In the present study, seven hydroxamic acid derivatives of nonsteroidal anti-inflammatory drugs (NSAIDs) (ibuprofen, fenoprofen, ketoprofen, indomethacin and diclofenac) were found to possess significant antioxidant, radical scavenging and metal chelating activities. The most active antioxidant and radical scavenger was N-methylhydroxamic acid of diclofenac (ANT = 88.0% and EC50 = 60.1 microg m...

The action of salicylhydroxamic acid and its halogen derivatives against tuberculosis, fungi, trypanosomae, and the biosynthesis of cholesterol are described. Their hypoglycemic and phospholipid lowering actions are also mentioned. The author suggested, in 1948, the use of salicylhydroxamic acid I (X = Y = Z = R = H)—called SH—as an antitubercular agent [26]. The suggestion was based on the hyp...

Induction of EBV lytic-phase gene expression, combined with exposure to an antiherpes viral drug, represents a promising targeted therapeutic approach to EBV-associated lymphomas. Short-chain fatty acids or certain chemotherapeutics have been used to induce EBV lytic-phase gene expression in cultured cells and mouse models, but these studies generally have not translated into clinical applicati...

Gas-liquid chromatography-mass spectrometry (GLC-MS) has been used for the separation, detection, and identification of 1,4-benzoxazin-3-ones (hydroxamic acids and lactams) and benzoxazolinones found in maize (Zea mays L.) extracts. Compounds of interest were partitioned into ethyl acetate from aqueous maize seedling extracts. For analysis by GLC-MS, trimethylsilyl derivatives were prepared, ch...

Reactive oxygen species, along with reactive nitrogen species, may play an important role in the pathogenesis and progress of many diseases, including cancer, diabetes and sickle cell disease. It has been postulated that hydroxyurea, one of the main treatments in sickle cell disease, achieves its activity partly also through its antioxidant properties. A series of hydroxyurea derivatives of L- ...

Several hydroxamic acids, viz., N-benzyl-N'-hydroxysuccinamide (BHS), poly[alpha,beta-(N-hydroxy)-DL-aspartamide] (PHA), poly[alpha,beta-(N-hydroxy-N-methyl-DL-aspartamide)] (PMHA) and poly[alpha,beta-(N-hydroxy)-DL- aspartamide]/poly[alpha,beta-(N-2-hydroxyethyl)-DL-aspartamide] (PHA-PHEA 1:1) were prepared and screened for their antimicrobial activity. Ten Gram-positive and 7 Gram-negative sp...

Aromatic amines can be metabolized by N-acetylation and N-hydroxylation to hydroxamic acids; these subsequently are conjugated to form the N,O-sulfonate and N,O-glucuronide conjugates. The N,O-sulfonates are highly labile metabolites that generate reactive intermediates involved in the covalent binding of the parent compound to protein, RNA and DNA, as well as to low molecular compounds like gl...

1. Acylation of 2-(N-hydroxyacetamido)fluorene and several other aromatic hydroxamic acids by carbamoyl phosphate was studied and compared with the acylating activity of acetyl-CoA. Acetyl phosphate was also studied. 2. The carbamoylation reaction had a pH optimum of 4.5. The reaction had a lag period of 1h and was then linear for 4h. This linearity ranged between 0.5mm- and 8mm-carbamoyl phosp...

The functionalisation of macrocyclic p-tertbutylcalix[4]arenes at the lower rim with hydroxamic acid and proline hydroxamic acid groups gives the calixarenes chelating properties similar to siderophores. The (1)H NMR spectrum of p-tertbutylcalix[4]arene tetrahydroxamic acid shows a broad band at 10.8 ppm in DMSO-d(6) attributed to NHOH protons. Diffuse reflectance spectral analysis of PVC membr...