Results 81 to 90 of about 7,109 (211)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Engineering of 2‐ketoacid Decarboxylases for Production of Isobutanol and Other Fusel Alcohols in Saccharomyces cerevisiae

Biotechnology and Bioengineering, Volume 123, Issue 4, Page 1036-1049, April 2026.
ABSTRACT Isobutanol is a fusel alcohol that can be produced microbially for use as a biofuel or upgraded into sustainable aviation fuel (SAF). A key enzyme in the isobutanol biosynthetic pathway is 2‐ketoacid decarboxylase (KDC), which irreversibly decarboxylates 2‐ketoisovalerate (KIV) to yield isobutyraldehyde.
Joshua J. Dietrich, Maelia Dziedzic, Jia Sun, Sri Harsha Adusumilli, Carla Gonçalves, Chris Todd Hittinger, Brian F. Pfleger   +6 more
wiley   +1 more source

Synthesis of Novel Nitro-substituted Triaryl Pyrazole Derivatives as Potential Estrogen Receptor Ligands

Molecules, 2007
Novel tetrasubstituted pyrazole derivatives bearing a nitro substituent on their A-phenol ring were synthesized and their binding affinity towards the estrogen receptor (ER) subtypes ERα and ERβ was determined.
Serkos A Haroutounian, Prokopios Magiatis, Konstantinos M Kasiotis, Fotini Naoum   +3 more
doaj   +1 more source

Preparation and Physicochemical Characterization of Water-Soluble Pyrazole-Based Nanoparticles by Dendrimer Encapsulation of an Insoluble Bioactive Pyrazole Derivative. [PDF]

Nanomaterials (Basel), 2021
Alfei S, Brullo C, Caviglia D, Zuccari G.   +3 more
europepmc   +1 more source

Pravastatin Corrects Endothelial Dysfunction in Ex Vivo Uterine Radial Arteries in Preeclampsia

Acta Physiologica, Volume 242, Issue 4, April 2026.
ABSTRACT Aim Endothelium‐dependent relaxation in isolated uterine radial arteries from normotensive (NT) and preeclamptic (PE) pregnancies, and the acute effects of pravastatin in the latter vessels were assessed. Pravastatin is hypothesized to alleviate endothelial dysfunction in PE via modulating aspects of NO and endothelium‐derived ...
Nathan M. Luque, Leo Leader, Sandra M. Lowe, Steven D. Horrowitz, Marianne Tare, Victoria Hinkley, Vladimir V. Matchkov, Maged M. Costantine, Irit Markus, Lu Liu, Shaun L. Sandow, Timothy V. Murphy   +11 more
wiley   +1 more source

Xanthohumol Pyrazole Derivative Improves Diet-Induced Obesity and Induces Energy Expenditure in High-Fat Diet-Fed Mice. [PDF]

ACS Pharmacol Transl Sci, 2021
Paraiso IL, Mattio LM, Alcázar Magaña A, Choi J, Plagmann LS, Redick MA, Miranda CL, Maier CS, Dallavalle S, Kioussi C, Blakemore PR, Stevens JF.   +11 more
europepmc   +1 more source

Visible‐Light Mediated Functionalization in Phe‐Containing Peptides Upon a Debenzylative Amination Process

Advanced Synthesis &Catalysis, Volume 368, Issue 6, 17 March 2026.
Selective late‐stage modification of N‐terminal phenylalanine short peptides is achived by visible‐light initiated reaction with N‐iodoimides in a debenzylation–amination process. This metal‐free method permits the incorporation of N‐containing heterocycles into the α‐position of the peptide backbone.
Guillermo Morales‐Ortega, Iván Pérez‐Cubero, Enrique Gómez‐Bengoa, Arkaitz Correa, Javier Carreras   +4 more
wiley   +1 more source

The Effect of Nano-Pyrazole Derivative of Thiosemicarbazone Magnetite on BRCA1, p53 and Bcl-2 Gene Expression in MCF-7 Breast Cancer Cell Line

Journal of Ardabil University of Medical Sciences, 2019
Background & objectives: Breast cancer is one of the most important causes of cancer deaths especially in developing countries. However, some synthetic compounds such as thiosemicarbazone and its metal derivatives can play a very significant role in ...
Mohammad Reza Izadpanah, Ali Saleh zadeh, Mohammad Zaiefi zadeh, Mohammad Nik pasand   +3 more
doaj  

Electro‐Mediated Redox Functionalization of Conjugated 1,3‐Dienes

Advanced Synthesis &Catalysis, Volume 368, Issue 6, 17 March 2026.
This review aims at providing a comprehensive view of the emerging field of electro‐mediated functionalization of conjugated 1,3‐dienes, highlighting key developments, mechanistic insights, and remaining challenges. It highlights the efficient use of electron as the sole reagent to access highly substituted allylic compounds from simple and readily ...
Ophélie Montiège, Jean‐François Brière, Cédric Schneider, Hélène Beucher   +3 more
wiley   +1 more source

Synthesis and Anti-Trypanosoma cruzi Activity of New Pyrazole-Thiadiazole Scaffolds

Molecules
Chagas disease, a silent but widespread disease that mainly affects a socioeconomically vulnerable population, lacks innovative safe drug therapy. The available drugs, benznidazole and nifurtimox, are more than fifty years old, have limited efficacy, and
Thamyris Perez de Souza, Lorraine Martins Rocha Orlando, Leonardo da Silva Lara, Vitoria Barbosa Paes, Lucas Penha Dutra, Mauricio Silva dos Santos, Mirian Claudia de Souza Pereira   +6 more
doaj   +1 more source