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Medicinal Chemistry

Tareq Abu-Izneid, Aneela Maalik, Saud Bawazeer, Ajmal Khan, Abdur Rauf, Taibi Ben Hadda, Haroon Khan, Mohamed Fawzy Ramadan, Imran Khan, Mohammad S Mubarak, Ghias Uddin, Alia Bahadar, Shujaat Ali Khan
BACKGROUND: Pistacia integerrima has many medicinal uses in therapeutic as well as folk medicine. P. integerrima has been used for the treatment of different ailments such as blood purifier, anti-inflammatory, and as remedy for gastrointestinal disorders such as vomiting and diarrhea, expectorant, cough, asthma and fever. OBJECTIVE: The main objective of this research work was to evaluate the effect of pistagremic acid (PA) isolated from the galls of Pistacia integerima in acute toxicity and gastrointestinal (GIT) motility tests...
October 7, 2016: Medicinal Chemistry
Huawei Zhang, Phillip Crews, Karen Tenney, Frederick A Valeriote
BACKGROUND: A growing evidence indicates that marine sponge Phyllospongia sp. is one of rich sources of 20, 24-bishomoscalane sesterterpenes with potent biological activities. In order to search more bioactive 20, 24-bishomoscalane sesterterpenes for new drug discovery, chemical investigation was carried out on an Indonesian marine sponge P. papyrecea. METHODS: Bioassay-guided fractionation was carried out on its dichloromethane extract. And nine compounds were purified and isolated using HPLC...
October 7, 2016: Medicinal Chemistry
Zeinab A Muhammad, Ghada S Masaret, Mohamed M Amin, Magda A Abdallah, Thoraya A Farghaly
BACKGROUND: Indane-1,3-dione, thiazole, bis-thiazole and rings are very interested moiety in - and analgesic drugs. OBJECTIVE: The goal of this work is to synthesis of new derivatives of bis--1,3,4- to investigate their -, -ulcerogenic and analgesic activities. METHODS: 1,1'-(1,2-phenylene)bis(3-phenylthiourea) (1) reacts with a number of N-aryl arenecarbohydrazonoyl chlorides 2 to give a series of new bis-1,3,4- 4. Also, reaction of bis-thiosemicarbazone of 1,3-indanedione 6 with another type of hydrazonoyl halides namely, N-aryl-2-oxapropanehydrazonoyl chlorides7 and ethyl-(N-arylhydrazono)chloroacetate 8 in dioxane under reflux in the presence of triethylamine give the respective bis-thiazole derivatives 9 and 10, respectively...
September 19, 2016: Medicinal Chemistry
Xiansheng Zhang, Jingwei Wu, Wei Liu, Yuqiang Liu, Yafei Xie, Qian Shang, Zhixing Zhou, Weiren Xu, Lida Tang, Jianwu Wang, Guilong Zhao
BACKGROUND: Gout is the most common inflammatory arthritis, which, if left untreated or inadequately treated, will lead to joint destruction, bone erosion and disability due to the crystal deposition. Uric acid transporter 1 (URAT1) was the promising therapeutic target for urate-lowering therapy. OBJECTIVE: The goal of this work is to understand the structure-activity relationship (SAR) of a potent lesinurad-based hit, sodium 2-((5-bromo-4-((4-cyclopropylnaphth-1-yl)methyl)-4H-1,2,4-triazol-3-yl)thio)acetate (1c), and based on that discover a more potent URAT1 inhibitor...
September 15, 2016: Medicinal Chemistry
Barbara V da Silva, Bianca N M Silva
BACKGROUND: Trypanosomiasis and leishmaniasis cause severe infections in humans and domestic animals in the tropics. Although typical diseases in Latin America, globalization and the migration of infected people has spread these diseases to countries in North America, Asia and Europe. Currently available drugs are not effective in the chronic phase, as well as causing side effects and the development of resistance. RESULTS: Among the chemical groups studied as potential anti-T...
September 9, 2016: Medicinal Chemistry
Jelena Savić, Sanda Dilber, Marina Milenković, Jelena Kotur-Stevuljević, Bojan Marković, Sote Vladimirov, Jasmina Brborić
BACKGROUND: Nonsteriodal anti-inflammatory drugs (NSAIDs) are numerous and widely used for more than 60 years, but there is still a strong need for developing novel selective NSAIDs. The need is justified by the fact that nonselective NSAIDs can produce serious gastric side effects and that some of the selective NSAID are withdrawn due to their cardiotoxic side effects. METHODS: Eight β-hydroxy-β-arylpropanoic acids, which belong to the arylpropanoic acid class of compounds, structurally similar to some nonsteroidal anti-inflammatory drugs (NSAIDs), were docked into 3D catalytic site of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2)...
September 7, 2016: Medicinal Chemistry
Gisela C Muscia, Silvia E Asis, Graciela Y Buldain
BACKGROUND: Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies. OBJECTIVE: In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared Method: A series of styrylquinoline derivatives was prepared from quinaldic acid and a variety of arylbenzaldehydes under eco-friendly conditions via Knoevenagel reaction and trifluoroacetic acid (TFA) as catalyst...
