The pictet-spengler reaction updates its habits

A Calcaterra, L Mangiardi, G Delle Monache… - Molecules, 2020 - mdpi.com
The Pictet-Spengler reaction (PS) is one of the most direct, efficient, and variable synthetic
method for the construction of privileged pharmacophores such as tetrahydro-isoquinolines …

Recent progress in the Horner-Wadsworth-Emmons reaction

JA Bisceglia, LR Orelli - Current Organic Chemistry, 2015 - ingentaconnect.com
The Horner-Wadsworth-Emmons reaction is one of the most reliable and widespread
synthetic tools for the stereocontrolled construction of ethylenic bonds. The versatility of the …

Emerging sulfated flavonoids and other polyphenols as drugs: Nature as an inspiration

M Correia‐da‐Silva, E Sousa… - Medicinal research …, 2014 - Wiley Online Library
Nature uses sulfation of endogenous and exogenous molecules mainly to avoid potential
toxicity. The growing importance of natural sulfated molecules, as modulators of a number of …

Recent advances on plasmin inhibitors for the treatment of fibrinolysis‐related disorders

RA Al‐Horani, UR Desai - Medicinal research reviews, 2014 - Wiley Online Library
Growing evidence suggests that plasmin is involved in a number of physiological processes
in addition to its key role in fibrin cleavage. Plasmin inhibition is critical in preventing …

Heparin mimetics with anticoagulant activity

AA Nahain, V Ignjatovic, P Monagle… - Medicinal research …, 2018 - Wiley Online Library
Heparin, a sulfated polysaccharide belonging to the glycosaminoglycan family, has been
widely used as an anticoagulant drug for decades and remains the most commonly used …

Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa

RA Al-Horani, P Ponnusamy, AY Mehta… - Journal of medicinal …, 2013 - ACS Publications
Inhibition of factor XIa (FXIa) is a novel paradigm for developing anticoagulants without
major bleeding consequences. We present the discovery of sulfated pentagalloylglucoside …

Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides

RA Al-Horani, UR Desai - Journal of Medicinal Chemistry, 2014 - ACS Publications
We recently introduced sulfated pentagalloylglucopyranoside (SPGG) as an allosteric
inhibitor of factor XIa (FXIa)(Al-Horani et al., J. Med Chem. 2013, 56, 867–878). To better …

Inhibitors of blood coagulation factor XIII

T Schmitz, CA Bäuml, D Imhof - Analytical biochemistry, 2020 - Elsevier
The blood coagulation factor XIII (FXIII) plays an essential role in the stabilization of fibrin
clots. This factor, belonging to the class of transglutaminases, catalyzes the final step of …

Small-molecule modulators of serine protease inhibitor proteins (serpins)

TF Kellici, ES Pilka, MJ Bodkin - Drug Discovery Today, 2021 - Elsevier
Highlights•Targeting serpins with drug-like molecules remains a challenge in drug
discovery.•Compounds targeting HSP47, antitrypsin, antithrombin, PAI-1 and neuroserpin …

Factor XIIIa inhibitors as potential novel drugs for venous thromboembolism

RA Al-Horani, S Kar - European journal of medicinal chemistry, 2020 - Elsevier
Abstract Human factor XIIIa (FXIIIa) is a multifunctional transglutaminase with a significant
role in hemostasis. FXIIIa catalyzes the last step in the coagulation process. It stabilizes the …