipecotic acid is considered to be one of the most potent inhibitors of neuronal and glial γ- aminobutyric acid (GABA) uptake in vitro. However nipecotic acid does not readily cross the blood-brain barrier (BBB) following peripheral administration, owing to its hydrophilic nature. OBJECTIVE: A series of substituted acetonaphthones tethered nipecotic acid derivatives were designed and synthesized with an aim to improve the lipophilicity and the blood-brain barrier (BBB) permeation...
January 15, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332596/synthesis-and-characterization-of-thiocarbohydrazones-and-their-inhibitory-potential-against-ignored-disease-leishmaniasis
#2
Nida Ghouri, Khalid Mohammed Khan, Arshia, M Iqbal Choudhary, Shahnaz Perveen
BACKGROUND: Leishmaniasis is a protozoan parasitic vector-borne disease which is endemic in 88 tropical countries. Infected sand fly is the main cause of this disease while, there are several vectors, parasites, and reservoirs involved in the transmission of this disease. Leishmania donovani, L. infantum, and L. chagasi are. common disease causing species, spread through sandflies. It is considered to be a focal disease having scattered foci. Leishmaniasis is a disease with a broad clinical spectrum...
January 14, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332599/the-synthesis-of-chalcones-as-anticancer-prodrugs-and-their-bioactivation-in-cyp1-expressing-breast-cancer-cells
#3
Ketan Ruparelia, Keti Zeka, Randolph R Arroo, Kenneth J M Beresford
BACKGROUND: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in tumours. CYP1B1 has been shown to be active within tumours and is capable of metabolising a structurally diverse range of anticancer drugs. Because of this, and its role in the activation of procarcinogens, CYP1B1 is seen as an important target for anticancer drug development. OBJECTIVES: To synthesise a series of chalcone derivatives based on the chemopreventative agent DMU-135 and investigate their antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332595/new-bis-pyrazolones-as-potential-leads-for-ros-inhibition-environment-friendly-green-synthesis-structural-characterization-and-in-vitro-studies
#4
Sahar Yousuf, Khalid Mohammed Khan, Uzma Salar, Almas Jabeen, Shakil Ahmed, Munira Taj Muhammad, Aisha Faheem, Shahnaz Perveen
BACKGROUND: Pyrazolones have identified as significant antioxidant agents and many marketed and clinically prescribed NSAIDs have pyrazolone ring as main scaffold. METHOD: Keeping in consideration the antioxidant potential of pyrazolone scaffold, new bis-pyrazolones 3-30 were synthesized by a green and enviroment friendly reaction route, in which two equivalents of 1-(4-chlorophenyl)-3-methyl-1H-pyrazol-5-ol were treated with one equivalent of benzaldehyde derivatives without any catalyst...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332593/facile-synthesis-crystal-structure-dft-calculation-and-biological-activities-of-4-2-fluorophenyl-3-3-methoxybenzyl-1h-1-2-4-triazol-5-4h-one-5
#5
Muhammad Saleem, Muhammad Rafiq, Yeon Ki Jeong, Dae Won Cho, Chong-Hyeak Kim, Sung-Yum Seo, Chang-Shik Choi, Seong-Karp Hong, Ki-Hwan Lee
BACKGROUND: In the past few decades, the design, synthesis and characterization of novel heterocyclic compounds with auspicious biological profile received the considerable attention of scientific community. Among them, the small and simple organic molecular backbone like triazole moiety have broad spectrum of applications in the medicinal as well as diagnostic areas. OBJECTIVE: The objective of present study was the synthesis, characterization and exploration of biological profile of 4-(2-fluorophenyl)-3-(3-methoxybenzyl)-1H-1,2,4-triazol-5(4H)-one (5)...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332598/synthesis-of-new-isoxazole-pyridazine-pyrimidopyrazines-and-their-anti-inflammatory-and-analgesic-activity
#6
Ameen Ali Abu-Hashem, Mohamed El-Shazly
BACKGROUND: Isoxazoles, pyridazines, and pyrimidopyrazines have recently attracted attention due to their potent pharmacological activities. They exhibited anticancer, neuroprotective, analgesic and anti-inflammatory effects. OBJECTIVE: Synthesis of novel isoxazoles, pyridazines, and pyrimidopyrazines through efficient high yield protocol and evaluating their analgesics and anti-inflammatory activities. METHOD: A series of novel isoxazole-, pyridazine-, pyrimidopyrazine derivatives were prepared from 5,8-alkyl-1,3-dimethyl-5,6-dihydropyrimido[5,6-e]pyrazine-2,4,7-trione (1a,b) as the starting material...
