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Medicinal Chemistry

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https://www.readbyqxmd.com/read/28067167/6-benzothiazolyl-ureas-thioureas-and-guanidines-are-potent-inhibitors-of-abad-17%C3%AE-hsd10-and-potential-drugs-for-alzheimer-s-disease-treatment-design-synthesis-and-in-vitro-evaluation
#1
Ondrej Benek, Lukas Hroch, Laura Aitken, Rafael Dolezal, Patrick Guest, Marketa Benkova, Ondrej Soukup, Karel Musil, Kamil Kuca, Terry K Smith, Frank Gunn-Moore, Kamil Musilek
BACKGROUND: The mitochondrial enzyme amyloid beta-binding alcohol dehydrogenase (ABAD) also known as 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) has been connected with the pathogenesis of Alzheimer's disease (AD). ABAD/ 17β-HSD10 is a binding site for the amyloid-beta peptide (Aβ) inside the mitochondrial matrix where it exacerbates Aβ toxicity. Interaction between these two proteins triggers a series of events leading to mitochondrial dysfunction as seen in AD. METHODS: As ABAD's enzymatic activity is required for mediating Aβ toxicity, its inhibition presents a promising strategy for AD treatment...
January 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031019/naphthyridines-with-antiviral-activity-a-review
#2
Inder Pal Singh, Sanjay Kumar, Shiv Gupta
BACKGROUND: Naphthyridine scaffold is an important pharmacophore in compounds which have shown various biological activities like antiviral, antimicrobial, anticancer, anti-inflammatory and analgesic etc. This scaffold is also reported to exhibit activity against HIV, HCMV, HSV, HPV and HCV. Antiviral activity displayed by many naphthyridine analogs is in nM range. Only few review articles are available in literature which describe about various biological activities of naphthyridines, but there is no comprehensive compilation particularly for antiviral activities...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031018/titanocenes-as-anticancer-agents-recent-insights
#3
Hana Skoupilova, Roman Hrstka, Martin Bartosik
BACKGROUND: Enormous success of antitumor agent cisplatin initiated interest in other organometallic complexes. A subclass of organometallic compounds termed metallocenes, characterized by a transition metal central atom (M) bound to cyclopentadienide (Cp-/[C5H5]-) ligands with the basic formula Cp2M, has gained increasing interest as promising anticancer agents. OBJECTIVES: This review is aimed at a progress in the development of organometallic titanium-based compounds focusing primarily on the evaluation of their cytotoxic activity and mechanism of action in relation to potential utilization as anticancer drugs...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28031017/nitric-oxide-signaling-and-the-cross-talk-with-prostanoids-pathways-in-vascular-system
#4
Bruno R Silva, Tiago D Paula, Michele Paulo, Lusiane M Bendhack
BACKGROUND: This review provides an overview of the cellular signaling of nitric oxide (NO) and prostanoids in vascular cells and the possible cross talk between their pathways, mainly in hypertension, since the imbalance of these two systems has been attributed to development of some cardiovascular diseases. It also deals with the modulation of vasodilation induced by NO donors. NO is a well-known second messenger involved in many cellular functions. CONCLUSION: In the vascular system, the NO produced by endothelial NO-synthase (eNOS) or released by NO donors acts in vascular smooth muscle cells, the binding of NO to Fe2+-heme of soluble guanylyl-cyclase (sGC) activates sGC and the production of cyclic guanosine-3-5-monophosphate (cGMP)...
December 28, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/28000551/antimicrobial-evaluation-of-5-substituted-aryl-1h-tetrazoles
#5
Liana Feinn, Joshua Dudley, Adiel Coca, Elizabeth Lewis Roberts
BACKGROUND: Tetrazole derivatives such as 1-substituted dinitrobenzyl tetrazoles and their oxa and selanyl analogs have previously been studied against drug-susceptible and multidrug-resistant mycobacteria. In addition, other tetrazole derivatives have been shown to inhibit CTX-M class A b-lactamases. OBJECTIVE: To study the antibacterial activity of 5-substituted aryl 1H-tetrazole derivatives. METHODS: The antibacterial activity of several known 5-substituted aryl 1H-tetrazole derivatives was evaluated against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa...
