New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for the aryl attached position two for benzimidazole decrease the capability of interaction and give less bending and smaller docking score and there is inverse relationship between increasing hindrances around phenolic hydroxyl and DNA polymerase inhibition for these compounds
In this research two series of the new derivatives of Trimethoprim and paracetamol drugs have been prepared which known as a high medicinal effectiveness. Series (A) is including the interaction of diazonium salt of trimethoprim and coupling with some substituted phenol compounds (2-amino phenol, 3-ethyl phenol, 1-naphthol, 2-nitro phenol, Salbutamol). Series (B) is including the interaction coupling alkali solution of paracetamol with diazonium salt of some substituted aniline compounds (Benzedine, 2, 3-di chloro aniline, Trimethoprim, Anilinium chloride, 2-nitro- 4-chloro aniline).Chemical structures of all synthesized compounds were confirmed by UV-visible and FTIR spectroscopy.
A 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 MoreThere is a continuous and massive need for newer cephalosporins that should have resistance against β-lactamases and can be used orally. An approach of using cephalexin, as a well-studied and potent antibacterial compound is considered to prepare new designed derivatives. These derivatives include the incorporation of amino acid moiety linked through an amide bond with the α-amino group of cephalexin. Certain aliphatic amino acids were used, such as glycine, alanine, valine and proline. The chemical structures of these derivatives were confirmed by IR spectroscopy and elemental analyses. All the synthesized compounds were subjected for preliminary evaluation of antimicrobial activity using well diffusion method, against certa
... Show MoreMany new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII] a, b and [VIII] a, b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII] a, b,[VIII] a, b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX] a, b and [X] ad). Finally, the new derivatives [XI] ac run out via the reacted compound [IX] a with different n-alkyl bromide (methyl bromide, ethyl bromide, and butyl bromide)
Three new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).
New derivatives of the anti-inflammatory, leprostatic drug dapsone 4 are synthesized, characterized and biologically screened by the treating the drug dapsone with chloroacetyl chloride in the presence of base. Both amino groups are acylated to give compound 6. The symmetrical acylated product then treated with Phenol, N-Acetyl-p-aminophenol, p-Chlorophenol, m-Chlorophenol, o-Hydroxybezoic acid and m-Hydroxybezoic acid to give compounds 8(a-f). The antimicrobial activity was tested for the synthesized compounds; activates were good compared to the parent drug. All the new compounds have scanned for their biological activities toward gram ‒ve and gram +ve (M. tuberculosis, S. pneumoniae, E. coli and P. mirabilis) bacteria, the synthesized
... Show MoreMany new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII]a, b and [VIII]a,b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII]a,b, [VIII]a,b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX]a,b and [X]a-d). Finally, the new derivatives [XI]a-c run out via the reacted compound [IX]a with di
Nitrogen-comprising heterocyclic compounds and their derivatives have empirically been invaluable as therapeutic agents. Fundamentally, 4-chloro-6-nitro-2-amino-1,3-benzothiazole 1 was synthesized via bromination of 2-chloro-4-nitro aniline with ammonium thiocyanate. This new heterocyclic haloorganoamino-1,3-benzothiazole derivative, was a starting material, which condensed and tethered with three different aromatic aldehyde pendant arm in presence of ethanol and glacial acetic acid isolating an interesting sequence of tridentate Schiff bases 2-4. These compounds were used for complexation reactions in 1:1 (metal: ligand) stoichiometry to obtain heteroleptic Al(III), Ni (II) and K(I) benzothiazole chelat
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