Results 81 to 90 of about 17,991 (268)

Further Structure‐Activity Relationship of G Protein‐Gated Inwardly Rectifying Potassium Channels 1/2 Activators: Synthesis and Biological Characterization of In Vitro Tool Compounds

ChemMedChem, EarlyView.
Work presented here details the design and characterize novel G protein‐gated inwardly rectifying potassium channels (GIRK)1/2 activators. A new 4,4‐difluorocyclohexylpyrazole have been identified that confers improved potency and selectivity for GIRK1/2 versus GIRK1/4.
Sumaiya Nahid, Fahad Imtiaz Rahman, Yu Du, Brittany D. Spitznagel, Sandeep K. Singh, Yashpal S. Chhonker, Daryl J. Murry, C. David Weaver, Corey R. Hopkins   +8 more
wiley   +1 more source

Consecutive hydrazino-Ugi-azide reactions: synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles

Beilstein Journal of Organic Chemistry, 2017
Isocyanide-based multicomponent reactions (IMCRs) allow the construction of relatively complex molecules through a one-pot synthesis. The combination of IMCRs in a consecutive or sequential fashion further extends the complexity of the molecules obtained.
Angélica de Fátima S. Barreto, Veronica Alves dos Santos, Carlos Kleber Z. Andrade   +2 more
doaj   +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

In Vitro Studies of Chromone-Tetrazoles against Pathogenic Protozoa, Bacteria, and Fungi

Molecules, 2015
In vitro studies to fourteen previously synthesized chromone-tetrazoles and four novel fluorine-containing analogs were conducted against pathogenic protozoan (Entamoeba histolytica), pathogenic bacteria (Pseudomonas aeruginosa, and Staphylococcus aureus)
Pedro A. Cano, Alejandro Islas-Jácome, Ángeles Rangel-Serrano, Fernando Anaya-Velázquez, Felipe Padilla-Vaca, Elías Trujillo-Esquivel, Patricia Ponce-Noyola, Antonio Martínez-Richa, Rocío Gámez-Montaño   +8 more
doaj   +1 more source

Deferasirox Derivatives as Inhibitors of Kallikrein‐Related Peptidases Associated to Neurodegenerative Diseases

ChemMedChem, EarlyView.
Dysregulated proteolysis mediated by kallikrein‐related peptidases (KLKs) and iron overload are involved in the progression of neurodegenerative diseases. Deferasirox, an clinically‐approved iron chelator, and its newly synthesized derivatives have been identified as inhibitors of major central nervous system KLKs with low cytotoxicity and effective ...
Rilès Boumali, Elodie David, Nancy Chaaya, Morane Lucas, Sabrina Aït Amiri, Valérie Lefort, Anthony Nina‐Diogo, Michèle Salmain, Isabelle Petropoulos, Vincent Corcé, Chahrazade El Amri, Candice Botuha   +11 more
wiley   +1 more source

Total Synthesis of Ectocarpin A

European Journal of Organic Chemistry, EarlyView.
A fully enantioselective total synthesis of ectocarpin A, a new oxylipin, has been achieved in 12 steps starting from tetrahydro‐1H‐cyclopentafuranone. Key steps include the formation of the chiral core, diastereoselective epoxidation, enzymatic desymmetrization of a 1,4‐diol, epimerization, and strategic Wittig and Julia‐Kocienski olefinations to ...
Alexandre Guy, Thierry Durand, Camille Oger   +2 more
wiley   +1 more source

Silica Sulfuric Acid as an Efficient Heterogeneous Catalyst for the Solvent-Free Synthesis of 1-Substituted 1H-1,2,3,4-Tetrazoles

Journal of Chemistry, 2013
Silica sulfuric acid (SSA) was found to be an efficient heterogeneous catalyst for the synthesis of 1-substituted 1H-1,2,3,4-tetrazoles from the reaction of primary amines with triethyl orthoformate and sodium azide under thermal and solvent-free ...
Davood Habibi, Hiva Nabavi, Mahmoud Nasrollahzadeh   +2 more
doaj   +1 more source

Tetrazoles of manno- and rhamno- furanoses

Tetrahedron, 1999
Abstract The synthesis of [3.3.0] bicyclic tetrazoles derived from D-manno and D-rhamnofuranose starting from D-mannose, and of L-rhamnofuranose starting from L-rhamnose is described. The key step in the formation of all three examples of this novel class of sugar mimics is an intramolecular [1,3]-dipolar cycloaddition of azide and nitrile moieties.
Benjamin G. Davis, Benjamin G. Davis, C. F. C. Smith, George W. J. Fleet, Alison A. Watson, Robert J. Nash   +5 more
openaire   +4 more sources

Real‐world effectiveness and tolerability of cenobamate in drug‐resistant epilepsy: A retrospective analysis of the patients included into the Early Access Programs (EAP) in Germany, France, and United Kingdom

Epilepsia Open, EarlyView.
Abstract Objective Investigate real‐world outcomes in drug‐resistant epilepsy (DRE) patients treated with cenobamate as adjunctive treatment to other antiseizure medications (ASMs) within the Early Access Programs (EAP) in Germany, France, and the United Kingdom.
Sylvain Rheims, Bernhard J. Steinhoff, Edouard Hirsch, Felix Rosenow, Arnaud Biraben, Rhys Thomas, Alessandro Lovera, Paola Lipone, Alessandro Comandini, Caroline Benoist, Elena Alvarez Baron, John Paul Leach, Karthinathan Thangavelu, Agnese Cattaneo   +13 more
wiley   +1 more source

Application of Ferulic Acid to Alleviate Chilling Injury of Banana Fruit by Regulating Redox, Phenylpropanoid, and Energy Metabolism

Food Frontiers, EarlyView.
This study investigated the effect of ferulic acid (FA) on the cold tolerance of banana fruit under 6°C‐storage for 7 days. In comparison with control, 3 mM FA treatment significantly alleviated chilling symptoms of banana fruit by enhancing phenylpropanoid metabolism and maintaining redox and energy homeostasis. ABSTRACT Banana fruit is susceptible to
Yu Hou, Min Gou, Zhengke Zhang, Lanhuan Meng, Lisha Zhu, Xiangbin Xu, Taotao Li, Yueming Jiang, Jianbo Xiao, Jiali Yang   +9 more
wiley   +1 more source