In search of novel antibacterial agent, a series of new isatin derivatives (3a-d) have been synthesized by condensation isatin (2,3-indolinendione) with piperidine (hexahydropyridine), hydrazine hydrate and Boc-amino acids respectively. Compounds synthesized have been characterized by IR spectroscopy and elemental analysis. In addition, the in vitro antibacterial properties have been tested against E. coli, P. aeruginosa, and Bacillus cereus, S. aureus by employing the well diffusion technique. A majority of the synthesized compounds were showing good antibacterial activity and from comparisons of the compounds, compound 3d has been determined to be the most active compound.
Abstract
The target derivative are gentamicin linked with L-Val- L-Ala by an ester linkage. These were synthesized by esterification method, which included the reaction of -OH hydroxyl group on (carbon No.5) of gentamicin with the acid chloride of the corresponding dipeptide, The preparation of new derivative of gentamicin involved protected the primary & secondary amine groups of Gentamicin, by Ethylchloroformate (ECF) to give N-carbomethoxy Gentamicin which was used for further chemical synthesis involving the free hydroxyl groups.
Then prepared dipeptide (L-Val- L-Ala) by conventional solution method in present DCC & HoBt then reacted with thionyl
... Show MoreThe fabrication of Solid and Hollow silver nanoparticles (Ag NPs) has been achieved and their characterization was performed using transmission electron microscopy (TEM), zeta potential, UV–VIS spectroscopy, and X-ray diffraction (XRD). A TEM image revealed a quasispherical form for both Solid and Hollow Ag NPs. The measurement of surface charge revealed that although Hollow Ag NPs have a zeta potential of -43 mV, Solid Ag NPs have a zeta potential of -33 mV. According to UV-VIS spectroscopy measurement Solid and Hollow Ag NPs both showed absorption peaks at wavelengths of 436 nm and 412 nm, respectively. XRD pattern demonstrates that the samples' crystal structure is cubic, similar to that of the bulk materials, with
... Show MoreNano crystalline copper sulphide (Cu2S) thin films pure and 3% Bi doped were deposited on glass substrate by thermal evaporation technique of thickness 400±20 nm under a vacuum of ~ 2 × 10− 5 mbar to study the influence of annealing temperatures ( as-deposited, and 573) K on structural, surface morphology and optical properties of (Cu2S and Cu2S:3%Bi). (XRD) X-ray diffraction analysis showed (Cu2S and Cu2S:3%Bi) films before and after annealing are polycrystalline and hexagonal structure. AFM measurement approves that (Cu2S and Cu2S:3%Bi) films were Nano crystalline with grain size of (105.05-158.12) nm. The optical properties exhibits good optical absorption for Cu2S:3%Bi films. Decreased of optical band gap from 2.25 to 2 eV after dop
... Show MoreThree complexes of copper(II) and iron(II) with mixed ligands acetylacetonebis(thio-semicarbazone)- ABTSH2 and benzaldazine- BA have been prepared and characterized using different physico-chemical techniques including the determination of metal contents, mole-cular weight, measurement of molar conductivity, magnetic moment, molar refraction, infrared and electronic spectra. Accordingly, octahedral complexes having general formulaes [Cu2(ABTSH2)2(BA)2Cl2]Cl2 and [M2(ABTSH2)2(BA)2(SO4)2] {M= Cu(II) or (Fe(II)} have been proposed. The resulted complexes screened for antifungal activity in vitro against the citrus pathogen Aspergillus niger and Fusarium sp. which caused root rot of sugar and the beans pathogen Alternaria sp. All the complex
... Show MoreIn this study NiO - CoO bimetallic catalysts are prepared with two Ni/Co ratios (70:30 and 80: 20) using the precipitation method of nitrate salts. The effects of Ni /Co ratio and preparation methods on the catalyst are analyzed by using different characterization techniques, i.e. atomic absorption (AA) , XRD, surface area and pore volume measurements according to the BET method . The results indicate that the best catalyst is the one containing the percentage of Ni :Co ( 70 : 30 ). Experiments indicate that the optimal conditions to prepare catalyst are stirring for three hours at a temperature of 60oC of the preparation , pH= (8-9) , calcination temperature at 400oC for two hours
... Show MoreThe reaction of some new Schiff bases ( 2-[(2-Amino – ethylimino)-methyl]-R , 2-({2-[(R-benzylidene)-amino]-ethylimino}-methyl)-R with Benzoyl chloride or Acetyl chloride were carried out. Subsequent reactions of these products N-(2-Amino-ethyl)-N-[Chloro-(R) –methyl]-benzamide or N-(2-{?-[chloro-(R) –methyl]-amino}-ethyl)-N-[chloro-(R) –methyl]- benzamide with thiourea afforded thioureas compounds. The synthesized compounds were confirmed by their IR,UV,spectra and C.H.N. analysis.
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.
The pandemic SARS-CoV-2 is highly transmittable with its proliferation among nations. This study aims to design and exploring the efficacy of novel nirmatrelvir derivatives as SARS entry inhibitors by adapting a molecular modeling approach combined with theoretical design. The study focuses on the preparation of these derivatives and understanding their effectiveness, with a special focus on their binding affinity to the S protein, which is pivotal for the virus’s access to the host cell. Considering molecular docking aspects in the scope of a study on nirmatrelvir derivatives and S protein, dynamics simulations with 25 nanoseconds of their binding are explored. The study shows that these derivatives might work as effective antivi
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