1. Sulphonamide drugs and their mechanism
Submitted by: Hassan khalid 3216
Submitted to: Dr. Afzal qamar
2. • Gerhard Domagk (1895–1964) discovered
• sulfa drugs in 1935.
• Mietzsch and Klarer for Domagk to test
were some related to the azo dyes. They
had the characteristic -N=N- coupling of azo dyes, but
one of the hydrogens attached to nitrogen had been
replaced by a sulfonamide group.
• In 1931 the two chemists presented a compound (KL 695)
that, although it proved inactive in vitro, was weakly active
in laboratory mice infected with streptococcus.
History
3. • The chemists made substitutions in the structure
of this molecule and, several months and
35 compounds later, produced KL 730, which
showed incredible antibacterial effects on diseased
laboratory mice. It was named prontosil rubrum and
patented as Prontosil.
• Among the early patients was Domagk’s own six-year-old
daughter, Hildegard, who had contracted a severe
streptococcal infection from an unsterilized needle.
Prontosil-the first sulfonamide drug
4. • Sulfonamides (sulphonamides) are a group of
man-made (synthetic) medicines that contain the
sulfonamide chemical group. They may also be
called sulfa drugs.
or
• The sulfa-related group of antibiotics, which are
used to treat bacterial infection and some fungal
infections.
What are sulfonamides
9. Sulfonamides structurally resemble p-
aminobenzoic acid (PABA), a precursor in
bacterial DHF synthesis. As false substrates,
sulfonamides competitively inhibit utilization of
PABA, and hence DHF synthesis. Because most
bacteria cannot take up exogenous folate, they are
depleted of DHF.
Mechanism of Action
