Supramolecular assemblies are generally described as inclusion/host-guest complexes comprised of two or more molecules that bind through non-covalent interactions. Exploring the application of these complexes as supramolecular drugs in pharmaceutical sciences has attracted great interest in recent years. Several investigations have proved that the complexes of antibacterial agents with various kinds of cyclic oligomers and metal ions enhanced their activity, and, in some cases, the complexes possessed higher healing properties than the parent drugs. Therefore, to develop a microbiologically potent supramolecular drug, we have investigated the complexation of the macrocyclic host with a guest molecule NSAID. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat inflammation, pain, and fever that are associated with bacterial infections. Pirfenidone (5-methyl-1-phenylpyridin-2-one)/PFD, an FDA-approved antifibrotic drug used for the treatment of idiopathic pulmonary fibrosis, is also an NSAID. The presence of anti-bacterial pyridone nucleus which is found in broad-spectrum fluoroquinolone antibiotics along with recent studies showing NSAIDs might have antibacterial properties piqued our interest in using PFD. The present work represents an unprecedented interplay of antibacterial activity of resorcinarene, a polyphenolic host together with its ability to interact chemically with an anti-inflammatory drug PFD, improving the overall antibacterial activity. The chemistry and the clinical activities involved in this study were investigated simultaneously by spectroscopic techniques, as well as by in vitro measurement of antibacterial activity against a Gram-positive and Gram-negative bacterium. The initial positive results obtained from this study could revolutionize the use of synthetically modifiable resorcinarene and their analogs in fine-tuning the clinical behavior of drugs

Supramolecular cocrystal of a pyridone NSAID (pharmaceutical active-pirfenidone) with cyclic macromolecules: A potential antimicrobial agent

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.