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.
1-[4-(2-Hydroxy-4, 6-dimethyl-phenylazo)-phenol]-ethanone (HL1) and 2-(4-methoxy-phenylazo)-3, 5- dimethyl-phenol (HL2) were produced by combination the diazonium salts of amines with 3, 5- dimethylphenol. The geometry of azo compounds was resolved on the basis of (C.H.N) analyses, 1H and 13CNMR, FT-IR and UV-Vis spectroscopic mechanisms. Complexes of La (III) and Rh (III) have been performed and depicted. The formation of complexes has been identified by using elemental analysis, FTIR and UV-Vis spectroscopic process as well, conductivity molar quantifications. Nature of complexes produced have been studied obeyed mole ratio and continuous alteration ways, Beer's law followed through a concentration scope (1×10-4 - 3×10-4 M). High molar
... Show MoreThe research includes the synthesis and identification of the mixed ligands complexes of M 2 Ions in general composition ,[M(Leu) 2 (SMX)] Where L leucine (C 6 H 13 NO 2 )symbolized (LeuH) as a primary ligand and Sulfamethoxazole C 10 H 11 N 3 O 3 S) symbolized (SMX)) as a secondary ligand . The ligands and the metal chlorides were brought in to reaction at room temperature in(v/v) ethanol /water as solvent containing NaOH. The reaction required the following [(metal: 2(Na Leu --): (SMX )] molar ratios with M(II) ions, Were M ( Mn ( II),Co (II),Ni(II),Cu( II),Zn (II),Cd(II)and Hg( The UV Vis and magnetic moment data revealed an octahedral geometry around M(II), The conductivity data show a non electrolytic nature of the complexes . The
... Show MoreNew heterocyclic derivatives of quinoline are reported. Reaction of quinoline-2-thiol 4 with hydrazine hydrate gave 2-hydrazionoquinoline 5. Treatment of 5 with CS2 in pyridine afforded 1,2,4-triazolo-[4,3-a]- quinolin-1-2H-thione 6, whereas the reaction of 5 with carboxylic acids namely formic acid or acetic acid, yielded the 1,2,4-triazol-[4,3-a]-quinolin 7 or 5-methyl-1,2,4-triazolo [4,3-a]-quinoline 8 through ring closure. Diazotization of 5 under acidic conditions produced the fused tetrazole compound 9, tetrzolo-[1,5-a]- quinoline. Moreover, treatment of 5 with active methlyene compounds gave two pyrazole derivatives 10 and 11. Azomethines 12a-e were prepared through condensation of 5 with aromatic aldehydes or ketones.
Heterocyclic systems, which are essential in medicinal chemistry due to their promising cytotoxic activity, are one of the most important families of organic molecules found in nature or produced in the laboratory. As a result of coupling N-(4-nitrophenyl)-3-oxo-butanamide (3) using thiourea, indole-3-carboxaldehyde, or piperonal, the pyrimidine derivatives (5a and 5b) were produced. Furthermore, pyrimidine 9 was synthesized by reacting thiophene-2-carboxaldehyde with ethyl cyanoacetate and urea with potassium carbonate as a catalyst. The chalcones 11a and 11b were synthesized by reacting equal molar quantities of 1-naphthaldehy
... Show MoreThe work include synthesis of nanocomposites (X / S / Ag) based on blend from Xanthan gum / sodium alginate polymers (X / S) with different loading of synthesized silver nanoparticales (0.01, 0.03 and 0.05 wt%) were added to the blend. The silver nanoparticles were prepared by reduction method and were characterized and analyzed using X-ray diffraction (XRD) and Atomic force microscope (AFM). XRD study showed the presence nanoparticle of silver with crystalline nature and face-centered cubic (FCC) structure and an average size of nanoparticles ranging from 32 to 37 nm. The surface study was performed using AFM which showed a fairly uniform shape to the nanocomposites and a spherical nature for the silver nanoparticles. The nanocomposite exh
... Show MoreFive N-substituted acrylamides were prepared by reaction of substituted aromatic primary amines with acryloyl chloride in the presence of triethyl amine. The synthesized acrylamides were allowed to introduce copolymerization reaction with three vinylic monomers including acrylonitrile, methyl acrylate and methyl methacrylate respectively to obtain eleven new copolymers having different physical properties which may used in different applications.
This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], the reaction of this compound with theiosemicarbazide led to produce a new carbothioamide compound [V], which was reacted with ethyl chloro acetate to yield the thioxoimidazolidin compound [VI]. The condensation reactions of this compound with different substituted aldehyde give new alkene derivatives [VII] ad. The synthesized compounds were characterized by melting points, FT-IR, 1H-NMR and Mass spectroscopy.