September 1, 2016: Medicinal Chemistry
Michał Antoszczak, Ewa Maj, Natalia Kleczewska, Joanna Wietrzyk, Lech Celewicz, Adam Huczyński
BACKGROUND: Pharmacophore hybridization by bioconjugation, in which two bioactive moieties are covalently linked, is one of the current strategies in drug discovery for the development of new compounds with improved affinity and efficacy relative to those of the parent molecules. Prompted by the idea that cancer cells may be effectively killed by 3'-azido-3'-deoxythymidine (AZT) and salinomycin (SAL) individually, we synthesized hybrids of these compounds. The development of this type of derivatives, which can easily penetrate the lipid-rich cell membranes and then undergo hydrolysis inside the cancer cells, is an important research area...
August 23, 2016: Medicinal Chemistry
Zhi-Yu Wei, Jia-Chun Liu, Wen Zhang, Ya-Ru Li, Chao Li, Chang-Ji Zheng, Hu-Ri Piao
BACKGROUND: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel antimicrobial agents. OBJECTIVE: As a part of our ongoing studies toward the development of novel antibacterial agents, the synthesis and antibacterial activity of a series of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives will be discussed in this study...
August 22, 2016: Medicinal Chemistry
Carlos A Méndez-Cuesta, Miguel Ángel Herrera-Rueda, Sergio Hidalgo-Figueroa, Hugo Tlahuext, Rosa Moo-Puc, Juan Bautista Chale-Dzul, Manuel Chan-Bacab, Benjamín Otto Ortega-Morales, Emanuel Hernández-Núñez, Oscar Méndez-Lucio, José L Medina-Franco, Gabriel Navarrete-Vazquez
BACKGROUND: Propamidine, an antiseptic aromatic diamidine is a toxic compound with potential use as antiprotozoal drug. On the other hand, benzimidazole derivatives have shown excellent antiparasitic effects. We designed hybrid molecules between propamidine and benzimidazole in order to retain the antiprotozoal action, but decreasing the toxic effect of the molecule. Objetive: Design and prepare 12 hybrids from propamidine and benzimidazole for testing their antiparasitic effect over three protozoa: Giardia intestinalis, Trichomonas vaginalis and Leishmania Mexicana, as well as conduct several in silico simulations such as toxicological profile, molecular docking and molecular dynamics in order to understand their potential mode of action...
August 11, 2016: Medicinal Chemistry
Takuji Shoda, Masashi Kato, Takuma Fujisato, Yosuke Demizu, Hideshi Inoue, Mikihiko Naito, Masaaki Kurihara
BACKGROUND: Estrogen receptors (ERs) are an important target for the management of breast cancers. Selective estrogen receptor down-regulators (SERDs) block ER activity, as well as reduce ERa protein levels in cells, and therefore are promising therapeutic agents for the treatment of breast cancers. OBJECTIVE: In order to develop potent SERDs, we prepared tamoxifen and fulvestrant hybrids and evaluated their binding activity and down-regulation of ERa. METHODS: We designed and synthesized tamoxifen derivatives, which had a 4,4,5,5,5-pentafluoropentyl group on the terminal alkyl chain...
August 5, 2016: Medicinal Chemistry
Amara Mumtaz, Sumera Zaib, Fareeha Zahoor, Azhar Nawaz, Aamer Saeed, Amir Waseem, Afsar Khan, Izhar Hussain, Jamshed Iqbal
BACKGROUND: In spite of substantial progress in scientific cognizance and medical technology, still infectious diseases are among the leading cause of morbidity and mortality. Creatinine and Schiff bases are well known for their diverse range of biological activities and thought to be emerging and useful therapeutic target for the treatment of several diseases. METHODS: The present work was aimed to illustrate the influence of substitution of amides and Schiff bases on creatinine and their antimicrobial, antioxidant and anti-urease effectiveness was determined...
August 5, 2016: Medicinal Chemistry
Takuji Shoda, Masashi Kato, Takuma Fujisato, Yosuke Demizu, Hideshi Inoue, Mikihiko Naito, Masaaki Kurihara
BACKGROUND: Estrogen receptors (ERs) are an important target for the management of breast cancers. Selective estrogen receptor down-regulators (SERDs) block ER activity, as well as reduce ERa protein levels in cells, and therefore are promising therapeutic agents for the treatment of breast cancers. OBJECTIVE: In order to develop potent SERDs, we prepared tamoxifen and fulvestrant hybrids and evaluated their binding activity and down-regulation of ERa. METHODS: We designed and synthesized tamoxifen derivatives, which had a 4,4,5,5,5-pentafluoropentyl group on the terminal alkyl chain...
