Current Medicinal Chemistry - Volume 13, Issue 1, 2006

Imidazoles are an important class of heterocycles and include many substances of both biological and chemical interest. They are part of a large number of highly significant biomolecules such as the essential amino acid histidine and related compounds, biotin, and the imidazole alkaloids. Insertion of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole drugs have broad applications in many Read More

The β3-adrenergic receptor (β3-AR) has been shown to mediate various pharmacological and physiological effects such as lipolysis, thermogenesis, and relaxation of the urinary bladder. Activation of the β3-AR is thought to be a possible approach for the treatment of obesity, type 2 diabetes mellitus, and frequent urination. Therefore, the β3-AR is recognized as an attractive target for drug discovery. On the other hand, activa Read More

Invertebrate animals, such as sponges, tunicates and bryozoans, are among the most important sources of biomedically relevant natural products. However, as these animals generally contain only low quantities of the compounds, further pharmacological development is in most cases difficult. There is increasing evidence that many metabolites, in particular polyketides and nonribosomally synthesized peptides, are not produce Read More

Heptahelical receptors are coupled to heterotrimeric GTP-binding proteins (G-proteins) which transduce most signals through their α and βγ subunits to effectors, enzymes and ion channels. Of the 367 heptahelical receptors for endogenous ligands, about 330 are potential targets for drug discovery with agonist, antagonist or inverse agonist properties. The term G-protein-coupled receptors (GPCRs) is a broader functio Read More

Among the strategies that can lead to the discovery of new drugs, the identification and use of privileged structures, molecular fragments that are able to interact with more than one target, gained particular attention, in an attempt to find new drugs in a shorter time with respect to other strategies. These structures, that have been identified mainly by empirical observations, can target only a given protein family, or can b Read More

Resveratrol (3,4',5-trihydroxystilbene, RESV) is a natural phenolic compound that exists as cis and trans isomers [c-RESV or (Z)-RESV and t-RESV or (E)-RESV, respectively]. t-RESV is a natural component of Vitis vinifera L. (Vitaceae), abundant in the skin of grapes (but not in the flesh) and in the leaf epidermis, and present in wines, especially red wines. In in vitro, ex vivo and in vivo experiments t-RESV exhibits a number of biologi Read More

The sol-gel process is an inorganic polymerization process taking place in mild conditions, allowing the association of mineral phases with organic or biological systems. The possibility to immobilize drugs, enzymes, antibodies and even whole cells without loss of their biological activity led to the development of diagnostic tools, drug delivery carriers as well as new hosts for artificial organ design. These systems take profit from th Read More

The number of people with diabetes is expected to rise from the current estimated 150 million to 220 million in 2010 and 300 million in 2025, and 90% is Type 2 diabetes or non-insulin dependant diabetes mellitus (NIDDM). Voglibose, one of the most important α-glucosidase inhibitors, delays the digestion and absorption of carbohydrates, thereby inhibiting postprandial hyperglycemia and hyperinsulinemia, and is the aid in the Read More