Rational Design of Alkylene-Linked Bis-Pyridiniumaldoximes as Improved Acetylcholinesterase Reactivators

Cholinesterase reactivation in vivo with a novel bis-oxime optimized by computer-aided design.

Recently, several bis-pyridiniumaldoximes linked by a variable-length alkylene chain were rationally designed in our laboratories as cholinesterase reactivators. Extensive in vitro tests of these oximes with acetylcholinesterase inhibited by two different organophosphate agents, echothiophate and diisopropylfluorophosphate, revealed one compound with particularly good reactivation kinetics and ...

Alkylene-bis-isothiocyanates: Novel Insect Growth Regulators

In search for selective anti-insect agents some monoand bis-isothiocyanates were prepared and tested on third instar larvae of Manduca sexta. The alkylene-bis-isothiocyanates 4, 5 and 6 had a novel effect preventing formation of the abdominal spiracles and of the hooks (crochets) at the following molt to the 4th instar. Some of these larvae died in the molt, while spiracles remained absent also...

In vitro Evaluation of New Acetylcholinesterase Reactivators as Casual Antidotes against Tabun and Cyclosarin

Rational Design of Improved Pharmabiotics

Herein we review the most recent advances in probiotic research and applications with particular emphasis on the novel concept of patho-biotechnology: the application of pathogen-derived (ex vivo and in vivo) stress survival strategies for the design of more technologically robust and effective probiotic cultures with improved biotechnological and clinical applications.

Docking Studies, Synthesis, and In-vitro Evaluation of Novel Oximes Based on Nitrones as Reactivators of Inhibited Acetylcholinesterase

Acetylcholinesterase has important role in synaptic cleft. It breaks down the acetylcholineatcholinergic synapsesand terminates the cholinergic effects. Some chemical agents likeorganophosphorus compounds (OPCs) including nerve agents and pesticides react withacetylcholinesteraseirreversibly. They inhibit normal biological enzyme action and resultin accumulation of acetylcholineand show toxic e...