Reactions of 2-hetarylacetonitriles 1 with ethyl 2-alkylsulfanyl-4-chloro-5-pyrimidinecarboxylates 4 were studied. The interaction of pyridine, benzimidazole and benzothiazole derivatives 1a–d affords a series of new condensed pyridopyrimidines 5–7. In the case of benzoxazole- and 4-arylthiazo...

A series of novel 2-butyl-4-chloro-1-methylimidazole derived peptidomimetics were designed, synthesized and evaluated for their Angiotensin Converting Enzyme (ACE) inhibitor activity. 2-Butyl-4-chloro-1-methylimidazole-5-carboxylic acid 2 obtained after oxidation of respective carboxaldehyde 1, ...

Two routes for the synthesis of homofascaplysin B, C and analogues have been established using the photocyclization as the key step. The first route is based on sequential photocyclization and photochemical dehydrogenation reactions of 2-chloro-3-acyl-1-[2-(indol-3-yl)ethyl]indoles in Cu(OAc)2- ...

K. A. Santarius, G. Falsone and H. Haddad. Effects of the sesquiterpene lactone tetraesters thapsigargicin and thapsigargin, from roots of Thapsia garganica L., on isolated spinach chloroplasts. Toxicon25, 389 – 399, 1987.—The effect of thapsigargicin and thapsigargin, extracted from the roots...

The potential systemic availability of retinoids from topically applied isotretinoin was assessed in 12 men with acne vulgaris. Isotretinoin 0.05% gel was apphed to patients at a daily dose of 20 gm (equivalent to 10 mg of isotretinoin) over a 1900 cm2 surface area of skin on the face, back, and...

A highly sensitive HPLC method with automated column switching was developed for the simultaneous determination of endogenous levels of 13-cis-retinoic acid (isotretinoin), all-trans-retinoic acid (tretinoin) and their 4-oxo metabolites in plasma samples from man, Cynomolgus monkey, rabbit, rat ...

A fully automated gradient high-performance liquid chromatographic method for the determination of isotretinoin, tretinoin and their 4-oxo metabolites in plasma was developed, using the column-switching technique. After dilution with an internal standard solution containing 20% acetonitrile, 0.5...

BackgroundA high-fat meal is needed for optimal absorption of isotretinoin. A new formulation of isotretinoin, which enhances absorption of isotretinoin in the absence of dietary fat, has recently been approved by the Food and Drug Administration (FDA).

β-amino acids are widely used in drug research, and S-3-amino-3-phenylpropionic acid (S-APA) is an important pharmaceutical intermediate of S-dapoxetine, which has been approved for the treatment of premature ejaculation. Chiral catalysis is an excellent method for the preparation of enantiopur...

Synthesis of complexes derived from hydrazones derived from both P-vanillin (H2L1) and its isomer O-vanillin (H2L2) of 2-hydrazinyl-2-oxo-N-phenylacetamide that coordinated with high magnetic metal ions of both Mn(II) and Co(II) were performed and characterized by different physicochemical metho...

Manganese(II), iron(II), cobalt(II), nickel(II), copper(II), and chromium(III) complexes of (E)-2-(2-(2-hydroxybenzylidene)hydrazinyl)-2-oxo-N-phenylacetamide were synthesized and characterized by elemental and thermal (TG and DTA) analyses, IR, UV–vis and 1H NMR spectra as well as magnetic mom...

The Cr(III) and Fe(III) complexes of hydrazones derived from the condensation of 2-hydrazinyl-2-oxo-N-phenylacetamide with both vanillin and o-vanillin synthesized and characterized by different conventional physicochemical techniques. The kinetic and thermodynamic parameters for the different d...

The development of O6-(3-[125I]iodobenzyl)-2′-deoxyguanosine ([125I]IBdG), the glycosylated analogue of the O6-3-iodobenzylguanine (IBG), as an agent for the in vivo mapping of the DNA repair protein alkylguanine-DNA alkyltransferase (AGT) is described. Synthesis of its tin precursor, O6-3-trim...

(−)-Cytisine and its derivatives, characterized by high affinity to neuronal nicotinic acetylcholine receptors (nAChRs), have been shown to be important probes in the research of central nervous system disorders. In this work new halogenated N-benzylcytisine derivatives were obtained, and struct...

The multi-millicurie production of the SPECT radiopharmaceutical N,N,N′-trimethyl-N′-(2-hydroxy-3-methyl-5-[123I]iodobenzyl)-1,3-propanediamine ([123I]HIPDM) in high specific activity is described. Using no-carrier-added electrophilic iododeprotonation reactions and HPLC purification, [123I]HI...

This study evaluated the effects of the adenosine A3 receptor agonist, N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide (IB-MECA), in two murine models of colitis, the dextran sodium sulphate-induced colitis and the spontaneous colitis found in interleukin-10 gene deficient mice. IB-MECA was gi...

As a continuation to our previous work concerning antitumor benzimidazoles, we have synthesized series of new derivatives of 2-(1-benzyl-2-methyl-1H-benzimidazol-5-ylimino)-3-(substituted)-thiazolidin-4-one (6a–e), 3-(2-methyl-1H-benzimidazol-5-yl)-2-substituted-thiazolidin-4-one (9a–f) and we...

Trichomonosis is a common sexually transmitted infectious disease linked to reproductive health complications. Recently, the benzimidazole nucleus has emerged as a promising scaffold to develop new trichomonicidal agents. Despite the fact that large amounts of experimental data have been accumul...

The intrinsic anion oxidation potential (ΔEv) and lithium ion pair dissociation energy (ΔEd) are two important properties for predicting the potential use of new lithium salts for battery electrolytes. In this work several cyano substituted fluoroalkylated benzimidazole and imidazole anions ha...

Photochemical ring substitution of the N-trifluoroacetyl derivatives of histamine and of L-histidine methyl ester by pentafluoroethyl radical provides the corresponding 2- and 4-pentafluoroethylated products in yields of 19% and 27%, respectively. Alkaline hydrolysis converts the 2-pentafluoroet...