The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Metronidazole has a half-life of 6.5 ± 2.9 hours. A number of studies have recently been conducted on the selective substitution of hydrogen with deuterium. which increases the bond strength, increasing the biological half-life and, consequently, the drug's metabolic stability also increases. In an attempt to address metronidazole's drawbacks and clinical resistance, deuterated metronidazole was synthesised, characterised, and tested for antibacterial, antifungal, and anti-tubercular activities. The metronidazole and its deuterated compound showed equipotent antifungal activity and aerobic antibacterial activity. Also, when compared with the non-deuterated compound, deuterated metronidazole exhibited better anaerobic antibacterial and anti-tubercular activity.
Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas wit
... Show MoreNebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formul
... Show MoreIn this publication, several six coordinate Co(III)-complexes are reported. The reaction of 2,3-butanedione monoxime with ethylenediamine or o-phenylenediamine in mole ratios of 2:1 gave the tetradentate imine-oxime ligands diaminoethane-N,N`-bis(2-butylidine-3-onedioxime) H2L1 and o-phenylenediamine-N,N`-bis(2-butylidine-3-onedioxime), respectively. The reaction of H2L1 and H2L2 with Co(NO3)2, and the amino acid co-ligands (glycine or serine) resulted in the formation of the required complexes. Upon complex formation, the ligands behave as a neutral tetradantate species, while the amino acid co-ligand acts as a monobasic species. The mode of bonding and overall geometry of the complexes were determined through physico-chemical and spectro
... Show MoreNew ligands, N1, N4-bis (benzo[d]thiazol-2- ylcarbamothioyl) succinamide (L1) and N1, N4- bis (benzylcarbamothioyl)succinamide (L2), derived from succinyl chloride and 2-amino benzothiazole or benzylamine, respectively, have been used to prepare a set of transition metal complexes with the general formula [M2(L)Cl4], where L=L1 or L2, M = Mn(II), Ni(II), Cu(II), Cd(II), Co(II), Zn(II) or Hg(II). The synthesized compounds were characterized using various analytical techniques including TGA, 13C NMR, mass spectroscopy, 1H and Fourier-transform infrared (FTIR) spectroscopy, magnetic measurement, molar conductivity, electronic spectrum, (%M, %C, %H, %N) and atomic absorption flame (AAF) analysis. The results showed that (L1, L2) bin
... Show MoreThree series of monomers, polymers and thioester cyclic compounds containing 4H-1,2,4-triazol-3-thiol moiety were synthesized and examined for their liquid crystalline properties. All monomers, polymers and thioester compounds were characterized by elemental analysis and FTIR, 1 H-NMR and mass spectroscopy. The phase transition and mesomorphic properties were investigated by polarized optical microscope (POM) and differential scanning calorimetry (DSC). The monomer with terminal phenyl substituent display dimorphism nematic and smectic A (SmA) mesophases. The corresponding polymers derived from acrylic and phenyl acrylic acid monomers show nematic mesophase. The only thioester cyclic compound derived from terephtaloyl chloride show nemati
... Show MoreThis study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s
... Show MoreThis study focused on the synthesis of novel polymers incorporating the 1,3,4-oxadiazole ring. Four polymers were specifically prepared by blending polymers (6-9) with polyvinyl alcohol (PVA) in defined ratios, resulting in the formation of blended polymers (10-13). The synthesized polymers were characterized using Fourier Transform Infrared (FTIR) spectroscopy and proton nuclear magnetic resonance (1H-NMR). The results showed that the structure aligned with the proposed synthetic polymers. Furthermore, the physical and thermal properties were studied using scanning electron microscopy (SEM), thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC). Additionally, the biological activity was examined against two s
... Show MoreThe aim of the work is the synthesis and characterization of the tridentate Schiff base (HL) containing (N and O) as donor atoms type (ONO). The ligand is: (HL) phenyl 2-(2-hydroxybenzylidenamino)benzoate This ligand was prepared by the reaction of (phenyl 2-aminobenzoate) with salicylaldehyde under reflux in ethanol and few drops of glacial acetic acid which gave the ligand (HL). The prepared ligand was characterized by (FT IR,UV–Vis) spectroscopy, Elemental analysis of carbon, hydrogen and nitrogen (C.H.N.) and melting point. The ligand was reacted with some metal ions under reflux in ethanol with (1 metal :2 ligand )mole ratio which gave complexes of the general formula: Pr III , Cr and III La III [M(L)2]Cl , M = Products were found to
... Show MoreNew Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N, N'E, N, N'E)-N, N'-(cyclohexane-1,3-diylidene)bis(4- fluor
... Show MoreNew Schiff-base ligands bearing tetrazole moiety and their polymeric metal complexes with Co(II), Ni(II) and Cd(II) ions are reported. Ligands were prepared in a multiple-step reaction. The reaction of sodium 2,6- diformylphenolate and cyclohexane-1,3-dione with 5-amino-2-fluorobenzonitrile resulted in the isolation of two precursors sodium 2,6-bis((E)-(3-cyano-4-fluorophenylimino)methyl)-4-methylphenolate 1 and 5,5'- (1E,1'E)-cyclohexane-1,3-diylidenebis- (azan-1-yl-1-ylidene)bis(2-fluorobenzonitrile) 2, respectively. The reaction of precursors with azide gave the required ligands; sodium 2,6-bis((E)-(4-fluoro-3-(1H-tetrazol-5- yl)phenylimino)methyl)-4-methylphenolate (NaL) and (N,N'E,N,N'E)-N,N'-(cyclohexane-1,3-diylidene)bis(4- fluoro-3-
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