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Future Medicinal Chemistry

Rajesh Radhamanalan, Manikandan Alagumuthu, Narsimaiah Nagaraju
AIM: Due to their effective binding affinity to receptors which are responsible for various diseases, benzimidazoles are often bioactive. Present study intended and carried out to synthesis, characterize and develop benzimidazole-based antiulcer drugs. Materials & methods: Established 8a-l were evaluated for gastric antisecretory/antiulcer properties using freshly prepared H+ -K+ -ATPase from goat fundus mucosa. Molecular docking was carried out to unveil best binding affinities with H+ -K+ -ATPase (protein data bank ID: 2XZB)...
July 18, 2018: Future Medicinal Chemistry
Lúcia Marciel, Mariana Q Mesquita, Rosalina Ferreira, Beatriz Moreira, Maria Graça Pms Neves, Maria Amparo F Faustino, Adelaide Almeida
AIM: Antibiotic resistance is an increasingly serious worldwide problem that needs to be addressed with alternative tools. Antimicrobial photodynamic therapy seems a promising approach but in some cases the synthesis of highly efficient photosensitizers requires laborious processes burdened by extensive chromatographic purifications. In this study, we evaluate the suitability of a formulation (Form-1) containing porphyrins bearing different charges, obtained during the synthesis of the highly efficient photosensitizer 5,10,15-tris(1-methylpyridinium-4-yl)-20-(pentafluorophenyl)porphyrin tri-iodide...
July 18, 2018: Future Medicinal Chemistry
Aladdin M Srour, Siva S Panda, Asmaa M M Salman, May A El-Manawaty, Riham F George, ElSayed M Shalaby, Andrew N Fitch, Nehmedo G Fawzy, Adel S Girgis
AIM: Synthesis of novel bronchodilatory active indole-pyridine conjugates. Results/methodology: Indole-pyridine conjugates (6a-n, 8a-i and 10a-c) were synthesized in a facile pathway through reaction of 2-[(1-alkyl-1H-indol-3-yl)methylene]malononitriles 4a,b with the corresponding ketone-containing compounds (5a-f, 7a-c and 9a,b) in the presence of sodium alkoxide. Single (6l, 8 g) and powder (6k, 8d) x-ray studies supported the structures. RESULTS: Histamine precontracted isolated tracheal rings of guinea pig exhibited the potent bronchodilation properties of 6c (about double-fold potency relative to the standard reference, theophylline)...
July 18, 2018: Future Medicinal Chemistry
Yicheng Mei, Baowei Yang
'Drug promiscuity' refers to a drug that can act on multiple molecular targets, exhibiting similar or different pharmacological effects. Drugs may interact with unwanted targets, leading to off-target effects (one of the main reasons for side effects). Thus, intervention to prevent off-target effects in the early stages of drug discovery could reduce the risk of failure. The conversion between target and off-target effects is important for drug repurposing. Drug repurposing strategies could reduce research and development costs...
July 18, 2018: Future Medicinal Chemistry
Mariangela Biava
No abstract text is available yet for this article.
July 18, 2018: Future Medicinal Chemistry
Lucas Vb Hoelz, Felipe A Calil, Maria C Nonato, Luiz Cs Pinheiro, Nubia Boechat
Malaria remains one of the most lethal infectious diseases worldwide, and the most severe form is caused by Plasmodium falciparum. In recent decades, the major challenge to treatment of this disease has been the ability of the protozoan parasite to develop resistance to the drugs that are currently in use. Among P. falciparum enzymes, P. falciparum dihydroorotate dehydrogenase has been identified as an important target in drug discovery. Interference with the activity of this enzyme inhibits de novo pyrimidine biosynthesis and consequently prevents malarial infection...
July 18, 2018: Future Medicinal Chemistry
Guohui Sun, Lijiao Zhao, Rugang Zhong, Yongzhen Peng
The DNA repair protein, O6 -methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6 -alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exhibited potential MGMT inhibitory activities. Although they were nontoxic alone, they also inhibited MGMT in normal tissues, thereby enhancing the side effects of chemotherapy. Therefore, strategies for tumor-specific MGMT inhibition have been proposed, including local drug delivery and tumor-activated prodrugs...
July 13, 2018: Future Medicinal Chemistry
Apeng Wang, Wenyan Li, Bin Wang, Kai Lv, Hongjian Wang, Mingliang Liu, Huiyuan Guo, Yu Lu
AIM: Tuberculosis (TB) is one of the world's deadliest chronic infectious diseases caused mainly by Mycobacterium tuberculosis (MTB). Many nitrofuran derivatives were found to possess promising anti-TB potential and have been widely studied. In our previous study, we discovered diazaspiro-nitrofuran IMB1701-1702 as potent anti-TB agents. METHODOLOGY: We report herein a series of nitrofuranyl methyl N-heterocycles based on IMB1701-1702. Results reveal that most of them show potent activity (minimum inhibitory concentration: <0...
July 11, 2018: Future Medicinal Chemistry
Chérif F Matta, Lou Massa
No abstract text is available yet for this article.
