Background: 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 on all derivatives. Molecular docking and ADMET analysis were performed on the final compounds, comparing them with standard drugs (ciprofloxacin and fluconazole). Results: The antimicrobial activity was assessed on two Gram-positive bacteria, Staphylococcus aureus and Bacillus licheniformis; two Gram-negative bacteria, Escherichia coli and Acinetobacter baumannii; and one fungus species, Candida albicans. Molecular docking has recorded higher docking scores for 3d and 3e compared to ciprofloxacin and fluconazole. The virtually active molecules showed an adequate drug-like profile and desired pharmacokinetic properties in the ADMET analysis. Conclusions: Most derivatives displayed significant antimicrobial activity, with compound 3e being the most active, followed by compound 3b. Molecular docking revealed higher scores for compound 3e compared to fluconazole and for compounds 3d and 3e compared to ciprofloxacin. ADMET analysis of compound 3e showed excellent absorption, consistent with its strong GIT absorption.
Azo ligand 11-(4-methoxyphenyl azo)-6-oxo-5,6-dihydro-benzo[4,5] imidazo[1,2-c] quinazoline-9-carboixylic acid was derived from 4-methoxyaniline and 6-oxo-5,6-dihydro-benzo[4,5]imidazo[1,2-c]quinazoline-9-carboxylic acid. The presence of azo dye was identified by elemental analysis and spectroscopic methods (FT-IR and UV-Vis). The compounds formed have been identified by using atomic absorption in flame, FT.IR, UV-Vis spectrometry magnetic susceptibility and conductivity. In order to evaluate the antibacterial efficiency of ligand and its complexes used in this study three species of bacteria were also examined. Ligand and its complexes showed good bacterial efficiencies. From the obtained data, an octahedral geometry was proposed for all p
... Show MoreA series of metal ion complexes of some divalent transition metal ions having the general composition [ML2Cl2]nH2O with 2-(benzo[d]thiazol-2-ylamino)-2- (5-chloro-2-hydroxy phenyl) acetonitrile ligand has been prepared from 5-chloro-2-hydroxy-benzaldehyde and benzo[d]thiazol-2-amine. Existence of cyanide as potassium cyanide in acidic medium was considered, characterized by elemental chemical analysis, conductance of molarity, magnetic susceptibility measurements, FTIR electronic spectral studies and mole ratio method. FTIR indicates the participation of amino and acetonitrile nitrogen which is coordinated with the central metal ion.
Crop diseases are usually caused by inoculum of pathogens which might exist on alternate hosts or weeds as endophytes. These endophytes, cum pathogens, usually confer some beneficial attributes to these weeds or alternate hosts from protection against herbivores, disease resistance, stress tolerance to secondary metabolites production. This study was therefore carried out to isolate potential crop pathogens which exist as endophytes on weed species in the University of Ilorin plantations. Green asymptomatic leaves were collected from 10 weed species across the plantations, and processed for their endophytic fungi isolation. Isolates were purified into pure cultures and used for molecular identification using the internal transcribed spac
... Show MoreThe purpose of this study was to isolate and identify additional products produced by direct laser irradiation, as well as to ascertain if laser irradiation may stimulate the synthesis of antibiotic compounds in a local Streptomycetes (Strept). Moreover, we postulate the mechanisms by which lasers function within living bacterial cells and suggest that sequential photochemical reactions may transpire following a designated period of irradiation. Thiophene was found as one of the most significant clinical products with antibacterial and anticancer properties. To accomplish these objectives, we selected two isolates: Streptomyces thinghirensis strain S10 (Strept thin), which inherently synthesizes an antibacterial agent, and Streptomyces lien
... Show Morecompound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show
... Show MoreA series of new coumarin and N-amino-2-quinolone derivatives have been synthesized. The reaction of coumarin (1) with excess of Hydrazine hydrate 98% yielded 1-amino-2-quinolone (2), Compound (2) was reacted with different Sulfonyl chloride to yield Sulfonamides [ N-(2-oxoquinolin-1(2H)-yl) methane sulfonamide (3), N-(2-oxoquinolin-1(2H)-yl) Benzene sulfonamide (4) and 4-methyl-N-(2-oxoquinolin-1(2H)-yl) benzene sulfonamide (5) ], while reaction of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy) acetic acid (8) with different amines yielded compounds [ 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(2-oxoquinolin-1(2H)-yl) acetamide (9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamide (10) ] th
... Show MoreFive N-substituted poly diimides were prepared by two steps. First step was included the preparation of five N-substituted diamides by reaction of adipoyl chloride with different amines .The second step was involved reaction of diamides with poly acryloyl chloride to obtain five new poly diimides having different physical properties which may used in different applications.