Para Aminosalicylic Acid

The success of early clinical trials of PAS (Fig. 8; 2a) in TB patients [119] prompted synthesis of analogs to enhance the activity of the parent compound. These analogs showed that PAS exhibits very specific SAR [120].

The mechanism of action of PAS is not fully understood, although folate biosynthesis has been proposed as the target, since inactivation of thymidylate synthase confers resistance [121]. PAS is generally poorly tolerated in patients due to gastrointestinal disturbances often leading to discontinuation of PAS administration.

Free phenol Free acid required essential

Primary amine required -_h2N

Minimum pharmacophore

Fig. 8 SAR of p-aminosalicylic acid (PAS)

^-Aminosalicylic Acid (PAS] 2a

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