The synthesis and evaluation of 5α-reductase inhibitory activity of some 4-azasteroid-20-ones and 20-oximes and 3β-hydroxy-, 3β-acetoxy-, or epoxy-substituted C₂₁ steroidal 20-ones and 20-oximes having double bonds in the A and/or B ring are described. Inhibitory activity of synthesized compounds was assessed using 5α-reductase enzyme and [1,2,6,7-³H]testosterone as substrate. All synthesized c...

Libraries of 1-methyl-2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones/oximes/O-methyloximes 1-14/15-28/29-42 and 7-methyl-2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-ones/oximes/O-methyloximes 43-48/49-54/55-60 were synthesized and their stereochemistry was established by 1D/2D NMR spectral and single crystal XRD studies. All the synthesized oximes and oxime ethers were screened for their in vitro antimic...

The pharmacokinetics and cardiovascular pharmacodynamics of two oximes were studied in unanesthetized pigs. Effects of 2-[(hydroxyimino)methyl]-1-methylpyridinium chloride (pralidoxime chloride; 2-PAM Cl; 50 mumol/kg) were compared with those of 1,1-methylene bis[4(hydroxyiminomethyl) pyridinium] dichloride (methoxime; MMB-4; 100 mumol/kg). Cardiopulmonary parameters were monitored and plasma c...

A series of the novel oleandomycin 9-oximes has been prepared and characterized by spectroscopic data and X-ray analysis. The antibacterial in vitro activities of the oximes (6-10) were compared with that of oleandomycin (1). Among the novel derivatives the most active compound was 8(R)-methyloleandomycin-9-oxime (9) in contrast ot its 8(S)-isomer (10) which possessed only low potency. Some pre...

The use of organophosphorus pesticides results in toxicity risk to non-target organisms. Organophosphorus compounds share a common mode of action, exerting their toxic effects primarily via acetylcholinesterase (AChE) inhibition. Consequently, acetylcholine accumulates in the synaptic clefts of muscles and nerves, leading to overstimulation of cholinergic receptors. Acute cholinergic crisis imm...

Reactivation of organophosphate (OP)-inhibited acetylcholinesterase (AChE) by oximes is the primary reason for their effectiveness in the treatment of OP poisoning. Reactivation is reported to accelerate by quaternary ligands such as decamethonium, which is devoid of nucleophilicity. The mechanism of this enhancement is not known. To better understand the acceleration phenomenon, we examined li...

Erbium(III) complexes of 2-hydroxy-l,4-naphthalenedione-1-oxime and its C-3 substituted derivatives are synthesized and characterized by elemental analysis, thermogravimetric analysis, infrared spectroscopy, magnetic susceptibility measurements 2-hydroxy-1,4-naphthalenedione-1-oxime derivatives are analysed using (1)H and (13)C NMR spectroscopy. The molecular composition of the synthesized comp...

Inhibition of synaptic acetylcholinesterase (AChE) by organophosphate (OP) nerve agents is the main reason for their toxicity. Oximes are used as antidotes to reactivate nerve agent-inhibited AChE. To understand the mechanism of oxime-induced reactivation, we generated several mutant AChEs. Reactivation studies conducted with wild-type and mutant AChEs revealed that the peripheral anionic site ...

A rapid and accurate method for analyzing pyridinium oximes-N-methylpyridinium2-aldoxime chloride, N,N’-trimethylene-(pyridinium-4-aldoxime) dihalide, and N,N’oxydimethyl(pyridinium-4-aldoxime) dich bride-in plasma, urine, and whole blood is described.The method is completely automated and requires small sample volumes. Concentrations ranging from 3 to 120 Eq./L. in biologic fluids can be deter...