SYNTHESIS, CHARACTERIZATION OF S-

TRIAZINE DERIVATIVES AND EVALUATION OF

THEIR PHARMACOLOGICAL ACTIVITY

1.
THE THESIS

Submitted to the

Jayoti Vidyapeeth Women’s University

For the degree of

Doctor of Philosophy
(PHARMACEUTICAL SCIENCES)

Supervised By: Submitted By:

JV’n Dr. Anurekha Jain JV’n Ms. Neha Yadav

DEPARTMENT OF PHARMACEUTICAL SCIENCES

FACULTY OF PHARMACEUTICAL SCIENCES
JAYOTI VIDYAPEETH WOMEN’S UNIVERSITY
JAIPUR (RAJASTHAN), INDIA
2020
5. CONCLUSIONS

S-Triazine molecule has a superior impact in the field of

pharmaceutical chemistry and medicinal chemistry, despite the fact
that it has not only worn as an antimicrobial, anti-inflammatory,
analgesic, anti-tumour, anti-proliferative, anti-angiogenic, anticancer
activity but in addition for other mutagenic problems. From the
entirety review, we can conclude that there was a diversified activity
contour that occurred due to the changes in the various position of a
molecule on the terminal.

The core intention of the current study was to synthesize

enhanced and therapeutically dynamic agents with lesser side effects.
Therefore various Novel s- Triazine derivatives were synthesized by
a series of reactions and were characterized by their IR, 1H NMR
spectra.

The main goal of this present work is that our synthesized and
screened molecules might be the lead molecules for the further
development for better pharmacological profile than pervious
existing drug molecules that are using for various diseases.

Trisubstituted s-Triazine derivatives LC01-LC22 were

synthesized, characterised and evaluated for antimicrobial activity.

There are twenty two s-Triazine derivatives synthesised and

characterised by various physiochemical and spectral analysis.
Synthesized compounds LC01-LC22 were evaluated for antibacterial
and antifungal activities. All the synthesised compounds have
significant activity against tested strains of bacteria and fungi.
Compounds those were screened for antibacterial activity showed

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 significant antibacterial activity in opposition to the tested
strains (E. coli, S. aureus, P. Aeruginosa and B. subtilis) and their
MIC was found to be better than that of standard (Chloramphenicol,
Ciprofloxacin).

Compounds those were screened for antifungal activity

showed significant antifungal activity in opposition to the tested
strains of fungi (C. albicans and S. Cerevisiae) and their MIC was
found to be better than that of standard (Nystatin, Greseofulvin).

It has been observed from the above study that newly

synthesized s-Triazine derivatives are more active against C.
albicans as compare to S. Cerevisiae.

Compound LC13 was most active against gram-ve

(Escherichia coli and Pseudomonas aeruginosa) where as LC19
was found most active against gram +ve (Bacillus subtilis and
Staphylococcus aureus).

Further, compound LC13 and LC19 can be used for further

antimicrobial studies.

All the synthesized compounds were subjected to Molecular

docking into the site of Cyclo-oxygenase 2 (Pdb ID: 1CX2) with the
aim to predict anti-inflammatory activity. Compound LC05, LC09,
LC12, LC18 and LC22 shows better interaction with protein and
high docking score as compared to reference ligand and shows
minimum bond length that means they may be considered as good
inhibitor of COX-2.

The molecular docking analysis of all the synthesized compounds revealed

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that the compound LC22 exhibit highest docking score i.e -178.103 with 3
interactions, While Compound LC12 shows highest interaction i.e. 09
interactions with -155.577 docking score. Hence, they may be considered as
good inhibitor of COX-2.

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