Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of Thiourea Derivatives Based on 3-Aminopyridin-2(1)-Ones.

Reactions with allyl-, acetyl-, and phenylisothiocyanate have been studied on the basis of 3-amino-4,6-dimethylpyridine-2(1)-one, 3-amino-4-phenylpyridine-2-one, and 3-amino-4-(thiophene-2-yl)pyridine-2(1)-one (benzoyl-)isothiocyanates, and the corresponding thioureide derivatives were obtained. Twelve thiourea derivatives were obtained and studied for their anti-diabetic activity against the enzyme α-glucosidase in comparison with the standard drug acarbose. The comparison drug acarbose inhibits the activity of α-glucosidase at a concentration of 15 mM by 46.

Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of 1,3,4-Thiadiazole Derivatives of 3-Aminopyridin-2(1)-ones.

This article reports on the synthesis of nine promising new 1,3,4-thiadiazole derivatives based on 3-aminopyridones, containing various acidic linkers. The synthesis was carried out by cyclizing the corresponding thiohydrazides - and anhydrides of glutaric, maleic, and phthalic acids upon heating in acetic acid solution. The conducted bio-screening of the synthesized new 1,3,4-thiadiazole derivatives containing different acidic linkers (butanoic, acrylic, and benzoic acids) showed that they have significant inhibitory activity against -glucosidase (up to 95.

Efficacy of a multitargeted, salicylic acid-based dermocosmetic cream compared to benzoyl peroxide 5% in Acne vulgaris: Results from a randomized study.

Introduction: Acne vulgaris (acne) is characterized by both inflammatory and non-inflammatory lesions. Benzoyl peroxide (BPO) 5% is approved to treat acne but may cause skin irritation and/or contact allergy.

Objectives: To compare the benefit in acne of a multitargeted dermocosmetic cream containing salicylic acid, lipohydroxy acid, niacinamide, 2-oleamido-1,3-octadecanediol, piroctone olamine, zinc, Aqua posae filiformis, and thermal spring water (DC-Eff) to BPO 5% gel.

Physicochemical properties and compatibility of sodium alginate and fucoidan solutions.

The interaction between linear sodium alginate and branched fucoidan were investigated using viscosity and tensiometric measurements. It was shown that water-soluble interpolymer complex is formed. The alginate-fucoidan complexation is due to the formation of a cooperative system of hydrogen bonds between the ionogenic and hidroxyl groups of sodium alginate and fucoidan and hydrophobic interactions.

Synthesis, Structure and Molecular Docking of New 4,5-Dihydrothiazole Derivatives Based on 3,5-Dimethylpyrazole and Cytisine and Salsoline Alkaloids.

The interaction results of 1,2-dibromo-3-isothiocyanatopropane with some pyrazoles as well as cytisine and salsoline alkaloids were presented in this paper. It was shown that the reaction resulted in one one-step and rather mild method for the preparation of the corresponding 1,3-thiazoline bromomethyl derivatives. The yield of this reaction was affected by the presence of a base and an order in which reagents were added.

Design, synthesis, spectroscopic characterization, computational analysis, and α-amylase and α-glucosidase evaluation of 3-aminopyridin-2(1)-one based novel monothiooxamides and 1,3,4-thiadiazoles.

Due to the growth in the incidence of diabetes mellitus throughout the world, the urgency in the search for new safe and effective inhibitors of α-amylase and α-glucosidase is increasing. In this work, we attempted to carry out studies on the synthesis, modification and comprehensive computer and biological research of new derivatives of monothiooxamides. It was shown that monothiooxamides based on 3-aminopyridin-2(1)-ones enter into transamidation reactions with hydrazine hydrate to form the corresponding thiohydrazides.

Cytoprotective Activity of Newly Synthesized 3-(Arylmethylamino)-6-Methyl-4-Phenylpyridin-2(1)-Ones Derivatives.

Currently, studies are being conducted on the possible role of the cytoprotective effect of biologically active substances in conditions of cerebral hypoxia or cardiomyopathies. At the same time, oxidative stress is considered one of the important mechanisms of cellular cytotoxicity and a target for the action of cytoprotectors. The aim of this study is to search for derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridin-2(1)-ones.