Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators

Abstract

A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, 1H-NMR and mass spectroscopy. The final compounds have been screened for in vitro pro-inflammatory cytokine inhibitory and in vivo anti-inflammatory activity. The biological results revealed that among all tested compounds some fused pyrroles, namely the pyrrolopyridines 3i and 3l, show promising activity. A docking study of the active synthesized molecules confirmed the biological results and revealed a new binding pose in the COX-2 binding site.

Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition

“…The anti-inflammatory activity shown by the above derivatives has drawn our interest to continue our research [44][45][46] for development of new anti-inflammatory agents. The synthesis and biological evaluation of new 2-furanone derivatives are reported herein.…”

γ‐Fe2O3@HAp@PBABMD@Cu magnetic nanoparticles: Efficient, green, and recyclable novel nanocatalyst for the synthesis of densely functionalized pyrrole‐pyrido[2,3‐d]pyrimidine hybrids

“…Considering the biological importance of pyrrole scaffolds, development of one-pot synthetic routes to construct a heterocyclic system containing this structural motif remains a topic of attention. [36][37][38][39][40][41][42] One of the main principles of green chemistry is to avoid the use or production of dangerous substances in the design, making, and application of the chemical product. On the basis of this fact, designing new methods by employing multi-component reactions (MCR) without using any harmful organic solvents [43][44][45][46] and using heterogeneous, recyclable catalysts makes these reactions powerful green chemical technology procedures, resulting in minimal pollution and waste material.…”

“…Similarly, the pyrrole skeleton, which is one of the most prominent N ‐heterocycles, is the key structure in natural and pharmaceutically substantial molecules and exhibited an extensive range of biological activities (Figure 1d,e). Considering the biological importance of pyrrole scaffolds, development of one‐pot synthetic routes to construct a heterocyclic system containing this structural motif remains a topic of attention 36–42 . One of the main principles of green chemistry is to avoid the use or production of dangerous substances in the design, making, and application of the chemical product.…”

Synthesis and Characterization of New Biologically Active Pyrrolo[2,3-b]Pyridine Scaffolds

“…[2]. They are displaying interesting chemical reactions and important biological actions such as antibacterial [3], antimycobacterial [4], anti-inflammatory [5], antifungal [6], antiparkinson's [7], antitumor [8], antiproliferative [9], antiviral [10], muscarinic antagonist [11], antimicrobial [12], anticancer [13][14][15]. In light of the above all, it was the target to design and synthesize the expected biologically active structures of pyrrolo [2,3-b] An essential component of the search for new leads in drug designing program is the synthesis of molecules, which are novel still resembling known biologically active molecules by virtue of the presence of some critical structural features.…”