Results 21 to 30 of about 3,116 (182)

Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. [PDF]

, 2015
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties ...
Allwood, Daniel M, Battilocchio, Claudio, Blakemore, David C, Fish, Paul V, Jenkinson, Stephen, Jessiman, Alan S, Ley, Steven V, McMurray, Gordon, Moore, Dianna E, Rouquet, Guy, Spain, Malcolm, Storer, R Ian   +11 more
core   +4 more sources

Fe‐Catalyzed α‐C(sp3)−H Amination of N‐Heterocycles

Angewandte Chemie, Volume 137, Issue 5, January 27, 2025.
An iron(II)‐catalyzed α‐selective C−H amination of N‐heterocycles is reported. It employs the N‐heterocycle as the limiting reagent and presumably involves the formation of a reactive Fe‐nitrene/imidyl radical species. This operationally simple method is amenable to the late‐stage functionalization of natural products and APIs.
Andrea Geraci, Olivier Baudoin
wiley   +2 more sources

Synthesis and study of biological activity of tetrahydro-1H-[3]-benzazepines [PDF]

, 2017
The 3-Benzazepines are an important class of compounds in drug discovery due to their biological activity such as analgesic, antihypertensive or anticancer properties as well as dopaminergic or antidopaminergic activity. In particular, the tetrahydro-1H-[
Díaz, Amelia, Lucena-Serrano, Ana, Lucena-Serrano, Cristina, López-Romero, Juan Manuel, Valpuesta-Fernandez, Maria   +4 more
core  

Metal‐Catalyzed C(sp2)–H Bond Functionalization of Indolinone‐ and Indanone‐Type Chemical Platforms En Route Toward Late‐Stage Functionalization

Advanced Synthesis &Catalysis, Volume 368, Issue 8, 15 April 2026.
An in‐depth survey dealing with the aromatic C—H bond functionalization of biologically‐relevant scaffolds featuring the indolinone and indanone core is discussed as they are unique aromatic scaffolds that are 1,2‐doubly fused with small five‐membered rings.
Vanessa Delahaye, Sylvie Dérien, Mathieu Achard, Rafael Gramage‐Doria   +3 more
wiley   +1 more source

Synthesis of bioactive compounds. Studies of their attachment to nanoparticles [PDF]

, 2017
The 1-aryl tetrahydroisoquinolines have attracted great attention in medicinal chemistry due to their biological activity. These compounds present antitumor, anti-HIV and antibacterial activities.
Díaz, Amelia, Lucena-Serrano, Ana, Lucena-Serrano, Cristina, López-Romero, Juan Manuel, Valpuesta-Fernandez, Maria   +4 more
core  

Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. [PDF]

, 2016
Notch is a key player in various developmental processes during the embryonic stage as well as in regulating tissue homeostasis, cell differentiation, and stem cell maintenance in adult life.
Dela Golshayan, Lucienne Juillerat-Jeanneret, Massard C., Müllberg J., Okada H., Rajesh Kumar, Shawber C.   +6 more
core   +1 more source

Research on synthesis of microwave‐assisted heterocyclic compounds with eco‐friendly solvents and transition metals via C–H activation

Bulletin of the Korean Chemical Society, Volume 47, Issue 4, Page 384-395, April 2026.
This review summarizes microwave‐assisted transition‐metal catalysis for constructing N‐ and O‐heterocycles, highlighting rapid C–H and pre‐activated C–X activation, improved selectivity, and green synthetic efficiency. Abstract Microwave‐assisted organic synthesis provides a rapid and sustainable platform for synthesizing various heterocycles ...
Woo‐Jin Park, Ye Ri Han, Hyejeong Lee
wiley   +1 more source

Comparative study of dopaminergic activity of tetrahydro-1H-[3]-benzazepines and their precursors [PDF]

, 2016
The discovery of the tetrahydro-1H-[3]-benzazepine SCH23390 [1], represented one of the most important advances in the study of dopaminergic receptors due to their behavior as a selective D1 receptor antagonist.
Contreras-Cáceres, Rafael, Díaz, Amelia, Lucena-Serrano, Cristina, López-Romero, Juan Manuel, Rivera-Ramirez, Alicia, Valpuesta-Fernandez, Maria   +5 more
core  

D1-like receptor activation improves PCP-induced cognitive deficits in animal models: Implications for mechanisms of improved cognitive function in schizophrenia [PDF]

, 2009
YesPhencyclidine (PCP) produces cognitive deficits of relevance to schizophrenia in animal models. The aim was to investigate the efficacy of the D1-like receptor agonist, SKF-38393, to improve PCPinduced deficits in the novel object recognition (NOR ...
Abdul-Monim, Abdul-Monim, Abdul-Monim, Amico, Apud, Arnsten, Benes, Benes, Briggs, Brown, Buchanan, Cahill, Castner, Ciliax, Creese, Davis, Dawson, Finger, Fletcher, Fletcher, George, Goldman-Rakic, Goldman-Rakic, Grace, Granon, Gray, Grayson, Grayson, Green, Guillin, Hagan, Hagger, Harvey, Haut, Hersi, Hirvonen, Ichikawa, Idris, Javitt, Jentsch, Jentsch, Jentsch, Joanna C. Neill, Kashima, Kebabian, Keefe, Kolb, Lahti, Lawler, Levey, Lidow, Lieberman, Marder, Marie L. Woolley, McAlonan, McLean, McLean, Meador-Woodruff, Meltzer, Meunier, Mu, Murray, Nagi F. Idris, Neill, Neill, Neumeyer, Okubo, Pantelis, Qandil, Rossi, Samantha L. McLean, Sawaguchi, Seeman, Siuciak, Snigdha, Snigdha, Snigdha, Snigdha, Spano, Steele, Sutcliffe, Sutcliffe, Tait, Tunbridge, Vincent   +84 more
core   +1 more source

Sulfur Ylides in Skeletal‐Editing—Ring Expansion Reactions

Helvetica Chimica Acta, Volume 109, Issue 3, March 2026.
Sulfur ylides (S‐ylides) are emergent diazo surrogates that enable skeletal editing and ring expansion with safer handling and broad functional group tolerance. This perspective covers pioneer works and highlights recent advances in the field, while outlining key challenges and future directions that may redefine the role of S‐ylides in modern ...
Arsala Kamal, Olaf Tjabben, Ana Matošević, Olga García Mancheño   +3 more
wiley   +1 more source