A Comprehensive Review on Journey of Pyrrole Scaffold Against Multiple Therapeutic Targets

Abstract

Heterocyclic compounds are that type of substances that are deeply intertwined with biological processes. Heterocycles are found in about 90% of commercially available medicines. In medicinal chemistry, finding new synthetic molecules with drug-like characteristics is a regular problem, which triggered the development of pharmacological molecules, the majority of which are based on N-heterocyclic motifs. Among the heterocycles, the pyrrole scaffold is the most commonly found heterocycle in both natural and synthetic bioactive compounds. Pyrrole has a five-membered heterocyclic ring with a plethora of pharmacophores, resulting in a library of different lead compounds. Pyrrole derivatives are physiologically active heterocyclic compounds that can be used as scaffolds for antibacterial, antiviral, anticancer, antitubercular, anti-inflammatory, and as enzyme inhibitors. On account of its extensive pharmacological profile, pyrrole and its various synthetic derivatives have drawn much attention among researchers to explore it for the benefit of humankind. This review presents an overview of recent developments in the pyrrole derivatives against multiple therapeutic targets.

Discovery of Conformationally Constrained Dihydro Benzo-Indole Derivatives as Pan-Metallo-β-Lactamase Inhibitors to Tackle Multidrug-Resistant Bacterial Infections

“…2A) signi cantly improved IMP-1 activity, attributed to its diverse therapeutic response pro le. Pyrrole is a versatile bioactive scaffold with several applications in drug discovery (such as anticancer, antipsychotic, anxiolytic, adrenergic antagonist, antiprotozoal, antibacterial, antifungal, and antimalarial) 32,33 . Next, we used conformational restriction technique for the enhancement of bioactive conformation, which is one of the successful strategies for improvement of the potency and/or selectivity; to constrain the conformation, the pyrrole in compound 9 was cyclized to the new class 4,5dihydro-1H-benzo[g]indole (dBI), resulting in compound 17a with two fold enhanced inhibitory e cacy against IMP-1 and thirteen fold enhanced inhibitory e cacy against VIM-1 (Fig.…”

Developments and applications of α-bromonitrostyrenes in organic syntheses

“…Bromonitroalkenes, especially bromonitrostyrenes are versatile building blocks for the construction of biological and pharmaceutical molecules and optically active compounds, such as dihydrofurans, 1,2 pyrroles, [3][4][5][6] and pyrazoles. [7][8][9] Selected examples of biologically active molecules containing pyrrole, furan, dihydrofuran, or cyclopropane cores are shown in Scheme 1.…”

Functionalized 2,3′-Bipyrroles and Pyrrolo[1,2-c]imidazoles from Acylethynylpyrroles and Tosylmethylisocyanide

“…The widespread applications of pyrroles, including their assemblies and the functionalized fused derivatives, in such fields as pharmacology, medicinal chemistry and materials science as well as their significance as precursors in the synthesis of many natural products have made this class of compounds one of the most important in heterocyclic chemistry [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 ].…”

“…Many products containing the pyrrole moiety exhibit a broad range of biological activities such as anticancer, antimicrobial, antiviral, anti-inflammatory, antipsychotic, antimalarial, insecticidal, etc. [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 ]. Based on pyrroles, anti-hyperlipidemic atorvastatin, anti-tumor agents sunitinib, vemurafenib, ruxolinitib and pemetrexed, vonoprazan used for the treatment of gastroduodenal ulcers, and nonsteroidal anti-inflammatory agents tolmetin, zomepirac and ketorolac were created.…”