January 11, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332597/synthesis-of-a-novel-class-of-1-3-oxathiolane-nucleoside-derivatives-of-t-705-and-evaluation-of-their-anti-influenza-a-virus-and-anti-hiv-activity
#7
Mingming Han, Xu Zhao, Xuedong Wu, Wei Huang, Xingzhou Li, Fang Yu
Backgroud: T-705 (Favipiravir) is a broad spectrum antiviral agent approved for stockpiling in Japan and currently in Phase 3 testing in the United States. Against influenza acts as a prodrug, converted intracellularly to selectively inhibit viral RNA-dependent RNA polymerase or similar enzymes. This is regarded as a novel antiviral mechanism of action, reducing cross-resistance to other existing anti-influenza drugs. OBJECTIVE: To develop new analogs, a class of 1,3-oxathiolane nucleoside derivatives of T-705 were designed and synthesized in this work...
January 11, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332594/in-vitro-and-in-silico-evaluation-of-non-quaternary-reactivators-of-ache-as-antidotes-of-organophosphorus-poisoning-a-new-hope-or-a-blind-alley
#8
Ondrej Soukup, Jan Korabecny, David Malinak, Eugenie Nepovimova, Ngoc Lam Pham, Kamil Musilek, Martina Hrabinova, Vendula Hepnarova, Rafael Dolezal, Petr Pavek, Petr Jost, Tereza Kobrlova, Jana Jankockova, Lukas Gorecki, Miroslav Psotka, Thuy Duong Nguyen, Karl Box, Breeze Outhwaite, Martina Ceckova, Ales Sofr, Daniel Jun, Kamil Kuca
BACKGROUND: In the last decade, the concept of uncharged reactivators potentially able to penetrate the CNS has been introduced as an alternative to the classic charged oxime reactivators. However, this concept brings with it several associated drawbacks such as higher lipophilicity, difficulty in administration, lower affinity to cholinesterases, and higher toxicity risk. OBJECTIVE: In this study we compare data obtained for a set of five classic charged reactivators and a set of three recently published uncharged oximes supplemented by two novel ones...
January 11, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332592/construction-of-an-m1gs-ribozyme-for-targeted-and-rapid-mrna-cleavage-application-on-the-ets-2-oncogene
#9
Chrisavgi Toumpeki, Dimitrios Anastasakis, Ioannis Panagoulias, Vassiliki Stamatopoulou, Tassos Georgakopoulos, Sofia Kallia-Raftopoulos, Athanasia Mouzaki, Denis Drainas
Background RNase P-mediated cleavage of target RNAs has been proposed as a promising tool for gene silencing. Ets-2 proto-oncogene controls the expression of a wide variety of genes involved in cancer and immunity. Objective Construction of a functional RNase P-based ribozyme (M1GS303) that targets Ets-2 mRNA Method The accessible sites for targeting of Ets-2 mRNA were identified by footprinting analysis. M1GS303 ribozyme was constructed by cloning. The activity of the ribozyme in the presence or absence of spiramysin in E...
January 11, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332591/anti-trypanosoma-cruzi-activity-in-vitro-of-phases-and-isolated-compounds-from-excoecaria-lucida-leaves
#10
Cristiane Franca da Silva, Ania Ochoa Pacheco, Rayane Nogueira Alves, Josean Fechine Tavares, Marcelo Sobral da Silva, Julio Cesar Escalona Arranz
BACKGROUND: Chagas disease is caused by the protozoan parasite Trypanosoma cruzi. This illness is found mainly in 21 Latin American countries and an estimated 8 million people are infected worldwide. The unsatisfactory chemotherapy provokes severe toxicity and resistant strains. Medicinal plants constitute a promising source of new drugs and remedies against all kinds of disorders, mainly infectious diseases arousing interest worldwide. OBJECTIVE: The aim of this study has been the isolation, structural identification and evaluation of the trypanocidal activity of samples present in the Excoecaria lucida Sw...
