New series of imidazole[1,2-a]pyridine-sulfonamides was designed and synthesized from 2-aminopyridine, which was reacted with p-bromo phenacyl bromide in the present of MgO to produce the corresponding imidazole[1,2-a]pyridine, which was then reacted with chlorosulfonic acid to produce 2-(4-bromophenyl)imidazole[1,2-a]pyridine-3-sulfonyl chloride [2]. Following that, treatment of (2) with different amines using the grand method to generate imidazole [1,2-a] pyridine sulfonamides. All the synthesized compounds have been characterized by FTIR, 1HNMR and 13CNMR and C.H.N analysis. The DFT, POM analysis and molecular docking were carried out on for all final compounds to investigate drug like attributes, and the results revealed showed that these compounds have an optimal drug ability score. According to the computational approach, the antioxidant activity and antiproliferative characteristics of the synthesized sulfonamides were examined using two cell lines (MCF-7 and hepG2) in varied times and different concentrations.
In contrast to the classical antibacterial sulfa drugs that are unsubstituted or monosubstituted, our newly synthesized analogs were designed to obtain sulfonamide moiety containing disubstituted hetero nitrogen atom. These compounds were formed successfully by chlorosulfonation of acetanilide and the product was treated with different cyclic amines and finally amide hydrolysis was necessary to get agents that were analyzed for IR, UV, CHN, melting points and solubility. At last, we studied their antibacterial activity on certain types of bacteria and we noticed the inactivity due to possible steric factor. Principly, this means these products have no inhibiting action against the used microbes.
A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di
... Show MoreIn this research a new compounds were synthesized started from compound 1 which was synthesized from two moll of piperidine (secondary cyclic amine) with dichloro acetic acid, compound 1 reacted by condensation reaction with methanol and H 2 SO 4 as a catalyst to give the ester compound 2. Compound 2 was reacted with hydrazine hydrate 80 % to give compound 3 , then the compounds 4-13 were synthesized from refluxing of compound 3 with the selected aldehydes and ketones via using few drops of glacial acetic acid, finely step the compounds 4-13 were reacted with phtalic anhydride to give compounds 14-23.. All these compounds were characterized by using of melting point, FTIR, 1 HNMR and mass spectroscopy. Scheme 1 and Scheme 2 shown the all re
... Show MoreIn this study new derivatives of Schiff bases 5-8, 1, 3-oxazepine 9-16 and tetrazoles 17-19 have been synthesized from the new starting material 1 which has synthesized the reaction of one mole of dichloro acetic acid and two moles of thiophenol, the esters 2-3 were synthesized from the reaction of compound 1 with methanol or ethanol respectively in the presence of H2SO4 as catalyst then 2, 2-dithiophenylaceto Hydrazide 4 were synthesized from the reaction of 2 or 3 with hydrazine hydrate 80%, Schiff bases 5-8 were synthesized from the reaction of 4 with appropriate aldehyde or ketone. Treatment of Schiff bases with maleic and phathalic anhydride in dry benzene to give 1, 3-oxazepen derivatives 9-16 and with sodium azide in tetrahydrofuran
... Show MoreBackground: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted o
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