Thiazolidinone its solubility and therapeutic activity can be

Thiazolidinone derivatives exhibits
less pharmacological activities on account of their little solubility in polar
solvent like water. The formation of inclusion complex of thiazolidinone makes
the augmentation of solubility and therapeutic potential in an noticeable amount.
In an encapsulation of compound with ?-cyclodextrins, its solubility and
therapeutic activity  can be enhanced
significantly. The analytical data  of  the synthesized compounds and their inclusion
complexes are depicted in Table-I and likely the spectral data are shown in
table–II. Analysis of    the
spectral characteristics and elemental sulphur composition evidences formation  of compounds and their inclusion complexes.  

                The melting point of the
compounds K and its inclusion complex are 202oC and 208oC,
the melting point of the compounds L and its inclusion complex are 161oC
and 168oC and the melting point of the compounds M and its inclusion
complex   are 135oC and 144oC
 respectively .The changes in melting
points of the inclusion complexes with their respective compounds  indicates its 
inclusion complex formation with ?-cyclodextrin. It due to some  that extra amount of thermal energy is essential
to bring the molecules out of the hollow space of the ?-cyclodextrin. Colours
like brownish red, deep yellow and dull brown are formed by synthesised  compounds 
 of K ,L and M . In the same way
the colour of their corresponding inclusion complex shows light yellowish,
brownish yellow and pale yellow respectively. The percentage of yield of
inclusion complexes are more in case of compound M.

We Will Write a Custom Essay Specifically
For You For Only $13.90/page!

order now

 The presence of
C-S,C-C,C-N,C=O,C-H, and N-H in the compound as expected  due to the IR spectra is formed at the region
of 667,1282,1595,1728 ,2960 and 3111 cm-1.Similarly the IR data of
inclusion complexes of K show characteristics absorption at
750,1246,1597,1730,2962 and 3315 cm-1 indicating the presence of

O,C-H and N-H bonds  in the compounds.  Likewise L and M compounds and their inclusion
complexes are found to be absorbed at the proper characteristic frequency as
given in table-II. The peaks of IR spectrum become broader, weaker and smoother
and the IR frequencies (C=O) undergo downward shift. But the frequency
undergoes a shift towards higher wave number after inclusion complex formation
in case of NH stretching vibration. The development of weak interaction like
H-bonding, Vannder Waals forces, hydrophobic interactions in between the host
and guest molecules19,20 leads to all these changes evidently demonstrate
transference of compounds into the cavity of ?-cyclodextrin .UV spectra of the
compounds and their inclusion also reveals that there is a small increase in
value after the formation of inclusion complex. The ? values of the inclusion
complexes are having low value as compare to their respective compounds from
which they are formed. This indicates that PMR signals are shifted towards up
field in the inclusion complex on account of the notable shielding factor which
arises through encapsulation within the cavity of ?-cyclodextrin.

                  With increasing concentration of
?-cyclodextrin solubility of these compounds increase linearly which can be
determined from aqueous phase solubility study. The stoichiometry of these
complexes may be 1:1 on account of  
slopes of all the plots were less than unity. By using Benesi-Hilderband
relation 19,the thermodynamic stability constants (KT) of
inclusion complexes were determined.Good linear correlations were obtained for
a plot of inverse of ?A verses inverse of  ?- CDo for compounds . The values
of KT for all the complexes were calculated with using the formula
of KT = Intercept/Slope. Subsequently, the KT values of
the inclusion complexes of compounds with ?- Cyclodextrin were found to be
313,295 and 276 M-1 respectively (Table 3). Which were remain within
100 to 1000 M-1(ideal values) representing substantial stabilities
for the inclusion complexes through host-guest interaction like vannder Waal’s
force, hydrophobic interaction etc. 20,21   The
interaction of the compound with ?-cyclodextrin for 1:1 stoichiometry were calculated
by determining stability constant (KT  values) with the help of thermodynamic
parameter at different temperatures.With increase in temperature  KT 
values were found to be decreasing.

antibacterial studies shows the diameter of 
zone of inhibition obtained by the compounds and their corresponding
inclusion complexes are given as in the figures (3,4,5).The test has been
carried by taking three bacterial strains namely E. coli , S. aureus and p.vulgaris .It evidently recommend that
inclusion complex formation increases the antibacterial activities considerably
extent. Compound containing para-chloro derivative exhibited maximum activity
than that of other two compounds among the tested substances against all the
tested bacterial strains. From this experiment, it  can be concluded that  compound having para-chloro  derivative of substituted thiazolidinone
has  more bio-accessible as compared to
two others .The   antibacterial activity of the inclusion
complexes  found to be increased after inclusion
formation due to solubility of the compounds which makes the compounds more bio-accessible
to specific tissues leading to increased drug activity.



I'm Mack!

Would you like to get a custom essay? How about receiving a customized one?

Check it out