The non-toxic trans isomer of combretastatin-A4 can be photoisomerised in physiological conditions to cis-CA4, a potential anticancer drug. Absorption at wavelengths with high tissue penetration can be achieved by functionalization with substituents influencing the degree of charge-transfer (CT)...

The cardi ovascular effects of a series of tertiary esters of arecaidine (1-methyl-1,2,5,6-tetrahydro-3-carboxy-pyridine) and isoarecaidine (1-methyl-1,2,5,6-tetrahydro-4-carboxy-pyridine) were investigated in the pithed rat. For some esters (e.g. arecoline, arecaidine propargyl ester, isoarecol...

Methylmethacrylate (MMA) sulfopropylmethacrylate (SPM) copolymer nanoparticles were prepared by free radical polymerization and the loading characteristics of the muscarinic agonists arecaidine propargyl ester (APE) and pilocarpine were investigated. The loading efficiency was mainly influenced ...

Arecaidine propargyl ester (APE) is a potent muscarinic agonist often used in pharmacological studies. To date, no sensitive quantitative analytical method for APE has been published. In this study, two methods for the quantitative determination of APE are compared: a colorimetric assay, based o...

A new type of polymer-supported amine, p-benzyloxybenzylamine (BOBA) resin, has been developed. BOBA resin is readily prepared from Merrifield's resin in two steps. Polymer-supported imines prepared from aldehydes and BOBA resin reacted with silyl enolates in the presence of a catalytic amo...

TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respect...

Retinoic acid receptor-related orphan receptors (RORs) are ligand-dependent transcriptional factors and members of the nuclear receptor superfamily. RORs regulate inflammation, metabolic disorders and circadian rhythm. RORγ is a promising therapeutic drug target for treating Th17-mediated autoi...

In the present study, we have further extended the structure–activity relationships for the tetrazolyl ureas class of compounds as potential FAAH and/or MAGL inhibitors, by replacing the dimethylamino group of the parent compounds 1 and 2 with bulkier groups or by introducing on the distal phen...

Leaves from Phyllanthus muellerianus (Kuntze) Exell. are traditionally used for wound healing in Western Africa. Aqueous extracts of dried leaves recently have been shown to stimulate proliferation of human keratinocytes and dermal fibroblasts. Within bioassay-guided fractionation the ellagitann...

Ethnopharmacological relevancePhyllanthus muellerianus (Kuntze) Exell. which belongs to the Family Euphorbiaceae is a shrub widely distributed in West Africa. It is used traditionally to manage wounds and wound infections, menstrual disorders, fevers, pain and inflammation. Hence to confirm its ...

Shewanella spp. are major causes of fish spoilage. Terminalia ferdinandiana (Kakadu plum) extracts were investigated for their ability to inhibit Shewanella spp. growth. Leaf and fruit extracts displayed potent growth inhibitory properties against all Shewanella spp. The methanolic leaf extract ...

SummaryThe yeast Sac3:Cdc31:Sus1:Thp1 (TREX-2) complex facilitates the repositioning and association of actively transcribing genes with nuclear pores (NPCs)—“gene gating”—that is central to integrating transcription, processing, and mRNA nuclear export. We present here the crystal structure...

Two series of N-[5-(2-furanyl)-2-methyl-4-oxo-4H-thieno[2,3-d]pyrimidin-3-yl]-carboxamide (4a–m) and 3-substituted-5-(2-furanyl)-2-methyl-3H-thieno[2,3-d]pyrimidin-4-ones (5a–m) were synthesised using appropriate synthetic route. All the test compounds 4a–m and 5a–m were assayed in vitro for...

The addition of a phase transfer catalyst during the epoxidation of perbenzylated glycals with oxone–acetone under biphasic conditions allows their complete epoxidation. The epoxides were readily transformed into methyl 1,2-trans-β-d-glycosides or 1,2-trans-β-d-glycopyranosyl azides (d-gluco ...

Three crown ether derivatives, 1,2-O-dioleoyl-3-O-{2-[(12-crown-4)methoxy]ethyl}-sn-glycerol (12C4L), 1,2-O-dioleoyl-3-O-{2-[(15-crown-5)methoxy]ethyl}-sn-glycerol (15C5L) and 2,3-naphtho-15-crown-5 (NAP5), have been incorporated into 1-palmitoyl-2-oleoyl-phosphatydilcholine (POPC) liposomes. Th...

Cation recognition plays a vital role in defining advanced functions of macromolecules in nature. An example of such an interaction is the action of a natural antibiotic, valinomycin, that behaves as a potassium ionophore. It encages the cation to transport it across a cell membrane and easily r...

2,3-Dioxanaphthalene derivatives of [3n]crown-n macrocycles were synthesised from 2,3-dihydroxynaphthalene and polyglycoldihalides and studied for their cationic recognition properties using steady state fluorescence spectroscopy. The association constants for the interaction of 2,3-naphtho[12]c...

A series of (−)-β-d-(2R,4R)-dioxolane-thymine-5′-O-aliphatic acid esters as well as amino acid esters were synthesized as prodrugs of (−)-β-d-(2R,4R)-dioxolane-thymine (DOT). The compounds were evaluated for anti-HIV activity against HIV-1LAI in human peripheral blood mononuclear (PBM) cells ...

The synthesis of (1R,2S)- and (1S,2R)-1-amino-2-(hydroxymethyl)cyclopropanephosphonic acids was accomplished using different strategies. The (1R,2S)-stereoisomer could be efficiently obtained by the cyclopropanation of ethyl diethoxyphosphorylacetate with the cyclic sulfate derived from (S)-3-be...

The stereoselective synthesis of (1R,2R)- and (1S,2S)-trans-2-(diphenylmethylideneamino)cyclopropanecarboxylic acid has been accomplished in six steps starting from (2S)- and (2R)-β-benzyl N-(tert-butoxycarbonyl)aspartate, respectively. The key-step in the reaction sequence is a stereoselective...