There have been new developments in the field of medical science
and usage of organic chemistry. The synthetic methodology used in the process
of preparing organic compounds is one of the most important discoveries and
innovation taken place in the recent decades. It's very objective in the modern
times is to provide better medicines and cure through new and possible drugs
for different diseases.
Since soluble polymers combines the benefits of classical homogeneous solution methodology with those of solid phase organic synthesis (SPOS);
1- it uses excessive reagents, easy isolation and purification of the final product with a higher stability of the system polymer-supported molecule.
2- Polyethylene glycol (PEG) with Mw=5000Da, is by far the most widely soluble support employed. Polyethylene glycol is one of the expensive polymer and ideal support for liquid phase combinatorial synthesis because it is easy to functionalize and also resistant to drastic operative conditions.
4- Furthermore, Polyethylene glycol dissolves easily in many organic solvents such as CH2CI2, CHCI3, tetrahydrofuran (THF), CH3OH, or H2O within the room temperature and it can be precipitated from solution by adding diethyl ether, tert-butyl methyl ether, propan-2- ol, or hexane.
5- Because of these features, PEG chemistry has shown a broad based application, which maybe in large part assigned the use of PEG where it conjugates to deliver drug, Oligonucleotides or enzymes.
6- The liquid phase peptide synthesis method is known for more than 25 years and it has been broadly applied to the synthesis of small organic molecules and combinatorial chemistry.
7- On the other hand, compound derived from 1, 3, 5 thiadiazinane-2- thiones (THTT) has received specific attention because of its pharmacological properties. It is best known that THTT present antibacterial activities which are obtained in compounds having lipophilic groups at the N-3 and hydrophilic ones at N-5 position that helps in liquid phase peptide synthesis.
8- It is to be considered that promising results are obtained with antiparasitic bioactivity with THTT derivates which shall be attributed to the interaction of cystenine proteinases, present in most groups of parasitic protozoa, with isothiocyanates, generated by hydrolysis of the THTT ring in protic medium.
9- Notwithstanding, it shall not be ruled out, it is very much possible that the rleased amino acids or dipeptide attached to N-5 of THTT ring, with other molecular targets, thereby enhances the antiparasitic activity as observed with these derivatives, should not be ruled out.
In previous studies, it is found that cytotoxicity has remarkable properties of derivatives against HeLa and HT-29 cells were also tested, and there are developed theoretical model to predict the influence of structure on the antitumor activity for this type of compounds which helps in Liquid phase peptide synthesis.
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