Quinolones

Publication Title: 
Drugs of Today (Barcelona, Spain: 1998)

Cystic fibrosis (CF) is a life-shortening disorder that affects over 30,000 people in the U.S. and 70,000 worldwide. CF is caused by mutations in the CFTR gene, which codes for the cystic fibrosis transmembrane conductance regulator (CFTR) protein. CFTR is a chloride and bicarbonate channel and regulates several ion transporters at the epithelial cell membrane, controlling hydration or ionic composition of epithelial secretions. Management of CF is currently supportive, but recent advances in drug development have focused on therapies that assist mutant CFTR function.

Author(s): 
McPhail, G. L.
Clancy, J. P.
Publication Title: 
Arzneimittel-Forschung

The general pharmacological profile of 7-fluoro-1-methyl-3-(methylsulfonyl)- 4(1H)-quinolone BTS 53 554, CAS 76568-68-8), the main metabolite of a new vasodilator, flosequinan (BTS 49 465), was investigated. 1. The central nervous system: BTS 53 554 at the dose of 30 mg/kg i.v. caused an increase in respiratory rate and a sedation in general behavior in rats. The drug also inhibited acetic acid-induced writhing and slightly decreased normal body temperature in mice. However, the drug at the doses up to 30 mg/kg i.v.

Author(s): 
Fujita, S.
Ikezono, K.
Umezato, M.
Hosoki, E.
Toba, Y.
Ishikawa, M.
Kusunoki, A.
Shintani, S.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Endocytosis is a fundamental process of eukaryotic cells and fulfills numerous functions, most notably, that of macromolecular nutrient uptake. Malaria parasites invade red blood cells and during their intracellular development endocytose large amounts of host cytoplasm for digestion in a specialized lysosomal compartment, the food vacuole. In the present study we have examined the effects of artemisinin and the quinoline drugs chloroquine and mefloquine on endocytosis in Plasmodium falciparum.

Author(s): 
Hoppe, Heinrich C.
van Schalkwyk, Donelly A.
Wiehart, Ursula I. M.
Meredith, Sandra A.
Egan, Joanne
Weber, Brandon W.
Publication Title: 
Malaria Journal

BACKGROUND: Anti-malarial drug resistance in Kenya prompted two drug policy changes within a decade: sulphadoxine-pyrimethamine (SP) replaced chloroquine (CQ) as the first-line anti-malarial in 1998 and artemether-lumefantrine (AL) replaced SP in 2004. Two cross-sectional studies were conducted to monitor changes in the prevalence of molecular markers of drug resistance over the period in which SP was used as the first-line anti-malarial.

Author(s): 
Spalding, Maroya D.
Eyase, Fredrick L.
Akala, Hoseah M.
Bedno, Sheryl A.
Prigge, Sean T.
Coldren, Rodney L.
Moss, William J.
Waters, Norman C.
Publication Title: 
Proceedings of the National Academy of Sciences of the United States of America

There is an urgent need for new antimalarial drugs with novel mechanisms of action to deliver effective control and eradication programs. Parasite resistance to all existing antimalarial classes, including the artemisinins, has been reported during their clinical use. A failure to generate new antimalarials with novel mechanisms of action that circumvent the current resistance challenges will contribute to a resurgence in the disease which would represent a global health emergency.

Author(s): 
Biagini, Giancarlo A.
Fisher, Nicholas
Shone, Alison E.
Mubaraki, Murad A.
Srivastava, Abhishek
Hill, Alisdair
Antoine, Thomas
Warman, Ashley J.
Davies, Jill
Pidathala, Chandrakala
Amewu, Richard K.
Leung, Suet C.
Sharma, Raman
Gibbons, Peter
Hong, David W.
Pacorel, Bénédicte
Lawrenson, Alexandre S.
Charoensutthivarakul, Sitthivut
Taylor, Lee
Berger, Olivier
Mbekeani, Alison
Stocks, Paul A.
Nixon, Gemma L.
Chadwick, James
Hemingway, Janet
Delves, Michael J.
Sinden, Robert E.
Zeeman, Anne-Marie
Kocken, Clemens H. M.
Berry, Neil G.
O'Neill, Paul M.
Ward, Stephen A.
Publication Title: 
Journal of Medicinal Chemistry

The continued proliferation of malaria throughout temperate and tropical regions of the world has promoted a push for more efficacious treatments to combat the disease. Unfortunately, more recent remedies such as artemisinin combination therapies have been rendered less effective due to developing parasite resistance, and new drugs are required that target the parasite in the liver to support the disease elimination efforts.

