Synthesis and Biological

Activities of Pyrazole
derivatives
By
Ahmed Basem chloope
Supervised by
Sawsan Kudeaier Abass
 Research objective
Shedding light on the methods of preparing pyrazoles
derivates , as well as focusing on environmentally friendly
methods of preparation, also review the pharmacological
importance.
Abstract

• Pyrazole and its derivatives can be prepared in their ways and

other environmentally friendly ways as well as used in
pharmaceutical as anti-inflammatory, anti-obesity, antidepressant,
Antianxiety, Anticancer.
 Pyrazole
• Pyrazoles are five-membered
heterocycles aromatic compound with
two adjacent nitrogen atoms
C3H3N2H.

• Pyrazole under goes electrophilic

substitution.

• The presence of the Pyrazole nucleus

in different structures leads to
diversified applications in different
areas such as technology, medicine
Figure 1-structure of Pyrazole
and agriculture.
Preparation of Pyrazole derivatives

1- Classical methods

involve approaches based either on the condensation of hydrazine

with 1, 3-dicarbonyl compounds or 1, 3-dielectrophiles, like Knorr
synthesis, diazoles. In 1883 Knorr was the first to synthesize the
first compound derived from Pyrazole. Condensation of hydrazines
with 1,3-dicarbonyl compounds is the classical method for the
synthesis of Pyrazole
Scheme1- Knorr synthesis
2- Green chemistry method

Green chemistry provides alternative synthetic pathway

for prevention of pollution in the utilization of set of
principals that reduces or eliminates the use or
generation of hazardous substances in the design,
manufacture, and application of chemical products or
processes

Scheme 2. General procedure for the synthesis of Pyrazole systems in the presence of
TBAB at room temperature
Biological activity

• Pyrazole and its derivatives are one of the

best and promising drug candidates. They
are anti-inflammatory, anti-microbial,
anticancer, anti-angiogenic, antiviral,
antioxidants neuroprotective, hypoglycemic
agents and platelet aggregation inhibitors

Figure 2. Pyrazoles and their biological

activities.
 Curcumin-3,4-Dichloro Phenyl
Pyrazole (CDPP)
could be used as a potential drug
candidate against adipogenesis
Fezolamineis used as an
antidepressant drug