December 20, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27991400/isolation-of-chemical-constituents-of-centaurea-virgata-lam-and-xanthine-oxidase-inhibitory-activity-of-the-plant-extract-and-compounds
#6
Burcu S Tuzun, Zsuzsanna Hajdu, Orsolya Orban-Gyapai, Zoltan P Zomborszki, Nikoletta Jedlinszki, Peter Forgo, Bijen Kıvcak, Judit Hohmann
BACKGROUND: Centaurea virgata Lam. is a species widely used in the traditional medicine in Turkey for the treatment of diabetes, allergy and gastric ulcers. The rationale of its use in the therapy has not been studied previously, therefore the present work aimed at the chemical-pharmacological evaluation of the plant. OBJECTIVE: The xanthine oxidase (XO) inhibitory activity of the MeOH extract and its subextracts (n-hexane, CHCl3 and remaining MeOH-H2O) prepared from C...
December 19, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27978787/synthesis-and-antiproliferative-activity-of-new-pyrazolo-3-4-c-pyridines
#7
Efthymios-Spyridon Gavriil, Nikolaos Lougiakis, Nicole Pouli, Panagiotis Marakos, Alexios-Leandros Skaltsounis, Sangkil Nam, Richard Jove, David Horne, Katerina Gioti, Harris Pratsinis, Dimitris Kletsas, Roxane Tenta
BACKGROUND: Several pyrazolopyridines possess promising pharmacological activities, mainly attributed to their antagonistic nature towards the natural purines in many biological processes. Cytotoxicity and anticancer potential of this class of compounds is mainly related to induction of apoptotic cell death and inhibition of protein kinases. OBJECTIVES: This prompted us to design, synthesize and study the antiproliferative activity of a number of new 3,7-disubstituted pyrazolo[3,4-c] pyridines...
December 13, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27924728/synthesis-and-immunosuppressive-activity-of-new-mycophenolic-acid-derivatives
#8
Karina Pereira Barbieri, Lucas Dos Reis Ercolin, Thierry Louat, Marisa Campos Polesi, Chung Man Chin, Iracilda Carlos Zeppone, Jean Leandro Dos Santos
BACKGROUND: Immunosuppressive drugs are widely used to prevent and treat allograft rejection and autoimmune diseases. Mycophenolic acid (MPA) and its derivatives are currently one of the most prescribed immunosuppressive drugs; however, metabolic drawbacks and variable inter- and intrapatient responses limit its use. OBJECTIVE: In order to find out new safe and effective immunosuppressive compounds we report here the synthesis and pharmacological evaluation of hybrid MPA derivatives containing the thalidomide/phthalimide subunits...
December 7, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27917709/synthesis-of-some-steroidal-derivatives-with-side-chain-of-20-and-22-hydrazone-aromatic-heterocycles-and-their-antiproliferative-acitivity
#9
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
https://www.readbyqxmd.com/read/27917708/synthesis-spectroscopic-characterization-and-antimicrobial-activities-of-benzoxazolone-derivatives
#10
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
https://www.readbyqxmd.com/read/27855596/a-microwave-promoted-assisted-method-for-rapid-prepararation-of-biaryl-seven-membered-lactones
#11
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
https://www.readbyqxmd.com/read/27855595/synthesis-biological-evaluation-and-docking-studies-of-sorafenib-derivatives-n-3-fluoro-4-pyridin-4-yloxy-phenyl-4-5-phenylpicolinamides
#12
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
https://www.readbyqxmd.com/read/27834135/synthesis-and-biological-evaluation-of-benzophenone-derivatives-as-potential-hiv-1-inhibitors
#13
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
https://www.readbyqxmd.com/read/27834134/elucidation-of-antiangiogenic-potential-of-vitexin-obtained-from-cucumis-sativus-targeting-hsp90-protein-a-novel-multipathway-targeted-approach-to-restrain-angiogenic-phenomena
#14
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
https://www.readbyqxmd.com/read/27823564/molecular-docking-and-pharmacophore-modeling-studies-of-fluorinated-benzamides-as-potential-cetp-inhibitors
#15
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
https://www.readbyqxmd.com/read/27823563/antioxidant-and-anticholinesterase-activities-of-some-dialkylamino-substituted-3-hydroxyflavone-derivatives
#16
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
https://www.readbyqxmd.com/read/27823562/anti-inflammatory-and-hypolipidemic-effect-of-novel-conjugates-with-trolox-and-other-antioxidant-acids
#17
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
https://www.readbyqxmd.com/read/27823561/synthesis-antitubercular-and-anticancer-activities-of-p-nitrophenylethylenediamine-derived-schiff-bases
#18
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
https://www.readbyqxmd.com/read/27748181/gastrointestinal-motility-and-acute-toxicity-of-pistagremic-acid-isolated-from-the-galls-of-pistacia-integerrima
#19
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
https://www.readbyqxmd.com/read/27748180/cytotoxic-phyllactone-analogs-from-the-marine-sponge-phyllospongia-papyrecea
#20
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
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