The aim of this study was to investigate the effect of pancreatic enzymes hydrolysis of camel αS-casein on their antioxidant, tyrosinase and urease inhibitory activities. Isolated αS-casein was hydrolyzed, fractionated and assayed for their antioxidant properties by using four complementary te...

ABSTRACTTransformation of polymorph I of clopidogrel hydrogen sulfate (CHS) to polymorph II of CHS during the crystallization was monitored by using in situ measurement of ultrasonic velocity. Drowning-out crystallization using methanol as a solvent and isopropyl alcohol as nonsolvent was carrie...

Clopidogrel hydrogen sulphate which belongs to a class of medicine called antiplatelet drugs. Chemically it is methyl (+)-(S)-α-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno [3,2-c] pyridine-5-acetate hydrogen sulphate having the empirical formula C16H17ClNO2S.HSO4 and molecular mass 321.82 g/mol. ...

The solubility of an active pharmaceutical ingredient (API) in various solvents is extremely important for its manufacturing and development as a drug. In this work, the solubility of two polymorphs of clopidogrel hydrogen sulfate (CHS) in the solvents of isopropanol (IPA) and ethyl acetate (EA)...

A novel three-solvent spherical crystallization method for producing monodisperse spherical particles with potential use in industry has been presented in this work. By combining the advantages of quasi-emulsion solvent diffusion (QESD) and spherical agglomeration (SA) method, the new approach a...

As a result of the chain of transformations from 1,3-butanedione with aryl and methoxy substituents through nitrosation and cyclization with hydrazine, the corresponding nitrosopyrazoles and aminopyrazoles were synthesized. According to this scheme, eight new previously unknown compounds were ob...

Histone deacetylase (HDAC) inhibitors are a class of potential therapeutics for the treatment of cancer. Bicyclic tetrapeptides equipped with methoxymethyl ketone and boronic acid as zinc-binding group were designed and synthesized. The inhibitory activities of these compounds were evaluated aga...

Pyridine-based Factor XIa (FXIa) inhibitor (S)-2 was optimized by modifying the P2 prime, P1, and scaffold regions. This work resulted in the discovery of the methyl N-phenyl carbamate P2 prime group which maintained FXIa activity, reduced the number of H-bond donors, and improved the physicoche...

The reactions of 1 equiv. of the ligand 3-(ethoxycarbonylmethyl-pyridin-2-ylmethyl-amino)-propionic acid methyl ester (2) with the Re(V) starting materials [ReOX3(PPh3)2] (X = Cl, Br) in refluxing chloroform yielded the Re(V)-oxo dihalide complexes [ReOX2{(C5H4NCH2)N(CH2CO2)(C2H4CO2CH3)}] (X = C...

A number of 2-arylpropionic acid non-steroidal anti-inflammatory drugs (‘profens’) undergo highly enantioselective inversion from the (R)- to (S)-enantiomer. The mechanism of this inversion reaction involves the initial enantioselective formation of a coenzyme A thioester followed by epimeriza...

Ibuprofen [racemic2-(4-isobutylphenyl)propionic acid] is a 2-arylpropionic acid nonsteroidal anti-inflammatory drug which undergoes unidirectional, R to S chiral inversion in vivo. It has been proposed that this chiral inversion phenomenon occurs via a coenzyme A (CoA) thioester intermediate. To...

Coenzyme A thioester formation is reported to be the first step of chiral inversion of R-ibuprofen. In order to investigate the mechanism of this reaction adenylate derivatives of the ibuprofen enantionmers were synthesized chemically. R- and S-ibuprofenyl-adenylates as well as free acids were i...

The D- and L- enantiomers of myo-inositol 1-phosphorothioate have been synthesized from 2,3,4,5,6-pentakis-O-benzyl myo-inositol in 6 steps, both compounds are substrates for inositol monophosphatase. D-glucopyranose 6-phosphorothioate did not serve as a substrate for the enzyme inositol synthas...

Using a combination of high-performance ion chromatography analysis and kinetic studies, the stereospecificity of myo-inositol hexakisphosphate dephosphorylation by the phytate-degrading enzyme P2 of Escherichia coli was established. High-performance ion chromatography revealed that the phytate-...

Several substituted derivatives of kynurenic acid were tested on the N-methyl-D-aspartate (NMDA) receptor/ion channel complex present in the guinea pig myenteric plexus, on the binding of [3H]glycine and of [3H]N-[M2-thienyl)cyclohexyl]piperidine ([3H]TCP) to rat cortical membranes and on the de...

Several derivatives of kynurenic and thiokynurenic acids were synthesized and tested for their ability to protect primary cultures of cerebellar granule cells against excitotoxic damage, and to affect the binding of [3H]glycine ([3H]Gly), [3H]α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid...

Despite overwhelming and tragic evidence of their detrimental and dangerous consequences, amphetamines remain significant drugs of abuse and addiction. The effects of 4-substituted amphetamines: 4-hydroxyamphetamine (4-HA), 4-methoxyamphetamine (4-MEA), 4-ethoxyamphetamine (4-ETA), 4-propoxyamph...

The appearance on the street of 4-ethoxyamphetamine (4-EA) led to the need for a reference standard to be synthesized. To satisfy concerns that this compound could be distinguished from the isomeric 2- and 3-ethoxyamphetamines (2-EA and 3-EA, respectively), standards for each of those substances...

Subchronic Toxicity Study in Rats with 1-Methyl-3-propylimidazole-2-thione (PTI): Effects on the Thyroid. Biegel, L. B., Cook, J. C., O'Connor, J. C., Aschiero, M., Arduengo, A. J., III, and Slone, T. W. (1995). Fundam. Appl. Pharmacol. 27, 185-194.A 90-day gavage study was performed to eva...

Parkinson's disease is characterized by the progressive degeneration of midbrain dopaminergic neurons. Buddleia lindleyana is a traditional Chinese herb, commonly called Zui Yu Cao. The purification and identification of pedicularioside A and other phenylethanoid glycosides from this plant ...