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Medicinal Chemistry

Chunfang Gan, Liang Liu, Jianguo Cui, Zhiping Liu, Haixin Shi, Qifu Lin, Haibing Sheng, Chunhui Yang, Yanmin Huang
BACKGROUND: The modification of steroidal structure is commonly used to change the biological activity of steroids in medicinal chemistry. Some steroids containing heterocycles exhibit distinct cytotoxicity against various cancer cell lines and have been gotten wide attention over the years by medicinal chemists for drug discovery. METHODS: Using pregnenolone and stigmasterol as starting materials, via different chemical reaction, two series of heterosteroids with side chain of 20- and 22-hydrazone aromatic cycles or heterocycles in their structures were synthesized and characterized by IR, NMR and HRMS...
December 5, 2016: Medicinal Chemistry
Nida Iqbal Siddiqui, Muhammad Ali Versiani, Khurshid Jawaid, Maryam Shafique, Abdul Hameed, Nida Ambreen, Aneela Karim, Khalid Mohammed Khan
: : Background: Pathogenic microbial diseases are now the key virulence in our daily life. Significant research has been carried out in order to trigger the bacterial infections. Amongst the organic molecules, oxazolone and derivatives were found to have excellent bioactivities including antimicrobial activities. METHODS: By keeping in mind the considerable antimicrobial activities of class benzoxazolones, a series of benzoxazolone derivatives 3-16 have been synthesized...
December 5, 2016: Medicinal Chemistry
Chunqi Hu, Jun Li, Wenting Du
BACKGROUND: Biaryl seven-membered lactones (BSLs), the target compounds are a class of bioactive compounds with anti-arrhythmic activity, which also serve as a starting material or structural units for chemical synthesis. OBJECTIVE: To report a simple and efficient procedure for the synthesis of biaryl seven-membered lactones. Method Under microwave, the umpolung reaction was promoted by N-heterocyclic carbenes under oxygen, with anhydrous potassium carbonate as base and with 1,4,7,10,13,16-Hexanoxacyclooctadecane (18-crown-6) as a phase-transfer catalyst...
November 17, 2016: Medicinal Chemistry
Min Wang, Chunjiang Wu, Shan Xu, Yan Zhu, Wei Li, Pengwu Zheng, Wufu Zhu
BACKGROUND: Sorafenib is an important VEGFR2/KDR inhibitors which is widely used for the treatment of cancer. OBJECTIVE: In this paper,two series of sorafenib analogues N-(3-fluoro-4-(pyridin-4-yloxy)phenyl)-4-phenylpicolinamides(13a-k) and N-(3-fluoro-4-(pyridin-4-yloxy)phenyl)-5-phenylpicolinamides (14a-k) were designed and synthesized. METHODS: Their structures were confirmed by various analytical methods, such as 1 H and 13 C NMR, m...
November 17, 2016: Medicinal Chemistry
Zhendong Song, Ping Wang, Shanshan Huang, Changyuan Wang, Ruirui Wang, Liumeng Yang, Yuhong Zhen, Kexin Liu, Yongtang Zheng, Xiaodong Ma
BACKGROUND: Although a number of agents can achieve high response in acquired immunodeficiency syndrome (AIDS) patients, safer and more active HIV inhibitors are still needed for the growing number of patients infected with resistant HIV virus strains. GW678248, is one of the most potent benzophenone derivatives, exhibiting high potency against a panel of HIV-1 virus (wild-type, K103N mutant, Y181C, etc.) at 1 nM/L concentrations. However, the safety issues associated with rash and liver metabolic enzymes ultimately led to discontinue its further development...
November 11, 2016: Medicinal Chemistry
Neha Sharma, Salman Akhtar, Qazi M Sajid Jamal, Mohammad A Kamal, M Kalim A Khan, M Haris Siddiqui, Usman Sayeed
BACKGROUND: Angiogenesis involves the process of sprouting of microvessels from preexisting microvasculature and is held responsible for the growth, malignancy and metastasis of cancer. Heat shock protein Hsp90 has been proven responsible for indirectly inducing multiple pathways leading to angiogenesis and metastasis in cancer. Recent researches shift towards proposing novel phytochemicals as possible antiangiogenic agents. OBJECTIVE: The study aims towards Virtual screening of compounds from Cucurbitaceae family and their Druglikeliness and PreADMET filtering in search of potent lead as Vitexin, targeting Hsp90 and hence restraining angiogenesis...
November 11, 2016: Medicinal Chemistry
Reema Abu Khalaf, Sarah Al-Rawashdeh, Dima Sabbah, Ghassan Abu Sheikha
BACKGROUND: Hyperlipidemia is one of the most common chronic diseases worldwide. Cholesteryl ester transfer protein (CETP) is a hydrophobic glycoprotein that facilitates the transfer of cholesteryl ester from the atheroprotective high-density lipoprotein (HDL) to the proatherogenic low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL). METHODS: In this work, synthesis and characterization of five fluorinated 3-benzylamino benzamides 8a-8c, 13a and 13b that target CETP activity was carried out...
November 4, 2016: Medicinal Chemistry
Burcu Culhaoglu, Asli Capan, Mehmet Boga, Mehmet Ozturk, Turan Ozturk, Gulacti Topcu
BACKGROUND: Flavones, are a class of naturally occuring polyphenolic compounds which have 2-phenylchromen-4-one structure. Various studies showed that flavones have several pharmacological activities such as antioxidant, anti-inflammatory, antimicrobial, cytotoxic, antitumour and antiallergic. In the present study, 3-hydroxyflavones also called flavonols, posessing 4'-dialkylamino moiety were synthesized, and their antioxidant and anticholinesterase activities were investigated by comparison with unmodified 3-hydroxflavone...
November 4, 2016: Medicinal Chemistry
Panagiotis Theodosis-Nobelos, Panos N Kourounakis, Eleni A Rekka
OBJECTIVES: A series of esters and amides, incorporating an antioxidant residue, such as trolox or caffeic acid, and various moieties with different biological activities, were synthesised. RESULTS: The obtained compounds demonstrated considerable anti-inflammatory, radical scavenging and antioxidant action. Thus, they could reduce carrageenan-induced rat paw oedema by 31-60% at 150 μmol/kg and inhibit rat microsomal membrane lipid peroxidation with IC50 values as low as 1...
November 4, 2016: Medicinal Chemistry
Raquel S Amim, Cláudia Pessoa, Maria C S Lourenço, Marcus V N de Souza, Josane A Lessa
BACKGROUND: Schiff bases have been greatly studied in biological field due to their wide range of pharmacological activities, such as antitubercular and antitumour. In the search of novel antitubercular agents, several compounds containing pharmacophoric group of ethambutol have been synthesized and evaluated against mycobacteria species causing tuberculosis. In this work, we investigate whether ethylenediamine, Schiff base as well as nitro group together could contribute to the formation of novel molecules with dual biological activities: antitubercular and anticancer...
November 4, 2016: 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
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