January 11, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29205121/synthesis-and-structure-activity-relationship-exploration-of-some-potent-anti-cancer-phenyl-amidrazone-derivatives
#11
Almeqdad Y Habashneh, Mustafa M El-Abadelah, Sanaa K Bardaweel, Mutasem O Taha
BACKGROUND: Amidrazones have been reported to have significant anti-tumor properties against several cancer cell lines. OBJECTIVES: The current project aims to profile the structure-anticancer activity relationship of phenyl-amidrazons. METHODS: Fifteen phenyl-amidrazone-piperazine derivatives were prepared and tested against four cancer cell lines (leukemia, prostate, breast and colon cancers). RESULTS: Six compounds illustrated low micromolar anticancer IC50 values, while the remaining compounds were either inactive or of moderate potencies...
December 4, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29205120/synthesis-and-in-vitro-antioxidant-activity-study-of-some-novel-substituted-piperazinyl-flavone-compounds
#12
Elmas Sari, Paweł Berczynski, Aleksandra Kładna, Irena Kruk, Oya B Dundar, Monika Szymanska, Hassan Y Aboul-Enein
BACKGROUND: A new series of 13 piperazinyl flavone derivatives has been synthesized and examined for their in vitro antiradical and antioxidant activities as response to the pharmacy industry's increasing demand for new non-toxic anti-inflammatory and anticancer drugs. METHODS: Their antioxidant activity was evaluated by the reactive oxygen species (ROS) scavenging assays, 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH ) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical cation (ABTS+ ) scavenging assays, and the ferric reducing antioxidant potency (TAC) method, and compared to known positive controls, herbal infusions, and penicillins...
December 3, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29205119/activity-of-rifabutin-and-hemi-synthetic-derivatives-against-mycobacterium-abscessus
#13
Ivy B Ramis, Ricardo Figueiredo, Daniela F Ramos, Priscila C B Halicki, Andrea von Groll, Miguel Viveiros, Maria do Ceu Costa, Pedro E A da Silva
BACKGROUND: Mycobacterium abscessus causes a wide range of clinical diseases that are difficult to treat. This microorganism is resistant not only to the classical antituberculosis agents but also to most of the antimicrobials that are currently available, resulting in limited therapeutic options and treatment failure. This scenario stresses the need to search for new drugs with activity against M. abscessus. OBJECTIVE: To evaluate in vitro the antimycobacterial activity and cytotoxicity of rifabutin (RFB 1) and ten derivatives (2-11) against M...
December 3, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29189174/xanthine-oxidase-inhibitory-and-molecular-docking-studies-on-pyrimidones
#14
Humaira Zafar, Sarosh Iqbal, Sumaira Javaid, Khalid M Khan, Muhammad I Choudhary
BACKGROUND: Xanthine oxidase is an important enzyme which catalyzes the production of uric acid and superoxide anion from xanthine. The over-production of these products lead to different disease conditions. For instance, uric acid is responsible of hyperuricemia, gout, and arthritis, while superoxide anion contributes to the oxidative stress, and related diseases. Hence XO is an important pharmacological target for the treatment of a range of diseases. METHODS: Based on the structural resemblance of pyrimidines with xanthine, a series of previously synthesized ethyl 6- methyl-2-oxo-1, 2, 3, 4-tetrahydro-5-pyrimidinecarboxylate derivatives were evaluated for XO inhibitory activity...