August 5, 2016: Medicinal Chemistry
Khairunnisa Abdul Ghaffar, Nirmal Marasini, Ashwini Kumar Giddam, Michael R Batzloff, Michael F Good, Mariusz Skwarczynski, Istvan Toth
BACKGROUND: Group A streptococcus (GAS) is an exclusively human pathogenic bacteria. A delay in treatment of GAS infection often lead to severe diseases such as rheumatic heart disease which attributes to hundreds of thousands deaths annually. For the past few decades, the quest for a commercial GAS vaccine has been futile. Currently one of the most investigated strategies to develop vaccine against GAS includes the use of conserved epitopes from major virulent factor of GAS, M-protein...
July 19, 2016: Medicinal Chemistry
Patrick-Denis St-Coeur, Marc Cormier, Véronique C LeBlanc, Pier Jr Morin, Mohamed Touaibia
BACKGROUND: Glioblastoma multiforme (GBM) is often associated with a poor survival prognostic for patients. The main reason seems to be the acquired or inherent resistance to the chemotherapeutic agent used to treat the tumor, temozolomide (TMZ). To this day, the most recognized pathway of resistance is the DNA Direct Repair pathway by the mean of the protein O6-methylguanine DNA-methyltransferase (MGMT). OBJECTIVES: To design and synthesize a series of MGMT inhibitors that can sensitize GBM cells to TMZ...
July 10, 2016: Medicinal Chemistry
Silvia Elizondo-Jimenez, Antonio Moreno-Herrera, Rogelio Reyes-Olivares, Edith Dorantes-Gonzalez, Benjamín Nogueda-Torres, Eduardo Alves Gamosa de Oliveira, Nelilma C Romeiro, Lidia Moreira Lima, Isidro Palos, Gildardo Rivera
BACKGROUND: Chagas disease is a public health problem caused by Trypanosoma cruzi. Cruzain is a pharmacological target for designing a new drug against this parasite. Hydrazone and N-acylhydrazone derivatives have been traditionally associated as potential Cruzain inhibitors. Additionally, benzenesulfonyl derivatives show trypanocidal activity. Therefore, in this study, the combination of both structures has been taken into account for drug design. METHODS: Seven benzenesulfonylhydrazone (BS-H) and seven N-propionyl benzenesulfonylhydrazone (BS-NAH) derivatives were synthetized and elucidated by infrared spectroscopy, nuclear magnetic resonance, and elemental analysis...
June 30, 2016: Medicinal Chemistry
Chun-Lung Yuan, Shih-Wei Lin, Meng-Hsuan Cheng
BACKGROUND: According to a review of recent literature, no previous studies have reported the dose-dependent selective inhibition of the antiproliferative activity using colony and sphere formation assays and immunoblotting in human hepatoma cells in response to doxorubicin and mitoxantrone structural analogs such as AM3. OBJECTIVE: We evaluated the anticancer activity of mitoxantrone (MIT) structural analogs 1,5-bis({2-[(2-hydroxyethyl) amino]ethyl}-amino)-anthracene-9,10-dione (AM3) in human hepatoma cells (Huh-7)...
June 22, 2016: Medicinal Chemistry
Rashad Al-Salahi, Hatem A Abuelizz, Rabab El Dib, Mohamed Marzouk
BACKGROUND: The antimicrobial activity of a synthesized series of 28 2-thioxo-benzo[g]quinazolin-4(3H)-one derivatives was evaluated in vitro against five Gram-positive bacteria, including Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus pyogenes. The antibacterial activity was extended to include five Gram-negative bacteria: Pseudomonas aeruginosa, Escherichia coli, Proteus mirabilis, Klebsiella oxytoca and Enterobacter cloacae...
June 9, 2016: Medicinal Chemistry
Luana Paracatu, Maria Luiza Zeraik, Luiza de Carvalho Bertozo, Aloisio de Andrade Bartolomeu, Luiz Carlos da Silva Filho, Luiz Marcos da Fonseca, Valdecir Farias Ximenes
BACKGROUND: Coumarin derivatives as dihydrocoumarins have been reported to have multiple biological activities, such as antioxidant and anti-inflammatory properties. Apocynin (APO), which is a substituted-methoxy-catechol, is the most commonly used inhibitor of the multienzymatic complex NADPH-oxidase. OBJECTIVE: To increase the potency of APO as an NADPH oxidase inhibitor and its antioxidant and anti-inflammatory activities, we synthesized a compound by combining the structural features of a dihydrocoumarin and APO...
June 9, 2016: Medicinal Chemistry
Blanka Klimova, Kamil Kuca, Michal Novotny, Petra Maresova
BACKGROUND: Cystic fibrosis (CF) is an incurable, chronic disease, which causes severe damages to respiratory and digestive tracts. It is the most common genetically inherited disease among caucasians. This disease is caused by defects in CF genes, the so-called mutations in cystic fibrosis transmembrane conductance regulator (CFTR) gene population. At present over 100,000 people suffer from this disease worldwide. OBJECTIVE: The purpose of this review study is to describe the pathophysiology of CF and provide the latest information on its diagnosis and treatment therapies with respect to the improvement of patient's quality of life and emphasis on targeted specialized care...
June 8, 2016: Medicinal Chemistry
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