Phenylketonuria (PKU) is an inherited metabolic disease caused by phenylalanine hydroxylase (PAH) deficiency. As the resulting high blood phenylalanine (Phe) concentration can have detrimental effects on brain development and function, international guidelines recommend lifelong control of blood...
An adduct between the tetrahydrogen form of decavanadate H4V10O282− and glycylglycine, with the stoichiometry Rb2H4V10O28·2Gly-Gly·2H2O, has been isolated and fully characterized. The crystal structure has been determined by X-ray diffraction data. The four hydrogen atoms of the polyvanadate f...
The effect of (D−)-fructose (fruit sugar), (D+)-galactose and (D+)-lactose (milk sugar) on the solute–solvent interactions occurred between the diphenhydramine-hydrochloride (DPH-HCl) drug and water was studied. To this end, the density, speed of sound and viscosity data for DPH-HCl drug in wat...
The title substance was prepared and studied to gain some insight into the structural basis for the well-known action of guanidinium salts as denaturation agents. The crystal structure has been determined from three-dimensional diffractometer X-ray data using Cu Kα radiation and refined by the ...
The infrared absorption spectra of glycine and the dipeptide glycylglycine have been measured using a novel spray-sampling technique which leads to better resolved spectra than the traditional crystal and solution methods. Spectra were recorded for a number of different alkali halide matrices. T...
Sol–gel molecularly imprinted materials (MIMs) are traditionally obtained by grinding and sieving of a monolith formed by bulk polymerization. However, this process has several drawbacks that can be overcome if these materials are synthesized directly in the spherical format. This work aimed at...
The results of ab initio SCFMO calculations using 3-21G and 4-21G basis sets for N-glycylglycine hydrochloride are presented. The optimized geometries from these calculations are compared with experimental bond lengths and bond angles obtained from X-ray crystallographic data. The vibrational sp...
We report a general approach for the synthesis of 5,6-dihydroindolo-naphthyridine ring system via an intramolecular cyclization of the indole NH to an alkene moiety as the key step.
An efficient, transition-metal-free cascade synthetic method has been developed for new 2-aryl/heteroaryl sulfonated benzo[f][1,7]naphthyridines. It is tert-butyl hydroperoxide (TBHP) mediated highly regioselective sulfonylation‒cyclization‒aromatization process between N-(3-aryl/heteroarylprop-...
Asymmetric syntheses of N-protected (R)-4-halo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines, advanced intermediates for the synthesis of highly potent and selective 5-HT2C agonists, are described. The key transformation involves ring opening of N-protected bicyclic sulfamidate (...
A novel series of 35 angularly fused pentacyclic 13H-benzo[f]chromeno[4,3-b][1,7]naphthyridines and 13H-benzo[f]chromeno[4,3-b][1,7]naphthyridin-5-ium chlorides were designed and synthesized. Their cytotoxic activities were investigated against six human cancer cell lines (NCIH23, HCT15, NUGC-3,...
Novel bacterial topoisomerase inhibitors (NBTIs) represent a new class of broad-spectrum antibacterial agents targeting bacterial Gyrase A and ParC and have potential utility in combating antibiotic resistance. A series of novel oxabicyclooctane-linked NBTIs with new tricyclic-1,5-naphthyridinon...
Visceral leishmaniasis is a parasitic disease that affects, among other areas, both sides of the Mediterranean Basin. The drugs classically used in clinical practice are pentavalent antimonials (SbV) and amphotericin B, which are nephrotoxic, require parenteral administration, and increasing dru...
A series of potential DNA-binding antitumor agents, 2-[ω-(alkylamino)alkyl]-9-methoxy-5-nitro-2,6-dihydroindazolo[4,3-bc][1,5]naphthyridines (2a–f), 10-aza derivatives of PZA, has been prepared by condensation of 9-chloro-2-methoxy-6-nitro-5,10-dihydrobenzo[b][1,5]naphthyridin-10-one (6) with ...
The production of a number of methyl esters such as methyl decanoate (MeDC), methyl salicylate (MeSC), and methyl benzoate (MeBZ) by esterification reactions of several carboxylic acids such as decanoic acid (DeC), salicylic acid (ScA), and benzoic acid (BeZ) with methanol, respectively, through...
Under certain dietary situations, rumen biohydrogenation results in the production of unique fatty acids that inhibit milk fat synthesis. The first of these to be identified was trans-10, cis-12 conjugated linoleic acid (CLA), but others are postulated to contribute to diet-induced milk fat depr...
Conjugated linoleic acid (CLA) has a number of beneficial health effects, including decreases in cancer incidence and atherosclerosis severity. However, dietary CLA intake is relatively low to promote the desired physiological effects. The CLA bacterial production in foods is a technological cha...
Conjugated linoleic acid (CLA) supplements have typically been comprised of 4 isomers (trans-8, cis-10; cis-9, trans-11; trans-10, cis-12; and cis-11, trans-13 CLA). Abomasal infusion of pure isomers has shown that trans-10, cis-12 CLA is a potent inhibitor of milk-fat synthesis, whereas cis-9, ...
The octadecadienoic conjugated linoleic acid (CLA) isomer with trans-11 and cis-13 double bonds (trans-11,cis-13 CLA) has been described in ruminant milk. For now, this specific CLA is suspected to derive exclusively from ruminal biohydrogenation of dietary α-linolenic acid. However, in rodents...
A quantitative GC method for conjugated linoleic acid (CLA) isomers of physiological significance (cis-9, trans-11 CLA and trans-10, cis-12 CLA) as non-esterified fatty acids (NEFA) or triacylglycerols (TAG) was developed. Furthermore, the effect of the internal standard addition point (sample o...
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