Drug biologically active molecule

The isosteric relationship of benzene and thiophene has often led medicinal chemists to substitute the sulfur containing heterocycle for benzene drugs in biologically active molecules. That this relationship has some foundation in fact is attested by the observation that the resulting analogs often possess full biologic activity. Alkylation of the diamine, 71 (obtained from aniline and the chloroethylamine), with 2-chloromethylthiophene affords the antihistamine methaphenylene (72) The correspond-... 

Halloysite was found to be a viable and inexpensive nanoscale container for the encapsulation of biologically active molecules and drugs as was first demonstrated by Price et al. [5-8]. Its physicochemical characterization as a novel drug delivery system was also reported by Levis and Deasy et al. [9,10], who further demonstrated the controlled release of diltiazem hydrochloride and propanol hydrochloride... 

He is an author of more than 150 papers published in international scientific journals. His scientific interests cover the synthesis of biologically active molecules and the development of new methodologies directed to synthesis automation applied to drug discovery and drug optimization. 

Since the origin, the most efficient source of drugs and biological active molecules is Nature. As reported by Newman and Cragg in a recent review [1], at least 25-30% of New Chemical Entities (NCE) going under study for pharmaceutical and clinical applications are primarily derived from Nature (N) or Natural Derived (ND), while only 30% are merely synthetic, as reported in Figure 2. 

Integral proteins include receptors for hormones and other biologically active molecules, including a great many drugs employed in human medicine. Included are carriers for molecules that the cell needs but that would otherwise be excluded from it by the lipid bilayer and channels for ions that must get in or out of the cell. Finally, integral proteins act as signaling devices to other cells in the environment. 

Synthesis of unusual amino acids, peptidomimetics, synthetic enzymes, and new drugs containing (5-lactam rings as an integral part of their structure, has currently renewed interest worldwide in this four-membered heterocycle [52-54]. Furthermore, the appropriately substituted and configured(5-lactam frameworks now constitute effective tools for the incorporation of a wide variety of both (5- and a-amino acids in short peptide segments of various biologically active molecules. 

Characterisation of the structure and conformation of small biologically active molecules is part of the standard approach to lead generation in drug design studies. In particular, it is now possible to automatically synthesise many thousands of small molecules and then rapidly measure their effects in a given pharmacological test system. The power of such techniques comes from the immense number of compounds which can be generated and screened for activity. Two studies have evaluated HPLC-NMR in the field, one based on a mixture of 27 closely related tripeptides [24] and the other on two separate mixtures of four aromatic compounds and three pentapeptides [25]. 

Initially, the purpose was to synthesize sila-analogs of known drugs for comparison of their efficiency and to get information on the mechanism of their action.475 As investigations continued, an increasing number of biologically active molecules appeared. Perhaps the best known of these molecules are the silatranes, compounds that have no analogous carbon counterpart.476... 

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