Pharmacologically Active Compounds and other Thiophene Derivatives

Literature data on thiophene structure-activity relationships of the last 10 years are reviewed. With regard to the broad spectrum of molecular structures the investigated compounds have been arranged according to their various therapeutic properties as indicated by the specific biological test systems. The interchange with the thiophene ring included mainly the following aromatic ring systems: benzene naphthalene, furan, pyndine, thiazole, pyrrole, and the respective indole, benzofuran, and benzthiazole analogs. Summarizing these findings it can be concluded that no general activity pattern can be given. Neither the exchange of the 2-thienyl moiety by the 3-thienyl nor the replacement of the thiophene ring by various aromatic rings resulted in a consistent superiority of any of the molecular structures.

Structure-Activity Relationships of Thiophene Derivatives of Biological Interest

Among a large variety of parasitic diseases caused by the invasion of the human body by a number of bacteria, fungi, viruses, protozoa and helminths, the helminth infections undoubtedly constitute a major medical and public health problem all over the tropical and subtropical regions of the world. Despite significant advances made in the treatment of helminth diseases, the rate of incidence of these infestations has not satisfactorily declined. This is primarily because these are basically the diseases of poor masses where inappropriate sanitation, low living standards, and lack of health education along with ideal environmental conditions for the survival and replication of the parasites facilitate the dissemination of infections. Another major reason for the wide spread of helminthiasis is that, earlier, it was not considered to be involved with higher risks of morbidity and mortality, and hence, was unable to draw the attention of medicinal chemists, parasitologists and medical and health personnel. However it was soon realized that the high worm burden on the population is not only responsible for several grave clinical complications but also greatly hampers the socioeconomic growth of the tropics by causing malnutrition and physical disability which finally leads to decreased working capacity in the people carrying helminth parasites. Furthermore, the presence of helminths in domestic animals induces less production of milk, fat, meat and wool, and thus, influences the economy of agricultural and dairy countries of the world

Treatment of helminth diseases — challenges and achievements

Reaction of enamines with semicarbazone-based amidoalkylating reagents: A straightforward synthesis of annulated 1-aminopyrimidin-2-one derivatives

Chapter 10 - Nitroaryl Compounds

A series of nitrothiophene compounds, with activity against Schistosoma mansoni in mice, is described and shown to be more effective than the corresponding nitrofurans.

Nitrothiophenes with schistosomicidal activity.

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Nitrothiophenes with schistosomicidal activity.