July 11, 2018: Future Medicinal Chemistry
Chérif F Matta, Michael C Hutter
No abstract text is available yet for this article.
July 11, 2018: Future Medicinal Chemistry
Shabir Ahmad Ganai, Zeenat Farooq, Shahid Banday, Mohammad Altaf
AIM: Aberrant activity of class I histone deacetylases (HDACs) has strong implications for various cancers. Targeting these HDACs with synthetic HDAC inhibitors has shown significant side effects such as atrial fibrillation and QT prolongation emphasizing the need of natural inhibitors as substitutes to synthetic ones. RESULTS: The binding propensity of the two plant-derived inhibitors apigenin and luteolin towards class I HDAC isoforms was checked using extra-precision molecular docking and implicit solvation MMGBSA...
July 11, 2018: Future Medicinal Chemistry
Ze Li, Fei Huang, Jianhui Wu, Lin Gui, Xiaoyi Zhang, Yaonan Wang, Shurui Zhao, Xiaozhen Wang, Shiqi Peng, Ming Zhao
AIM: The modification of platelet inhibitor to enhance its targeting capacity toward platelets is of clinical importance. Thus, (1R, 3S)-1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid (MTCA), a platelet inhibitor, was modified with Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val (KKV), platelet targeting peptide, to form MTCA-KKV. MATERIALS & METHODS: MTCA and MTCA-KKV were synthesized to identify the effect of KKV modification on MTCA and platelets. RESULTS: Atomic force microscopy imaged MTCA-KKV effectively accumulated on activated platelets...
July 5, 2018: Future Medicinal Chemistry
Jürgen Bajorath
No abstract text is available yet for this article.
July 3, 2018: Future Medicinal Chemistry
Jelena Melesina, Lucas Praetorius, Conrad V Simoben, Dina Robaa, Wolfgang Sippl
For two decades, a classical pharmacophore model comprising a zinc binding group, a linker and a cap group, has been used for the development of histone deacetylase (HDAC) inhibitors. However, some of the recently reported selective HDAC inhibitors targeting additional, usually subtype specific, cavities in the binding pocket show supplementary features which do not fit this classical pharmacophore. We, therefore, propose an extended pharmacophore model, which can describe almost all currently known HDAC inhibitors...
July 3, 2018: Future Medicinal Chemistry
J B Brown
No abstract text is available yet for this article.
July 3, 2018: Future Medicinal Chemistry
Ruijuan Wang, Xiaoping Ma, Shan Su, Yanjun Liu
AIM: We aimed to investigate the effect of triptolide on cisplatin resistance in ovarian cancer cell lines. METHODS: The apoptosis of ovarian cancer cell lines A2780 and A2780/CP70 was determined by flow cytometry. Protein expression levels of  Hexokinase 2 (HK2) were detected by western blot. Possible mRNAs which target HK 2 expression were predicted through online tools miRbase. RESULTS: Triptolide-promoted cell apoptosis of cisplatin-resistant ovarian cancer cell line A2780/CP70...
July 3, 2018: Future Medicinal Chemistry
John Bo Mitchell
No abstract text is available yet for this article.
July 3, 2018: Future Medicinal Chemistry
Carmen Abate, Mauro Niso, Francesco Berardi
Identification of sigma-2 receptor (sig-2R) has been controversial. Nevertheless, interest in sig-2R is high for its overexpression in tumors and potentials in oncology. Additionally, sig-2R antagonists inhibit Aβ binding at neurons, blocking the cognitive impairments of Alzheimer's disease. The most representative classes of sig-2R ligands are herein treated with focus on compounds that served to study sig-2R biology and to produce sig-2R: fluorescent ligands; multifunctional anticancer agents; and targeting nanoparticles...
July 3, 2018: Future Medicinal Chemistry
Shaimaa A Moussa, Essam Eldin A Osman, Nahed M Eid, Sahar M Abou-Seri, Samir M El Moghazy
AIM: Discovery of novel series of colchicine binding site inhibitors (CBSIs). MATERIALS & METHODS: Isoxazoline 3a-d, pyrazoline 4a-b, 7a-f and 8a-f, cyclohexenone 9a-b and 10a-b or pyridine derivatives 11a-b were synthesized and evaluated for their inhibition of tubulin polymerization and cytotoxicity. Most of the compounds displayed potent to moderate antitumor activity against leukemia SR cell line.7c, 7e and 11a were more potent than colchicine with IC50 of 0...
July 3, 2018: Future Medicinal Chemistry
Yih Ching Ong, Lukasz Kedzierski, Philip C Andrews
Even after 70 years, pentavalent antimonials sodium stibogluconate and meglumine antimoniate remain the most important and cost-effective antileishmanial drugs. However, the drugs cannot be delivered orally and treatment involves intravascular or intramuscular injections for 28 days under strict medical monitoring due to the toxicity of Sb(III). The main alternatives, amphotericin B, pentamidine and miltefosine, are expensive and not without their own problems. Bismuth sits below antimony in the periodic table and is considered to be relatively nontoxic to humans while being capable of providing powerful antimicrobial activity...
July 2, 2018: Future Medicinal Chemistry
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