November 29, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29189173/prodrugs-for-nitroreductase-based-cancer-therapy-1-metabolite-profile-cell-cytotoxicity-and-molecular-modeling-interactions-of-nitro-benzamides-with-ssap-ntrb
#15
Tugba Gungor, Gulden Yetis, Ferah Cömert Onder, Esra Tokay, Tugba Taşkın Tok, Ayhan Celik, Mehmet Ay, Feray Kockar
BACKGROUND: Directed Enzyme Prodrug Therapy (DEPT) as an alternative method against conventional cancer treatments, in which the non-toxic prodrug is converted to highly cytotoxic derivative, has attracted an ample attentions in recent years for cancer therapy studies. OBJECTIVE: The metabolite profile, cell cytotoxicity and molecular modeling interactions of a series of nitro benzamides with Ssap-NtrB were investigated in this study. METHOD: A series of nitro-substituted benzamide prodrugs (1-4) were synthesized and firstly investigated their enzymatic reduction by Ssap-NtrB (S...
November 29, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29165092/synthesis-characterization-and-biological-activities-of-new-symmetric-bis-1-2-3-triazoles-with-click-chemistry
#16
Fatih Celik, Yasemin Unver, Burak Barut, Arzu Ozel, Kemal Sancak
BACKGROUND: 1,2,3-Triazole and its derivatives have important biological activities such as antimicrobial, anti-allergic, analgesic, anti-HIV, antiinflammatory, anticancer, antimalarial and antituberculosis. Other significant triazole derivatives are 1,2,4-triazoles which play a very important role in the medicinal chemistry due to the antiinflammatory, antimicrobial, antimigraine, anticancer, antimicrobial and antimycotic activities. In this study, we aimed to synthesize a new series of bis-1,2,3-triazole derivatives including 1,2,4-triazole to obtain more effective biological activities METHODS: In this study, a new series of bis-1,2,3-triazole compounds (9,10,11) were synthesized...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29165091/antibacterial-assessment-of-heteroaryl-vinyl-benzyl-and-alkyl-tetrazole-compounds
#17
Joshua Dudley, Liana Feinn, Heather DeFrancesco, Erica Lindsay, Adiel Coca, Elizabeth Lewis Roberts
BACKGROUND: In previous reports, the antibacterial properties of certain tetrazole derivatives have been described. We have previously reported the antibacterial properties of aryl 1H-tetrazole compounds. OBJECTIVE: To study the antibacterial activity of 5-substituted heteroaryl, vinyl, benzyl, and alkyl 1H-tetrazole derivatives. METHODS: The antibacterial properties of heteroaryl, vinyl, benzylic, and aliphatic tetrazole derivatives were investigated against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29165090/inhibition-of-adipogenesis-by-thiourea-derivatives
#18
Hina Siddiqui, Sarah Shafi, Farah Mukhtar, Asma Ejaz, Atta-Ur-Rahman, M Iqbal Choudhary
BACKGROUND: Obesity is one of the major health problem with inherent risk of type 2 diabetes, hypertension, CVDs etc. Adipogenesis is a major contributor in the process of obesity. Inhibition of adipocytes is one of the key approach to treat obesity. OBJECTIVE: To discover the new inhibitors of adipogenesis as the treatment for the obesity. METHOD: We describe here the synthesis and anti-adipogenic activity of thiourea derivatives 1-14. These derivatives were synthesized by the reactions of phenyl and pentafluorophenyl isothiocyanate with different aromatic amines...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29165089/a-novel-method-to-synthesize-phosphocreatine-and-phosphocreatine-prodrugs
#19
Maria Arkel, Patrizia Garbati, Annalisa Salis, Gianluca Damonte, Nara Liessi, Enrico Adriano, Umberto Benatti, Maurizio Balestrino, Enrico Millo
Background Adenosine triphosphate (ATP) is the energy currency of the body; it takes part in various and indispensable metabolic processes for the maintenance of cell homeostasis, degrading to its hydrolysis product, adenosine diphosphate (ADP). Efficient ways to restore ATP are therefore necessary in the cells. When the cell lacks energy due to ischemic conditions or high ATP demand, phosphocreatine gives its phosphate group to ADP that converts to ATP, in a reaction catalyzed by the enzyme creatine kinase...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29110620/vitamins-based-novel-target-pathways-molecules-as-possible-emerging-drug-targets-for-management-of-tuberculosis
#20
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
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