Thiophene derivatives in medicinal chemistry

Likewise, benzo[6]thiophenes have also been the subject of several biologically oriented studies. The structurally rather simple sulfonamide 100 was identified as a carbonic anhydrase inhibitor 05BMCL4872 , whereas methanesulfonate salts of the guanidine derivatives lOI displayed cardioprotective activity 05BMCL2998 . A series of 5-amidinobenzo[6]thiophene derivatives have been identified as dual inhibitors of factors IXa and Xa 05BMCL29 . The 

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Thiophene-containing molecules can be found in both natural products and synthetic chemotherapeutics. Bithiophene 1, a naturally occurring nematocide, is isolated from the roots of Echinops spaerocephalus, whereas tiaprofenic acid, an anti-inflammatory agent, is a synthetic thiophene derivative. Moreover, thiophene is a useful template for four-carbon homologation via reduction [1], as well as a bioisostere of the benzene ring and other heterocycles in medicinal chemistry. 

The coupling of thiophene derivatives, particularly thiopheneboronic acids, is frequently employed in medicinal chemistry and also in materials science. In a recent example 2-thiopheneboronic acid was coupled with a triazolopyridine derivative (6.4.) in the presence of [1,1-bis(diphenylphosphino)ferrocenyl]palladium dichloride in 83% yield6... 

Much of the current interest in benzo[ ]thiophene chemistry owes its origins to the wide range of biological and other activities shown by many of its derivatives. In medicine, benzo[ ]thiophene derivatives have been patented as laxatives,7 contraceptives,8 and antiinfluenza agents.9 In... 

THIOPHENE, SELENOPHENE, ANDTELLUROPHENE DERIVATIVES IN MEDICINAL AND ENVIRONMENTAL CHEMISTRY... 

The large number of reports pertaining to the synthesis of thiophene and its derivatives corroborates the continuing intrigue and importance of these compounds in biology, chemistry, industry, and medicine <88H(27)1731, 91FOR87, 91HC(44/4)397>. 

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