A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (
A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f
... Show MoreObjective: Schiff’s and Mannich bases of isatins are an important group of heterocyclic compounds which are of great importance in medicinal chemistry as antimicrobial agents. In the vision of these facts, new bis-Schiff bases and Mannich bases of isatins were synthesized. Methods: Three different bis-Schiff bases (3a-c) have been synthesized by reacting isatin, 5-fluoroisatin and 5-methoxy isatin with thiophene-2- carboxaldehyde using hydrazine hydrate to link between the carbonyl compounds, and then these bis- Schiff bases were condensed with two different secondary amines (piperidine and morpholine) separately, and formaldehyde to form the Mannich bases (4a-c and 5a-f), respectively. Results: The structures of the newly synthesized com
... Show MoreTwo series of bent core mesogen containing 1,2,4-traizole ring [X]a-e and [XI]a-e were synthesized by many steps starting from esterification of isophthalic acid with methanol to yield diester compound [I] which was converted to their acid hydrazide [II] and the acid hydrazide reacted with ammonium thiocyanate or phenyl isothiocyanate to yield compounds [III] and [IV] , respectively . Then cyclization by 4% NaOH to yielded 1,2,4 traizole-3- thiol compounds [V] and [VI], respectively, afterword adding hydrazine hydrate to yield compounds [VII] and [VIII] .These compounds condensated with different substituted aldehyde to give new Schiff bases[X]a-e and [XI]a-e,respectively. The synthesized compounds were characterized by melting points ,
... Show MoreThe 4-(?-bromo acetyl)-4?-toluene sulfonanilide (2) was used as key intermediate to synthesize new heterocyclic compounds. This bromo compound was synthesized via sulfonation of amino group of p-amino acetophenone using Hinsburg method with 4-toluene sulfonyl chloride to form 4-acetyl-4?-toluene sulfonanilide (1) which is used as a starting material in this work. This compound was brominated to yield compound (2) which is used as a precursor to synthesize new five and seven membered heterocyclic compounds such as substituted 1,3-oxazoles (3,4), 1,3-thiazole derivatives (5-7), thiourea compounds (8a,b), 1,3-Thiazoline-2-thione compounds (9a-f) and 1,2,5-triazepine compounds (11a-d). The synthesized compounds were identified depending u
... Show MoreObjective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
... Show MoreA series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these
... Show MoreStarting from bis (4,4'-diamino phenoxy) ethan(1), a variety of phenolicschiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis, some derivatives evaluated by thermal analysis (TGA).
A set newly complexes with the general formula [M(L)Cl2] are resulting from the reaction of a new schiff base ligand [Ethyl (6R,7R)-7-((E)-2-((2-ethoxy-2- oxoethoxy)imino)-2-(2-(((E)-4-nitrobenzylidene) amino) thiazol -4- yl) acetamido) -8- oxo -3- vinyl -5- thia -1-aza bicyclo [4. 2.0] oct -2- ene -2- carboxylate] (L). This ligand was derived from the reaction of the two substances 4-nitrobenzaldehyde and precursor (P). Reaction the ligand with metal ions M= Mn(II), Co(II), Ni(II), Cu(II) and Cd(II) afforded new complexes which are characterized by FT-IR and Electronic Spectra. These measurements indicate that the complexes have a tetrahedral geometry. The Penicillin-Binding Protein 3 (PBP3) of Staphylococcus aureus and the target protein
... Show More