Abstract
Thiophene and its substituted derivatives are very important class of heterocyclic compounds which shows interesting applications in the field of medicinal chemistry. It has made an indispensable anchor for medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules. It has been reported to possess a wide range of therapeutic properties with diverse applications in medicinal chemistry and material science, attracting great interest in industry as well as academia. It has been proven to be effectual drugs in present respective disease scenario. They are remarkably effective compounds both with respect to their biological and physiological functions such as anti-inflammatory, anti-psychotic, anti-arrhythmic, anti-anxiety, anti-fungal, antioxidant, estrogen receptor modulating, anti-mitotic, anti-microbial, kinases inhibiting and anti-cancer. Thus the synthesis and characterization of novel thiophene moieties with wider therapeutic activity is a topic of interest for the medicinal chemist to synthesize and investigate new structural prototypes with more effective pharmacological activity. However, several commercially available drugs such as Tipepidine, Tiquizium Bromides, Timepidium Bromide, Dorzolamide, Tioconazole, Citizolam, Sertaconazole Nitrate and Benocyclidine also contain thiophene nucleus. Therefore, it seems to be a requirement to collect recent information in order to understand the current status of the thiophene nucleus in medicinal chemistry research.
Highlights
Heterocyclic compounds are extensively distributed in nature and have versatile synthetic applicability and biological activity which helped the medicinal chemist to plan, organize and implement new approaches towards the discovery of novel drugs [2]
The results showed the importance of the carbon–nitrogen bond in biological systems because of which antimicrobial activities for these N-containing compounds were reported
All the synthesized compounds were screened for their antibacterial and antifungal activities against various microbes such as B. subtilis, E. coli, P. aeruginosa and C. albicans by the cup-plate agar diffusion method
Summary
As the world’s population is increasing at an alarming rate, health problems have become a very serious clinical problem. Heterocyclic compounds are extensively distributed in nature and have versatile synthetic applicability and biological activity which helped the medicinal chemist to plan, organize and implement new approaches towards the discovery of novel drugs [2]. Thiophene was discovered as a contaminant in benzene [4] It has the molecular mass of 84.14 g/mol, density is 1.051 g/ml and Melting Point is − 38 °C. Biological activities of thiophene derivatives Thiophene nucleus containing compounds show various activities like for example 1-[1-(2,5-dimethylthiophen3-yl)ethyl]-1-hydroxyurea (1) act as an anti-inflammatory agent; the maleate salt of 1-(2,5-dimethylthiophen-3-yl)3-(5-methyl-1H-imidazol-4-yl)propan-1-one (2) work as serotonin antagonists and is used in the treatment of Alzheimer’s disease.
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