Author(s): 
Cross, R. Matthew
Flanigan, David L.
Monastyrskyi, Andrii
LaCrue, Alexis N.
Sáenz, Fabián E.
Maignan, Jordany R.
Mutka, Tina S.
White, Karen L.
Shackleford, David M.
Bathurst, Ian
Fronczek, Frank R.
Wojtas, Lukasz
Guida, Wayne C.
Charman, Susan A.
Burrows, Jeremy N.
Kyle, Dennis E.
Manetsch, Roman
Publication Title: 
Malaria Journal

Available anti-malarial tools have over the ten-year period prior to 2012 dramatically reduced the number of fatalities due to malaria from one million to less than six-hundred and thirty thousand. Although fewer people now die from malaria, emerging resistance to the first-line anti-malarial drugs, namely artemisinins in combination with quinolines and arylmethanols, necessitates the urgent development of new anti-malarial drugs to curb the disease. The quinolones are a promising class of compounds, with some demonstrating potent in vitro activity against the malaria parasite.

Author(s): 
Beteck, Richard M.
Smit, Frans J.
Haynes, Richard K.
N'Da, David D.
Publication Title: 
Journal of Environmental Pathology, Toxicology and Oncology: Official Organ of the International Society for Environmental Toxicology and Cancer

Compounds possessing antimutagenic properties (polyphenols, tannins, vitamins, etc.) have been identified in fruits, vegetables, spices, and medicinal plants. Terminalia arjuna (Combretaceae), a tropical woody tree occurring throughout India and known locally as Kumbuk, is a medicinal plant rich in tannins and triterpenes that is used extensively in Ayurvedic medicine as a cardiac tonic. The aim of the present collaborative work was to test six solvent extracts from the bark of Terminalia arjuna for antigenotoxic activity using in vitro short-term tests.

Author(s): 
Scassellati-Sforzolini, G.
Villarini, L. M.
Moretti, L. M.
Marcarelli, L. M.
Pasquini, R.
Fatigoni, C.
Kaur, L. S.
Kumar, S.
Grover, I. S.
Publication Title: 
Food and Chemical Toxicology: An International Journal Published for the British Industrial Biological Research Association

Rubia cordifolia L. (Rubiaceae) is an important medicinal plant used in the Ayurvedic medicinal system. Its use as a traditional therapeutic has been related to the treatment of skin disorders and cancer. Besides its medicinal value, anthraquinones from this plant are used as natural food colourants and as natural hair dyes. Dyes derived from natural sources have emerged as important alternatives to synthetic dyes. Alizarin (1,2-dihydroxyanthraquinone) was isolated and characterized from R. cordifolia L. and evaluated for its antigenotoxic potential against a battery of mutagens viz.

Author(s): 
Kaur, Prabhjit
Chandel, Madhu
Kumar, Subodh
Kumar, Neeraj
Singh, Bikram
Kaur, Satwinderjeet
Publication Title: 
Psychopharmacology

RATIONALE: Dopamine D2-like partial agonists such as aripiprazole have received some attention as potential pharmacotherapies for the treatment of psychostimulant addiction. However, the preclinical evaluations so far have focused on acute effects of aripiprazole. OBJECTIVES: We tested the hypothesis that aripiprazole, both as acute and as chronic treatment, would preferentially decrease cocaine self-administration while sparing behavior maintained by a natural reinforcer, resulting in a shift in the allocation of behavior from cocaine-taking towards the alternative reinforcer.

Author(s): 
Thomsen, Morgane
Fink-Jensen, Anders
Woldbye, David P. D.
Wörtwein, Gitta
Sager, Thomas N.
Holm, Rene
Pepe, Lauren M.
Caine, S. Barak

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