Objectives:
Thiophene is one of the most important heterocyclic scaffolds with notable
pharmacological properties. Thiophene and its derivatives are of particular interest among sulphurcontaining
heterocycles because of their similarities to numerous natural and synthetic compounds
with identified potential. The purpose of this study is to extensively analyse the synthetic pathways
adopted for synthesising thiophene derivatives and investigate their various biological functions.
Methods:
A comprehensive review of the existing literature was conducted to collect data pertaining
to the methods that are employed for the synthesis of thiophene derivatives. A comprehensive
search was carried out through relevant databases, including work published in 2024. A variety of
synthesis procedures were identified and arranged, encompassing both traditional approaches like
the Gewald reaction and contemporary ones like microwave-assisted synthesis and green synthesis.
In addition, a comprehensive compilation of in vitro and in vivo studies was conducted to investigate
the biological effects of 50 distinct thiophene derivatives. The primary focus of the studies was
on various activities such as anti-cancer, anti-inflammatory, antiprotozoal, antibacterial, antioxidant,
and antiviral functions.
Results:
Diverse methodologies have been employed in the synthesis of thiophene derivatives,
encompassing both conventional and modern methods. Furthermore, the biological potential of
thiophene derivatives was investigated, demonstrating a broad range of actions. Key structural elements
necessary for biological activity were clarified by investigations of the structure-activity
relationship.
Conclusion:
The biological potential and flexible synthesis pathways of thiophene derivatives
make them attractive candidates for use in medicinal and pharmaceutical chemistry. Understanding
the different synthesis methods and biological actions of thiophene derivatives may assist rational
design and create novel treatments for a variety of conditions. The potential for these compounds to
be further explored and optimised is considerable for the next drug development initiatives.
