Design, Synthesis, Structural Insights, Tyrosinase Inhibition, and Sun Protection Factor of New Thiosemicarbazone Derivatives.

Tyrosinase, a key protein in the biosynthesis of melanin pigments, is crucial in determining skin pigmentation. Inhibiting tyrosinase activity is a promising approach for treating conditions related to excessive pigmentation. For the synthesis of more potent tyrosinase inhibitors, we combined two approaches, para-substitution and lipophilicity, to enhance the inhibitory properties of ()-2-(4-hydroxybenzylidene)hydrazine-1-carbotiamide, whose enzyme inhibitory properties have been previously demonstrated.

Biological Potential of Extracts: α-Glucosidase and Antibiofilm Activities In Vitro.

Type 2 diabetes (T2D), characterized by insulin resistance and β-cell dysfunction, requires continuous advancements in management strategies, particularly in controlling postprandial hyperglycemia to prevent complications. Current antidiabetics, which have α-amylase and α-glucosidase inhibitory activities, have side effects, prompting the search for better alternatives. In addition, diabetes patients are particularly vulnerable to yeast infections because an unusual sugar concentration promotes the growth of spp.

Computational Approach to Identifying New Chemical Entities as Elastase Inhibitors with Potential Antiaging Effects.

In the aging process, skin morphology might be affected by wrinkle formation due to the loss of elasticity and resilience of connective tissues linked to the cleavage of elastin by the enzymatic activity of elastase. Little information is available about the structural requirements to efficiently inhibit elastase 1 (EC 3.4.

Exploring the 1-(4-Nitrophenyl)-3-arylprop-2-en-1-one Scaffold for the Selective Inhibition of Monoamine Oxidase B.

A small library of 1-(4-nitrophenyl)-3-arylprop-2-en-1-one derivatives was synthesized to identify new human monoamine oxidase B selective inhibitors. Their inhibitory activity toward MAO-A and MAO-B isoforms was evaluated to determine their potency and selectivity. All newly synthesized compounds were nanomolar inhibitors of the B isoform with IC concentrations ranging from 120 to 2.

: Phytochemistry and Antidiabetic Properties.

L. () is an evergreen shrub (Anacardiaceae family) primarily found in the Mediterranean region. The plant has been thoroughly characterized, resulting in a high concentration of bioactive compounds as flavonoids and phenolics.