Pd-mediated functionalization of polysubstituted pyrroles: Their evaluation as potential inhibitors of PDE4

Living on pyrrolic foundations – Advances in natural and artificial bioactive pyrrole derivatives

“…Preparation of the key starting reagent was also realised in a one-pot regime, in a reaction of 4-iodoaniline with phenacyl bromide and ethyl glyoxylate, in the presence of pyridine. The resultant iodopyrrole was treated with terminal alkynes, yielding ethyl 2-benzoyl-1-(4-alkynylaryl substituted phenyl)-5-phenyl-1H-pyrrole-3-carboxylate (47) [104].…”

Synthesis of 2-Aminopyrroles Via Metal-Free Annulation of Ynamides with 2H-Azirines

“…Polysubstituted 2-aminopyrroles are fundamental structural motifs in numerous natural products and pharmaceuticals, such as marine alkaloids rigidins A, B, C, D, and E, MEK inhibitors, PDE4 inhibitor, and antagonize L-type calcium channels antagonizer MNP001, MBL inhibitor, human 15-lipoxygenase-1 (h-15-LOX-1) inhibitor, and antimycotic agents . Although considerable efforts have been devoted to preparing various functionalized pyrrole derivatives, , only a limited number of methods have been developed for the synthesis of 2-aminopyrroles, which are difficult to access via general approaches for pyrrole construction.…”

Synthesis and evaluation of novel spiro derivatives for pyrrolopyrimidines as anti-hyperglycemia promising compounds

“…Almost 70–80% of patients die from one of these two conditions. The International Diabetes Federation (IDF) listed Egypt among the world top 10 countries in the number of patients with diabetes 3–5 . In Egypt, the predominance of diabetes is around 15.56% among adults (age: 20 and 79 years), with an annual death of 86,478 related to diabetes 2 .…”