Roles of Fluorine in Drug Design and Drug Action

2019 ◽  
Vol 16 (10) ◽  
pp. 1089-1109 ◽  
Author(s):  
Satya Prakash Gupta
Keyword(s):  
Hydrogen Bond ◽  
Fluorine Atom ◽  
Steric Effect ◽  
Drug Action ◽  
Receptor Interaction ◽  
Drug Molecule ◽  
Hydrogen Bond Interactions ◽  
Life Threatening ◽  
Drug Receptor ◽  
Drug Receptor Interaction

The article discusses the basic properties of fluorine atom that have made it so useful in drug development. It presents several examples of therapeutically useful drugs acting against many life-threatening diseases along with the mechanism as to how fluorine influences the drug activity. It has been pointed out that fluorine, due to its ability to increase the lipophilicity of the molecule, greatly affects the hydrophobic interaction between the drug molecule and the receptor. Because of its small size, it hardly produces any steric effect, rather due to electronic properties enters into electrostatic and hydrogen-bond interactions. Thus, it greatly affects the drug-receptor interaction and leads to increase the activity of the drugs.

scholarly journals Computer-Controlled Muscle Paralysis with Atracurium in the Sheep

1986 ◽  
Vol 14 (1) ◽  
pp. 7-11 ◽  
Author(s):  
D. G. Lampard ◽  
W. A. Brown ◽  
N. M. Cass ◽  
K. C. Ng
Keyword(s):  
Infusion Rate ◽  
Recovery Time ◽  
Neuromuscular Transmission ◽  
Receptor Interaction ◽  
Muscle Paralysis ◽  
Observed Behaviour ◽  
Integrated Electromyogram ◽  
Computer Controlled ◽  
Drug Receptor ◽  
Drug Receptor Interaction

Paralysis was maintained in sheep by computer-controlled infusion of atracurium, using the integrated electromyogram as a measure of neuromuscular transmission. A number of experiments were conducted to ascertain the average infusion rate required to achieve a given level of paralysis for one hour. Each experiment yielded a point on a plot of paralysis versus infusion rate. A dose-response curve based upon a simple model of drug receptor interaction at the neuromuscular junction was fitted to the experimental points by least squares and is able to provide a useful explanation of clinically observed behaviour. The recovery time was also measured in each experiment and plotted against both prior level of paralysis and prior average infusion rate.

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