Селекция перца на гетерозис с использованием линейного материала, полученного в процессе отдаленной гибридизации

Hybrids were originated by diallelic crossing of seven lines created by introgression selection. The features of inheritance of quantity locus traits were studied. The promising hybrids were distinguished from standard ones by a higher yield at early-term harvesting 0.1-0.5 kg. on square meter as well as for total harvesting 1.1 1.9 kg. on square meter.Изучены гетерозисные гибриды перца, полученные в результате диаллельных скрещиваний семи линий, созданных методом интрогрессивной селекции. Выявлены особенности наследования количественных полигенных признаков. Перспективные гибриды превосходили стандарт по ранней урожайности на 0,1 - 0,5 кг/м2, а по общей урожайности на 1,1 - 1,9 кг/м2

Synthesis and Antibacterial Activity of Sulfanilamides Containing Sterically Hindered Phenol Fragments

Abstract: New sulfanilamide derivatives containing sterically hindered phenol fragments have been synthesized via modification of the amino group by reaction with 3,5-di-tert-butyl-4-hydroxybenzyl acetate and diazotization followed by diazo coupling with 2,4-di-tert-butylphenol. 4-Aminobenzenesulfonamide derivatives at the sulfonamide group have been obtained by converting acetyl-protected 4-aminobenzenesulfonyl chloride to the corresponding sulfonohydrazide and reacting the latter with 3,5-di-tert-butyl-4-hydroxybenzyl acetate, sterically hindered hydroxybenzaldehydes, and N-(3,5-di-tert-butyl-4-hydroxybenzyl)isatin. Modification of sulfanilamide with sterically hindered phenol fragments significantly increased antibacterial activity

Synthesis of hybrid compounds by benzylation of acylhydrazones with 3,5-di-tert-butyl-4-hydroxybenzyl acetate

N-Benzylation of acylhydrazones of the hydroxybenzaldehyde series with 3,5-di-tert-butyl-4-hydroxybenzyl acetate was performed at room temperature in the absence of acid or base catalysts. Carboxamides do not react with 3,5-di-tert-butyl-4-hydroxybenzyl acetate under similar conditions. N-Benzylation of isoniazid and (diphenylphosphoryl)acetic acid hydrazones was shown to be an efficient method for the synthesis of new hybrid compounds containing moieties of biologically active acylhydrazones and sterically hindered phenols. N-Benzyl derivatives of isoniazid and (diphenylphosphoryl)acetic acid hydrazones containing a hydroxy group at the ortho position of the aromatic ring are formed as individual E isomers with respect to the C-N double bond

Bi-functional sterically hindered phenol lipid-based delivery systems as potential multi-target agents against Alzheimer's disease: Via an intranasal route

© The Royal Society of Chemistry. New lipid-based nanomaterials and multi-target directed ligands (MTDLs) based on sterically hindered phenol, containing a quaternary ammonium moiety (SHP-s-R, with s = 2,3) of varying hydrophobicity (R = CH2Ph and CnH2n+1, with n = 8, 10, 12, 16), have been prepared as potential drugs against Alzheimer's disease (AD). SHP-s-R are inhibitors of human cholinesterases with antioxidant properties. The inhibitory potency of SHP-s-R and selectivity ratio of cholinesterase inhibition were found to significantly depend on the length of the methylene spacer (s) and alkyl chain length. The compound SHP-2-16 showed the best IC50 for human AChE and the highest selectivity, being 30-fold more potent than for human BChE. Molecular modeling of SHP-2-16 binding to human AChE suggests that this compound is a dual binding site inhibitor that interacts with both the peripheral anionic site and catalytic active site. The relationship between self-assembly parameters (CMC, solubilization capacity, aggregation number), antioxidant activity and a toxicological parameter (hemolytic action on human red blood cells) was investigated. Two sterically hindered phenols (SHP-2-Bn and SHP-2-R) were loaded into L-a-phosphatidylcholine (PC) nanoparticles by varying the SHP alkyl chain length. For the brain AChE inhibition assay, PC/SHP-2-Bn/SHP-2-16 nanoparticles were administered to rats intranasally at a dose of 8 mg kg-1. The Morris water maze experiment showed that scopolamine-induced AD-like dementia in rats treated with PC/SHP-2-Bn/SHP-2-16 nanoparticles was significantly reduced. This is the first example of cationic SHP-phospholipid nanoparticles for inhibition of brain cholinesterases realized by the use of intranasal administration. This route has promising potential for the treatment of AD