represents an approach used by the medicinal chemist for the rational modification Keywords: Bioisostere, Isostere, Drug design, Replacement, Pseudoatoms. + + Chem. Rev. , 96, − Bioisosterism: A Rational Approach in Drug Design George A. Patani and Edmond J. LaVoie* Department of. Pharmacologyonline 1: () ewsletter Bhatia et al. A Review on Bioisosterism: A Rational Approach for Drug Design and Molecular Modification.

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Benz[e]- indole 67, Figure 63the pyrrolo analogue of the Figure Previ- ous research has very effectively illustrated the 5. The use of this replacement in the design of novel Figure 7.

Structure-Activity Relationships of the Benzophenone Nucleus. In this example of bioisosteric replacement, pharmacological activity was retained.

The correct use of the strategy of molecular modification also allows the identification of new classes of lead compound with attractive pharmacotherapeutic activity, maximizing the chances for success in discovering medications both more efficient and of safer use, minimizing the efforts of synthetic work.

Conclusion Bioisosterism represents a successful strategy in rational drug design, useful in molecular modification and design of new therapeutically attractive drug substances of different pharmacological deisgn. Substitution D-ribofuranosyloxazolecarboxamide oxazofurin, with the different divalent isosteres including sele- 55a.


The methylsulfonimide, however, To illustrate the applicability of these replace- was only one-tenth as active as the carboxylic acid ments, the literature outlines a systematic structure- derivative 90e, Table One such replacement of the ester group is a heterocycle. Isomorphism, Isosterism and Covalence. Examples of various atoms and molecules are [8]: Activity of Certain Synthetic Compounds.

J Am Chem Soc ; Carbonyl Group Bioisosteres common acceptor nucleus on the dopamine recep- Carbonyl group bioisosteres for the purposes of this tor. Oxophenarsine metabolite of arsphenamine contribute to its activity against the syphilis organism. Ring [33] bioisosterism, is the most frequent relationship in drugs of different therapeutic classesas can be seen in Fig.

Cancer Res ; Retin- Boyd, S.

Bioisosterism: A Rational Approach in Drug Design | javier vera –

Phar- DeFronzo, R. These similarities based on electronic and conformational aspects as well as the physicochemical properties such as p Ka and log P. Quaternary Ammonium Functional Groups.

Cyclic Carbamate Analogues of Pilocarpine.

Bioisosterism: A Rational Approach in Drug Design.

An example is illustrated by guanosine analogues having a monovalent isosteric replacements. In many instances, SO2CH3 0. A number atom with stronger electron-withdrawing groups of less known replacements have not been reviewed such as the cyano or the trifluromethyl resulted in because of their inability to demonstrate bioisoster- less potent analogues Table Inhibition of angiotensin II formation occurs by inhibition of endothelial angiotensin-converting enzyme ACE.


Novel Potassium 4- 3,4-Disubstitutedphenyl pyridines and Derivatives Thereof.

Replacement of the hydroxyl with an amino group resulted in more potent activity toward 5-LO while the potency toward CO remained the same. Divalent Booisosterism Involving Double pursuing graduate studies in pharmaceutics.

J Pharm Sci ; With the pair of corticos- teroids with a methyl substituent Z CH3replacement of hydrogen with fluorine at the 9R position, 3d, also increased anti-inflammatory activ- ity relative to 3c.

Rotationally Restricted Mimics of Rigid Molecules: This short duration of action retention of biological activity. Molar refractivity is an index of relative size.

P-aminosulfanilamide 42an active metabolite of Prontosil which was able to provide cures of streptococcal infections in mice revolutionized chemotherapy and on later elucidation of its mechanism of action shows similarity of its structure with p-aminobenzoic acid PABA, This study, for example, did provide insight interchange and the hydroxyl-amino interchange into structural features which were critical to their was discussed previously.

Synthesis and Anti-inflammatory Activity of Subasinghe, N.