The binding of Coenzyme A and its acyl derivatives to carnitine acetyltransferase (EC 2.3.1.7) has been studied in this Department as part of an investigation into the mechanism of action of this enzyme. A CoA analogue lacking the reactive -SH group was needed for this work, and such an analogue...

1.1. The presence of an enzyme in dog skeletal and heart muscle and ox, chicken, and rat liver, which catalyzes the fixation of C14O2 by butyryl coenzyme A (CoA) is described. The reaction requires adenosine triphosphate (ATP) and Mn++ or Mg++.2.2. The relative rates of carboxylation of acetyl-C...

Publisher SummaryThis chapter elaborates a method for the enzymatic determination of acetoacetyl coenzyme A. The method is based on the principle that β-hydroxyacyl dehydrogenase (HOADH) catalyzes the reaction in the fatty acid cycle as described in the chapter. The reaction is pyridine nucleot...

Publisher SummaryCoenzyme A is a constituent of practically every living cell. It is the coenzyme for the transfer of acetyl groups and for lipid metabolism. It takes part in a large number of important biochemical reactions. Some of those are suitable for the determination of CoA. In the cataly...

The nickel- and iron-containing enzyme acetyl-CoA synthase (ACS) catalyzes de novo synthesis as well as overall cleavage of acetyl-CoA in acetogens, various other anaerobic bacteria, methanogens, and other archaea. The enzyme contains a unique active site metal cluster, designated the A cluster,...

Publisher SummaryThis chapter provides an overview of acetyl-CoA. It is the common intermediate in the oxidation of carbohydrates, fatty acids, and certain amino acids, and it is the point of entry for terminal oxidation in the citric acid cycle. Acetyl-CoA is also the precursor for the biosynth...

Publisher SummaryThis chapter describes a method for the enzymatic determination of acetyl coenzyme A. The best method for the determination of acetyl-CoA makes use of enzymatic acetylation of aromatic amines. This has the following advantages over other methods: the difference in free energy fo...

The potential use of pyrroloquinoline quinone disodium salt (BioPQQ™), as a supplemental food ingredient, was evaluated in a range of oral toxicity studies in rats including an acute study, a 14-day preliminary and a 28-day repeated-dose study, and a 13-week subchronic study. The median lethal d...

An evaluation of N,N-dipropargyl-2-phenylethylamine (DPGPEA) as a prodrug to increase brain levels of 2-phenylethylamine (PEA) was conducted in rats. A 0.1 mmol/kg (IP) dose of DPGPEA was administered and produced marked elevations of PEA levels in brain, liver and blood which were sustained for...

1.1. N-(3-Chloropropyl)phenylethylamine (CPPEA) was examined as a possible prodrug of the neuromodulator trace amine β-phenylethylamine (PEA) in rat tissues.2.2. CPPEA produced sustained elevation of PEA levels in rat brain, blood and liver.3.3. Rat brain concentrations of noradrenaline, dopami...

The uncatalyzed addition of N-(tert-butoxycarbonyl)-2-tert-butyldimethylsilyloxypyrrole 3 to 1,4-quinones bearing an electron withdrawing group at C-2 is reported. Use of 2-methoxycarbonyl-1,4-benzoquinone 4 and 2-methoxycarbonyl-1,4-naphthoquinone 5 provided an efficient synthesis of the pyrrol...

Phenols are deprotected with weak bases from their tert-butoxycarbonyl (Boc) derivatives. Boc deprotection with bases can avoid side reactions during the deprotection with acids. We note the lability of the Boc to bases and are able to utilize it as a new cleavage condition for synthetic studies.

A novel methodology for the synthesis of guanidines from amines has been developed using polymer assisted synthesis, potentially allowing the preparation of series of compounds in a high throughput manner. The methodology comprises the use of polymer-supported carbodiimide as the activating agen...

The synthesis of the unusual amino acids N-(tert-butoxycarbonyl)-l-vinyl glycine and N-(tert-butoxycarbonyl)-l-homophenylalanine starting from commercially available d-xylose via an alkylative fragmentation method is described.

Potential energy surface scan was performed and the most stable molecular structure of the N,N-di-tert-butoxycarbonyl (Boc)-2-amino pyridine (DBAP) molecule was predicted. The most stable molecular structure of the molecule was optimized using B3LYP method with cc-pVTZ basis set. Anticancer acti...

A highly efficient gram-scale method for the C(4)-functionalization of sydnone imine hydrochloride derivatives was developed. This new approach was realized through consecutive reactions including the preparation of a C(3)-substituted N6-tert-butoxycarbonyl sydnone imine derivative, deprotonatio...

A series of (R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives was designed, synthesized, and evaluated as novel inhibitors of dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes. Most of the synthesized compounds demonstrated good ...

Emergence and spread of multidrug resistant strains of Plasmodium falciparum has severely limited the antimalarial chemotherapeutic options. In order to overcome the obstacle, a set of new side-chain modified 4-aminoquinolines were synthesized and screened against chloroquine-sensitive (3D7) and...

Protein tyrosine phosphatase 1B (PTP1B) is implicated as a key negative regulator of the insulin and leptin signal-transduction pathways. PTP1B inhibitors have emerged as attractive and potent pharmaceutical agents for the treatment of type 2 diabetes and obesity. We identified a series of 2-eth...

A concise, scaleable route to both isomers of Z-2-tert-butoxycarbonylamino-6-hydroxyhex-4-enoic acid from 2-butyne-1,4-diol, utilizing l- and d-acylase enzymes is presented. These intermediates were readily converted to multigram quantities of N-Boc-(2S,4S,5R)- and N-Boc-(2R,4R,5S)-bulgecinine.