One Pot Multicomponent Synthesis of Anti-inflammatory Active Tetrahydrofuro[3,2-c]pyridinone-2-carboxylate Derivatives

Tangeti, Venkata Swamy; Reddy, Boyi Harika; Evangeline, K. Sharon

doi:10.14233/ajchem.2018.21039

Cited by 4 publications

(1 citation statement)

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“…The therapeutic significance of fused pyridinone-furans as antiinflammatory drug candidates via inhibition of neutrophil-derived bGLU has been reported [234]. Compounds bearing MeO and CF 3 substituents on ring B (Fig.…”

Section: Pyridinone Pyrimidinones and Quinazolinonementioning

confidence: 99%

Therapeutic significance of β-glucuronidase activity and its inhibitors: A review

Awolade

Cele

Kerru

et al. 2020

European Journal of Medicinal Chemistry

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BiomarkerEnzyme inhibition Molecular target Structure activity relationship a b s t r a c tThe emergence of disease and dearth of effective pharmacological agents on most therapeutic fronts, constitutes a major threat to global public health and man's existence. Consequently, this has created an exigency in the search for new drugs with improved clinical utility or means of potentiating available ones. To this end, accumulating empirical evidence supports molecular target therapy as a plausible egress and, b-glucuronidase (bGLU) e a lysosomal acid hydrolase responsible for the catalytic deconjugation of b-D-glucuronides has emerged as a viable molecular target for several therapeutic applications. The enzyme's activity level in body fluids is also deemed a potential biomarker for the diagnosis of some pathological conditions. Moreover, due to its role in colon carcinogenesis and certain drug-induced dose-limiting toxicities, the development of potent inhibitors of bGLU in human intestinal microbiota has aroused increased attention over the years. Nevertheless, although our literature survey revealed both natural products and synthetic scaffolds as potential inhibitors of the enzyme, only few of these have found clinical utility, albeit with moderate to poor pharmacokinetic profile. Hence, in this review we present a compendium of exploits in the present millennium directed towards the inhibition of bGLU. The aim is to proffer a platform on which new scaffolds can be modelled for improved bGLU inhibitory potency and the development of new therapeutic agents in consequential.

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Section: Pyridinone Pyrimidinones and Quinazolinonementioning

confidence: 99%