Benzoic Acid and Aniline Analogues with Potential Local Anaesthetic Profile

It fact, the esters of benzoic acid derivatives are derived from cocaine, while the amides of aniline derivatives are obtained from isogramine. 

The following general arrangement holds good with regard to the chemical structures of esters and amides  

however, pertinent to mention here that the ester as well as the N-substituted functional moieties are nothing but bioisosteres as illustrated below and it further expatiates and justifies the strategical presence of such groups in almost identical locations in the various tailor-made structurally designed local anaesthetics. 

Salient Features The various salient features influencing the functional moieties vis-a-vis the lipophilic and hydrophilic characterstics of the local anaesthetics are enumerated as under  

It is vehemently assumed that the local anaesthetics get bound to various tissue and plasma proteins by means of three vital physical forces, namely Van der Waals forces dipole-dipole attractions and electrostatic forces as illustrated below in Fig. 5.1. 

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BENZOIC ACID AND ANILINE ANALOGUES WITH POTENTIAL LOCAL ANAESTHETIC PROFILE ... 

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