Novel β‐Lactam Compounds as Activators for Polyphenoloxidase

Abstract

A copper-containing enzyme polyphenol oxidase (other name is tyrosinase) plays crucial role in melanin biosynthesis, as a compound responsible for human pigmentation. Non controlled loss of melanin can cause hypopigmentation disease. The hypopigmentatory disorder can be treated with melanogenesis stimulators. Here, twenty-four new β-lactam compounds were synthesized, characterized and in vitro effects of them on banana tyrosinase investigated. The enzyme has been purified from banana by an affinity gel comprised of Sepharose4BÀ L-tyrosine-p-aminobenzoic acid. The results showed that the compounds have an effect on increasing the activity of tyrosinase enzyme. Molecules having a notable tyrosinase activator effects are compound 3 h (79.86) and compound 4 n (61.30). The maximal activation, 131% was determined at 130 μM concentration. These results suggested that compounds 3 h and 4 n might represent a novel approach for an effective therapy for diseases associate with tyrosinase dysfunction, such as vitiligo and hair graying.

Synthesis, Antimicrobial, Antioxidant, Toxicity and Anticancer Activity of a New Azetidinone, Thiazolidinone and Selenazolidinone Derivatives Based on Sulfonamide

“…Recent studies demonstrated that sulfonamides are active to prevent cancerous cells [4]. 2-Azetidinones (β-lactams) are saturated four-membered ring heterocyclic compounds containing three carbon atoms, a nitrogen atom, and a carbonyl group [5]. The name ''β-Lactam'' is given to cyclic amides because the nitrogen atom is associated with the β-carbon atom relative to the carbonyl group.…”

Synthesis, Characterization and Antibacterial Evaluation of Novel Β- Lactam and Thiazolidin-4-One Derivatives Having Thiadiazinyl Ring

“…The newly synthesized compounds' antibacterial potentiality may change as a result of the conversion of azomethine (CH=N) into βlactam and thiazole ring derivatives. Several biological activities associated with azomethine compounds have been documented in the literature, including antibacterial, antifungal, anti-inflammatory, and anticancer properties [23][24][25][26][27][28][29][30][31][32][33][34][35][36] .…”