The binding and interaction of carbamoylcholine with the nicotinic acetylcholine receptor was investigated using photolytically release carbamoylcholine (‘caged’ carbamoylcholine). Upon UV flash activation of this photolabile substrate analog, characteristic changes in the IR absorbance spectr...

Three sequential treatments of an N-protected tribromoimidazole with n-BuLi / electrophile in a 1-pot process leads to N-protected 2,4,5-trisubstituted imidazoles. The method can be applied to the preparation of the immediate of carmethizole.

The solution stability and degradation mechanism of Carmethizole HCl (1, NSC-602668), an experimental anti-cancer drug, were studied. An apparent pKa value of 4.2 at 25°C and ionic strength = 0.15 M (NaCl) was determined for 1 by potentiometric titration. The degradation 1 in aqueous solution p...

A new efficient six-step synthesis of carmethizole, a novel bis-carbamate alkylating agent, and syntheses of related nitrogen analogues are described, using a key 4,5-disubstituted imidazole intermediate 8.

This study synthesized 20 sclareol derivatives. The antifungal activities of these derivatives were evaluated in vitro against five phytopathogenic fungi using the mycelium growth rate method. Among all the tested compounds, compound 16 with one iodine atom and three hydroxyl groups displayed hi...

Epidermal growth factor receptor (EGFR) signaling pathway has been previously investigated for its significant role in the progression of different types of malignant tumors, where development of small molecules targeting EGFR is well known strategy for design of antitumor agents. Herein, we rep...

Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alcohol derivatives showed significant cytotoxic activities. Compound 1...

Novel 4-substituted 2-pyridin-2-ylamides were developed using in-silico ligand-based drug design (LBDD) in an attempt to identify inhibitors of SH2-containing 5′-inositol phosphatase 2 (SHIP2), which is implicated in insulin-resistant type 2 diabetes. Among the compounds synthesized, N-[4-(4-ch...

In the present study, a series of 3-benzylquinazolin-4(3H)-ones were synthesized and characterized. Their vasodilative effects were evaluated by wire myograph on isolated rat mesenteric arterial ring induced contraction with 60 mM KCl. The SAR of target compounds was discussed preliminarily. Amo...

An 11-step synthesis of endo,endo-2-amino-6-[(E)-2′-phenyl]ethenylbicyclo[2.2.1]heptane (6) and the corresponding (Z)-isomer (7) was carried out in an attempt to make a compound that could trap the purported amine radical cation intermediate during monoamine oxidase (MAO)-catalyzed oxidation of...

Within the series of chiral 3,3′-(1,2-ethanediyl)bis[2-arylthiazolidin-4-ones], the 3,4-dimethoxyphenyl substituted derivative was found in the primary anti-inflammatory screening to be endowed with superior in vivo properties and good safety profile. Such a lead compound was modified by elimin...

Twenty-eight 1,2-diarylethylenediamines were investigated in a search for highly sensitive fluorogenic reagents for catecholamines (norepinephrine, epinephrine and dopamine). They all react with epinephrine used as a model catecholamine under mild conditions (pH 6.5–6.8, 37–50°C) in the prese...

Eight 1,2-diarylethylenediamines in the meso- or DL-form produce fluorescence when heated with reducing carbohydrates in an alkaline medium. Of the diamines, meso-1,2-bis(4-methoxyphenyl)ethylenediamine is the most favourable reagent for reducing carbohydrates, including 2- deoxy sugars, amino s...

Amino acids are essential for life, and have many functions in metabolism. One particularly important function is to serve as the building blocks of peptides and proteins, giving rise complex three dimensional structures through disulfide bonds or crosslinked amino acids. Peptides are frequently...

Amino acids are essential for life, and have many functions in metabolism. One particularly important function is to serve as the building blocks of peptides and proteins, giving rise complex three dimensional structures through disulfide bonds or crosslinked amino acids. Peptides are frequently...

Publisher SummaryThis chapter discusses the unnatural diamino acid derivatives as scaffolds for creating diversity and as linkers for simplifying screening in chemical libraries. The methodologies employed for the use of the protected aromatic scaffold and L-2, 3-diaminopropionic acid Dpr(phenyl...

Compared with the better-studied canonical amino acids, the distribution, metabolism and functions of natural non-canonical amino acids remain relatively obscure. Natural non-canonical amino acids have been mainly discovered in plants as secondary metabolites that perform diversified physiologic...

Amino acids play an important role in cellular processes and are building blocks for peptides and proteins, which take part in regulatory processes within each organism. Hence a large variety of biotechnologically or synthetically produced therapeutic drugs are peptides and proteins. Due to the ...

•ObjectiveTo determine the nature and characteristics of a unique hemoglobin variant that causes a spurious increase in glycated hemoglobin (Hb Alc).

BackgroundThe leading cause of death in patients with Fukuyama congenital muscular dystrophy (FCMD) is congestive heart failure or respiratory dysfunction, which is same as that in Duchenne muscular dystrophy (DMD). Recent studies reported that renal dysfunction is a common complication and an i...