Results 351 to 360 of about 2,712,589 (407)

Synthesis, Antimycobacterial Activity and Computational Insight of novel 1,4‐Benzoxazin‐2‐one Derivatives as Promising Candidates Against Multidrug‐Resistant M. tuberculosis

ChemMedChem, Accepted Article.
To search for new antitubercular agents, we have designed, synthesized, and evaluated a series of 1,4‐benzoxazinone‐based compounds. These molecules showed potent antimycobacterial activity, with MIC between 2 and 8 μg/mL. This interesting profile included activity against several drug‐resistant strains and minimal cytotoxicity against mammalian Vero ...
Daniele Zampieri, Maria Grazia Mamolo, Emanuele Carosati, Diletta Pasin, Alessandro De Logu, Gianluigi Cabiddu, Marko Jukic   +6 more
wiley   +1 more source

Hybrid Molecules as Efficient Drugs against Multidrug‐Resistant Malaria Parasites

ChemMedChem, EarlyView.
Among hybrid molecules currently developed as antimalarial drug candidates, emoquine‐1 exhibits high activity against all the multidrug‐resistant Plasmodium strains tested up to now, including artemisinin‐resistant quiescent parasites, critical parameters for promising antimalarial drugs. It is also curative in mouse malaria.
Anne Robert, Lucie Paloque, Jean‐Michel Augereau, Flore Nardella, Michel Nguyen, Bernard Meunier, Françoise Benoit‐Vical   +6 more
wiley   +1 more source

Synthesis and Biological Evaluation of Bicyclic Pyrazolines with Promising Antimicrobial Activities

ChemMedChem, EarlyView.
Continuous flow technology is exploited for the generation of bicyclic pyrazolines via photo‐click reactions. These heterocyclic species contain a valuable 3D scaffold along with a polar succinimide moiety. Subsequent antimicrobial testing reveals that halogenated moieties such as chlorine atoms and trifluoromethoxy groups enhance the potency of these ...
Debora Caviglia, Anna Maria Schito, Susanna Penco, Chiara Brullo, Marcus Baumann   +4 more
wiley   +1 more source

First‐in‐Human Phase 1 Study to Evaluate the Clinical Pharmacology Properties of RBN‐3143, a Novel Inhibitor of Mono‐Adenosine Diphosphate Ribosyltransferase‐PARP14

Clinical Pharmacology in Drug Development, EarlyView.
Abstract RBN‐3143 is an inhibitor of PARP14 in development for inflammatory diseases. Multiple assessments were conducted to evaluate the clinical pharmacology properties of RBN‐3134. A randomized, double‐blind, placebo‐controlled study assigned healthy volunteers (HVs) to single ascending doses (SADs) (25‐1000 mg) or multiple ascending doses (MADs ...
Thomas M. Polasek, Alexandra Cole, Viviana Bozón, Erika Manyak, Jonathan Novak, Barbara Yang, Briohny A. Johnston, Sudha Parasuraman, Kushal J. Paneliya, Virna Schuck   +9 more
wiley   +1 more source

EXERCISE EFFECTS ON MUSCLE GLUCOSE UPTAKE AND INSULIN ACTION [PDF]

, 2008
Derave, Wim
core   +1 more source

Antihypertensive Effect of New Agonist of Adenosine Receptor in Spontaneously Hypertensive Rats. [PDF]

Arq Bras Cardiol
de Souza Rocha B, Silva JSD, Pedreira JGB, Montagnoli TL, Barreiro EJ, Zapata-Sudo G.   +5 more
europepmc   +1 more source

Adenosine and Adenosine Receptors [PDF]

American Journal of Respiratory Cell and Molecular Biology, 1990
In the last decade, there has been renewed interest in extracellular signaling by adenosine and adenine nucleotides. The potent cardiovascular effects of these agents were originally described by Drury and Szent-Gy6rgyi in 1929 (1). This report was followed by a flurry of interest in the use of adenosine as an antihypertensive agent, which subsided ...
openaire   +2 more sources

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Adenosine and adenosine receptors in colorectal cancer

International Immunopharmacology, 2020
CD39 (nucleoside triphosphate diphosphohydrolase) and Ecto-5-nucleotidase (CD73) have been recognized as important factors mediating various pathological and physiological responses in the tumor microenvironment. Elevated expression of CD73 and CD39 is correlated with the over-production of adenosine in the tumor region.
A.V. Sevbitov, Makwan Peydaveisi, Ali Masjedi, Farnaz Hajizadeh, Sima Heydarzedeh Asl, Farhad Jadidi-Niaragh, Ghasem Ghalamfarsa, Fariba Karoon Kiani   +7 more
openaire   +2 more sources