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Pyrazolone (pyrazolonderivatives) drugs include antipyrine, aminopyrine, analgin, isopropylantipyrine, phenylbutazone, and oxycloth Oxyphenb-utazone, feprazone, etc.
, have antipyretic, analgesic, anti-inflammatory and anti-rheumatic effects
.
As early as 1884, antipyrine has been published as an antipyretic, analgesic and anti-inflammatory drug.
14.
1.
1 Physical and chemical properties and uses
14.
1.
1.
1 Physical and chemical properties
Among the pyrazolones, aminopyrine, analgin, butazepine, oxybutazone, etc.
are all derivatives of antipyrine, and the basic structure is a cyclic compound (pyrazolone) with extended aniline side chain.
According to the different positions of the carbonyl group and hydrogen on the pyrazole ring, it is acidic or basic
.
The metabolites of aminopyrine, antipyrine and diazepam are alkaline; phenylbutazone and oxybutazone are acidic because the 3,5-dicarbonyl group of the pyrazole ring enhances the hydrogen at the 4th position
Figure 14-1 The general structure of pyrazolone drugs
Table 14-1 Pyrazolone drugs and their metabolic physicochemical properties
14.
1.
Pyrazolone drugs can inhibit the synthesis and release of hypothalamic prostaglandins, restore the normal responsiveness of the body temperature regulation central sensory neurons, and have an antipyretic effect; at the same time, they can also have an analgesic effect by inhibiting the synthesis of prostaglandins
.
Aminopyrine can also inhibit the synthesis and release of prostaglandins in inflammatory local tissues, stabilize the lysosomal membrane, affect the phagocytosis of phagocytes, and play an anti-inflammatory effect
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