(R)-N-(2-Heptyl)-N-methyl-propargylamine (R-2HMP) and (R)-N-(2-heptyl)-propargylamine (R-2HPA) are analogs of R-deprenyl. R-Deprenyl, a selective monoamine oxidase B inhibitor, is a mechanism-based inactivator of purified CYP2B1. The aim of the present study was to determine whether R-2HMP and R-2HPA behaved like deprenyl with respect to inhibiting cytochrome P450 (CYP450) enzyme activity. The ...

A series of cyclic 2,6-bis-(1,2,3-triazolyl)-pyridine anion receptors with thiourea functionalities were synthesized by click reaction of 2,6-diazidopyridine with protected propargylamine followed by condensation of a bisthiocyanate derivative with a series of diamines. Their chloride binding affinities as well as their transport properties in POPC bilayers were examined. These receptors were f...

Rasagiline (Azilect) is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, rasagiline binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. Therapeutic doses of the drug which inhibit brain MAO-B by 95% or more cause minimal inhibition of MAO-A, ...

A new 1D chained Ca(II) coordination polymer—namely, [CaL2(H2O)2]n (HL = 3,5-bis(4-pyridylmethoxy)benzoic acid)—was synthesized though the reaction of Ca(ClO4)2·4H2O, 3,5-bis(4-pyridylmethoxy)benzoic acid and NaOH in H2O/CH3CH2OH (v:v = 1:2) solution. Its structure was determined by elemental analysis, infrared spectrum, and single-crystal XRD. Structural analyses show that each Ca(II) ion is e...

Highly active Cu (II) complex with 1,4-dihydroxy anthraquinone as a cheap and accessable ligand could be used as a catalyst for the preparation of structurally different propargylamines from a one-pot, three-component reaction of terminal alkynes, aldehydes, and secondary amines with high yields under solvent-free conditions. The 1,4-dihydroxy anthraquinone is a very efficient Cu(II) scavenger ...

Synthesis, characterization, and properties of new thermally curable polysulfone containing benzoxazine moieties in the side chain were investigated. First, chloromethylation and subsequent azidation processes were performed to form polysulfone containing pendant clickable azide groups. Independently, antagonist 3,4-dihydro-3-(prop-2-ynyl)-2H-benzoxazine was prepared by using paraformaldehyde, ...