Discussion of the doctoral thesis of the student “Suhaib Eid Saleh

Discussion of the doctoral thesis of the student “Suhaib Eid Saleh

 The public discussion took place for the Doctoral student (Suhayb Eid Saleh Al-Fahdawi)

 At Anbar University, College of Science, Department of Chemistry, for his tagged thesis

"(Synthesis, characterization of novel 4-H-Chromen-4-one heterocyclic derivatives and their) "

 On Sunday, 7/14/2024, in Ibn Sina Hall..

The discussion committee consisted of:

Fallujah University - University Presidency - Chairman

Prof. Dr. Ahmed Suleiman Hamad

Anbar University - College of Science - Member

Prof. Dr. Muhammad Abdel Karim Talak

Anbar University - College of Education for Pure Sciences – Member

Prof. Dr. Abdullah Hussein Kashash

Anbar University - College of Science- member

Prof. Dr. Khaled Farouk Abdul Ghafour

Anbar University - College of Applied Sciences (HIT)-Member

Assist. Prof. Dr. Rasim Farraj Muslim

Anbar University - College of Education for Girls-member and supervisor

Prof. Dr.  Walid Faraj Hammadi

Anbar University - College of Science, member and supervisor

Assist. Prof. Dr. Ali Karim Aliwi

 The chemical compound 4H-chromene-3-carbaldehyde substitution is used in scientific study for several purposes. Typically, It is used in organic synthesis, particularly for the synthesis of heterocyclic compounds. The chemical compound 4-amino-4H-1,2,4-triazole-3-thiol with different substitutions is recognized for its exceptional characteristics and applications in several fields, including as its ability to combat microbes, prevent fingerprints, and fight against breast cancer. Our research thesis can be divided into three chapters, 1st chapter including introduction about chromeno derivatives, triazole derivatives, Schiff base, seven members ring, five members ring and six members ring and their medicinal application activities. There are four categories in the second chapter: 1st synthesis of chromone derivatives by reaction using 2-hydroxy acetophenone with various substitutions and DMF and POCl3 as catalysts under cold conditions, we produced 4H-chromene-3-carbaldehyde with substitution. 2nd synthesis of Triazole derivatives by reaction using various substitutions carboxylic acid with thiocarbohydrizide under heat conditions, we produced Triazole with different substitution, in another hand, we prepare Triazole derivatives by react different aromatic ester compound with hydrazine hydrate and CS2 in present of KOH as catalysts. 3rd synthesis of Schiff base derivatives by reaction using 4H-chromene-3-carbaldehyde substitution Triazole derivatives in present of acidic medium.  We got  Schiff base various substitutions. The 4th  is type of synthesis  of five , six and seven members ring  heterocyclic  compound. New 1,3-oxazepine derivatives(sex member ring) were synthesized from the Schiff base substituted and anhydrides corresponding to the presence of benzene as a solvent and glacial acetic acid as a catalyst to give the desired products. The synthesis of novel 1,3-thiazinan derivatives involves the use of a Schiff base replaced with 3-mercaptopropanoic acid, using THF as the solvent.

 A synthesis of novel 1,3-thiazolidine-4-one derivatives (five member ring) were achieved by reacting Schiff base substituted compounds with thioglycolic acid. This reaction requires the presence of acetonitrile as a solvent and zinc chloride as a catalyst.

The last chapter is about the results of our compounds. Condensing methyl salicylate and methyl benzoate with different substituents at different locations resulted in a wide variety of unique 1,2,4-triazole molecules. These compounds contain numerous molecules with beneficial pharmacological effects. We employed elemental analysis, Fourier transform infrared spectroscopy (FTIR), 1H nuclear magnetic resonance (NMR), and mass spectral data to determine the structures of these derivatives. We conducted in vitro studies on each compound to ascertain their antibacterial and anti-cancer activity. The testing technique required using two different bacterial strains. According to Gram (+) and Gram (-), the initial study's findings suggest that several discoveries possess qualities that warrant further investigation and should prioritize future studies. We tested ten compounds, following the guidelines of the net program. The compounds (KT9+6, BT2+6, DT2+5, KT6+7, and BT6+7) all have very good inhibition at 100 ppm concentration. The reason is according to functional group, and we  investigated the result according to a literature review.

Tahran University has performed the breast cancer test in vitro for these ten compounds and compared the cell viability of healthy cells and damaged cells. The lower IC50 value indicates greater drug potency and suggests that the drug is effective at inhibiting cancer cell growth. It suggests that cancer cells are more sensitive to the drug. Figure 3-167 showed that the IC50 had a different value. The IC50 values were KT9+6, KT9+7, DT2+5, KT6+7, and BT6+7. The results show that all compounds inhibit cell growth in a concentration-dependent manner when compared to the control. A higher IC50 value indicates lower drug potency, suggesting that the drug may be less effective in inhibiting cancer cell growth. It indicates a lower sensitivity of cancer cells to the drug.Higher IC50 values of some chromene derivatives (ET2+5, BT2+6, BT8+7, ET2+6, and ET7+5) indicate lower potency.

Now we have performed toxic tests because the compounds have become active due to their toxicity. It is possible for a compound to have a low IC50 value and be highly effective in inhibiting a target, but at the same time, it may also exhibit significant toxicity. In our application study, we got a lower IC50 value for KT9+6, KT9+7, DT2+5, KT6+5, and BT6+7, which indicates a higher potency of a compound in inhibiting a specific target. However, we can’t say the compounds don’t have toxicity because toxicity is a complex property that involves multiple factors, including the specific target or pathway being affected, the dose or concentration of the compound, and the organism or system being studied.

 

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