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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.

Background A new series of thiophene analogues was synthesized and checked for their in vitro antibacterial, antifungal, antioxidant, anticorrosion and anticancer activities. Results A series of ethyl-2-(substituted benzylideneamino)-4,5,6,7-tetrahydrobenzo[ b ]thiophene-3-carboxylate derivatives were synthesized by using Gewald synthesis and their structures were confirmed by FTIR, MS and 1 H-NMR. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method, antiproliferative activity against human lung cancer cell line (A-549) by sulforhodamine B assay, antioxidant activity by using DPPH method and anticorrosion activity by gravimetric method. Conclusion Antimicrobial screening results showed that compound S 1 was the most potent antibacterial agent against Staphylococcus aureus, Bacillus subtilis , Escherichia coli and Salmonella typhi having MIC value 0.81 µM/ml and compound S 4 also displayed excellent antifungal activity against both Candida albicans and Aspergillus niger (MIC = 0.91 µM/ml) when compared with cefadroxil (antibacterial) and fluconazole (antifungal) as standard drug. The antioxidant screening results indicated that compound S 4 and S 6 exhibited excellent antioxidant activity with IC 50 values 48.45 and 45.33 respectively when compared with the ascorbic acid as standard drug. Anticorrosion screening results indicated that compound S 7 showed more anticorrosion efficiency (97.90%) with low corrosion rate. Results of anticancer screening indicated that compound S 8 showed effective cytotoxic activity against human lung cancer cell line (A-549) at dose of 10 −4 M when compared with adriamycin as standard.

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Aus den Phenylessigsäureaniliden (I) werden über die Amide (II) die Diaryl‐tetrahydroisochinoline (III) hergestellt, die ebenso wie eine Reihe ähnlicher Verbindungen wie (lW‐(VII) werden (zum Teil IR‐.