Especially from BCS IV drugs. I need some drugs list for aminoacid prodrug. I would like to have some example of drugs list for prodrug aminoacid derivatives to synthesis.
Dear Sir. Concerning your issue about the drugs list for aminoacid derivatives prodrug from BCS IV drugs. Prodrugs are biologically inactive agents that upon biotransformation in vivo result in active drug molecules. Since prodrugs might alter the tissue distribution, efficacy and the toxicity of the parent drug, prodrug design should be considered at the early stages of preclinical development. In this regard, natural and synthetic amino acids offer wide structural diversity and physicochemical properties. Amino acids are transported by multiple transporters with overlapping substrate specificities, and Naþ-independent neutral amino acid transporter, LAT1 (SLC7A5), transports L-type large neutral amino acids with branched and aromatic side chains such as leucine (Leu), isoleucine (Ile), phenylalanine (Phe), methionine (Met), tyrosine (Tyr), histidine, tryptophan (Trp), and valine (Val). LAT2 (SLC7A6) has also broad substrate specificities and transports L-isomers of neutral alpha-amino acids such as Tyr, Phe, Trp, threonine, asparagine, Ile, cysteine, serine (Ser), Leu, Val, and glutamine (Gln) with a high affinity and histidine, alanine (Ala), Met, and glycine (Gly) with a low affinity. LAT1 and LAT2 transport also several exogenously synthesized drugs such as L-dopa, alphamethyldopa, melphalan, and gabapentin. LAT1 protein is abundant in the colon, and its abundance markedly decreased at the level of jejunum and ileum. In contrast, LAT2 exhibits relative homogeneous presence across the digestive tract in human and rat intestine. When these LAT substrate drugs were taken with foods, the oral bioavailability is significantly reduced. I think the following below links may help you in your analysis:
I have gone through your answer thank you for spending enough time to answer.
I would like to know some example of drugs which can react with amino acids thereby enhancing its physicochemical properties viz solubility, stability and also bioavailability enhancement. I have already done work on repaglinide which has acid functional group reacts with glycine. like wise i would like to know some more examples of drugs.