1. A new series of organophosphorus compounds derived from N-substituted maleamic esters by reaction with dimethyl and diethyl phosphorodithioic acid was synthesized.2. Two isomers, with chemical structures analogous to malathion were obtained for each maleamic ester assayed.3. They were charact...

Fukinone (I), a new sesquiterpene ketone, was isolated from Petasites japonicus Maxim. Its structure and absolute configuration were established by the interconversion from isopetasol (V), a sesquiterpene of known absolute configuration, to dihydrofukinone (II).

A sesquiterpenoid ketone was isolated from leaf extracts of Petasites hybridus. The available sample (50 μg) was characterised from MS data obtained by deuterium labelling in transitu in the GLC column, and was identified as fukinone, except that optical homogeneity was not established.

The boron trifluoride etherate catalyzed reaction of 7-epimeric 3β,7-diacetoxy-9β,11β-epoxy-5α-lanostanes 1 and 2 in acetic anhydride resulted in the formation of a series of skeletally rearranged products, mainly 19(10→9β)abeo-lanostanes. 19(10→9β),30(14→8α)Bis-abeo-lanostane derivati...

A series of anthrapyridazone derivatives with one or two basic side chains at various positions in the tetracyclic chromophore have been synthesized. The key intermediates in the synthesis are 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-diones 1, 12 and 15 monosubstituted at position 2 (4d, 16a–e...

The cysteine-specific modifiers we reported previously, N-ethylmaleimide (NEM) and iodoacetanilide (IAA), have been applied to label cysteine residues of peptides in combination with electrospray ionization mass spectrometry (ESI-MS/MS), and their scope in proteomic studies was examined. Peptide...

Fifteen substituted 2-(pyrazol-1-yl)acetanilides were synthesized by N-alkylation of pyrazole and some of its derivatives with several 2-iodoacetanilides. The new compounds exhibited local anaesthetic and antiarrhythmic actions. The new compounds have been characterized by elemental chemical ana...

Nine substituted 2-(pyrazol-1-yl)-dialkylacetanilides were synthesized by N-alkylation of pyrazole and its derivatives with several 2-iodoacetanilides. The new compounds exhibited local anesthetic and antiarrhythmic actions. They have been characterized by elemental chemical analysis, UV–Vis, I...

We have developed a methodology for quantitative analysis and concurrent identification of proteins by the modification of cysteine residues with a combination of iodoacetanilide (IAA, 1) and 13C7-labeled iodoacetanilide (13C7-IAA, 2), or N-ethylmaleimide (NEM, 3) and d5-labeled N-ethylmaleimide...

This study reports a simple and efficient method for the direct iodination of substituted anilines with molecular iodine and copper acetate in acetic acid producing 2-iodoacetanilies and 2-iodoanilines. Employing density functional theory (B3LYP) and MidiX basis set, computational study is perfo...

Hydrogen sulfide (H2S), previously known as a toxic gas, is now recognized as a gasotransmitter along with nitric oxide and carbon monoxide. However, only few methods are available for quantitative determination of H2S in biological samples. 2-Iodoacetanilide (2-IAN), a thiol-reacting agent, has...

(±)-6α- and β-Methylestra-1,3,5(10)-trien-17β-ol (VII a and b; R = Me) and (−)-13β- ethyl-6β-methylgona-1,3,5(10)-trien-17β-ol (VIIb; R = Et) have been totally synthesized from 3-m-methoxyphenylbutyl bromide. The second compound has been converted to various (±)-13β- ethylgon-4-en-3-one...

IntroductionThis study aimed to determine the efficacy of different Leucovorin regimens to reduce oral mucositis in children with acute lymphoblastic leukemia after high-dose Methotrexate (HD-MTX).

RésuméIntroductionLe méthotrexate (MTX) est un antimétabolite utilisé dans le traitement de certains cancers, de maladies auto-immunes et, très couramment en dermatologie, du psoriasis cutané ou articulaire. Les toxicités secondaires à un surdosage en MTX sont essentiellement cutanée, ...

ObjectiveMethotrexate is one of the most widely used disease-modifying anti-rheumatic drugs. The hepatotoxicity of methotrexate resulted in poor compliance with therapy. The current study was designed to analyse the combined therapy of andrographolide (AD) and methotrexate (MTX) for complete Fre...

Gold nanoparticles functionalized with 3-mercapto-1-propansulfonate (AuNPs-3MPS) have been prepared and loaded with Methotrexate (MTX), an immunosuppressive agent used in the systemic treatment of moderate–severe inflammatory diseases. The effects of the [email protected] topically administered...

As has been well recognized, methotrexate (MTX) leads to a state of immunosuppression and can provide a basis for the development of lymphoproliferative disorders (LPDs). MTX-associated LPDs can affect nodal sites as well as extranodal sites, though the manifestation of an LPD in the form of mul...

Drug resistance and recurrence are the main clinical challenges in chemotherapy of lymphoma. Methotrexate (MTX), especially high dose MTX (HD MTX), is extensively used to treat some aggressive subtypes of lymphoma, such as Burkitt’s lymphoma, in order to overcome drug resistance. But poor solub...

Chaulmoogra oil based methotrexate loaded nanoemulsion was prepared via emulsification technique using tween 80 and ethanol as surfactants. The formulation was characterized by FTIR and TEM. The prepared nanoemulsion has an average particle size of 34 nm with negative surface charge and has pH c...

The plasma concentrations of methotrexate (MTX) and its major metabolite 7-hydroxy methotrexate (7-OH-MTX) are highly correlated with the toxicities in patients with high-dose MTX therapy. Routine monitoring of MTX and 7-OH-MTX plasma levels is useful for dose adjustment of rescue drugs and toxi...