Till now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine to form new Schiff bases 4(a-e), and dimer Schiff base (6) as final products. The structures of the newly synthesized compounds were identified using two spectroscopic methods; (Fourier- transform infrared) FTIR and proton nuclear magnetic resonance spectroscopy (¹H-NMR) analysis. The preliminary in vitro antibacterial and antifungal screening results of new isatin derivatives [4(a-e) and 6] reported moderate to potent antimicrobial activity, the compound 4c exhibited moderate broad-spectrum antibacterial and antifungal activities compared to other derivatives. Moreover, compounds 4c and 6 have a good inhibitory effect against B. subtilis while amoxicillin (standard drug) shows no activity. For antifungal activity compounds (4a-c and 4e) have considerable activity towards C. albicans, whereas compound 4d exhibits slight activity and 6 of no activity.
The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydro
... Show MoreA new ligand [4-chloro-N-(1,5-dimethyl-3-oxo-2-phenyl-2,3- dihydro-1H-pyrazol-4-ylcarb amothioyl) benzamide] (CAP) was synthesized by reaction of P-ChloroBenzoyl isothio cyanate with 4- aminoantipyrine,The ligand was characterized by micro elemental analysis C.H.N.S.,FT-IR,UV-Vis and1H13CNMR spectra, some transition metals complex of this ligand were prepared and characterized by FT-IR, UV-Vis spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were [M(CAP)2(H2O)2]Cl2(M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral
A new ligand [ 2-chloro-N- (1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro -1H-pyrazol- 4-ylcarbamothioyl)acetamide](L) was synthesized by reacting the Chloro acetyl isothiocyanate with 4-aminoantipyrine,The ligand was characterized by(C HNS) elemental microanalysis and the spectral measurements including Uv-Vis ,IR ,1H and13C NMR spectra, some transition metals complex of this ligand were prepared and characterized by Uv-Vis, FT-IR spectra, conductivity measurements, magnetic susceptibility and atomic absorption. From the obtained results the molecular formula of all prepared complexes were [M(L)2(H2O)2]Cl2 (M+2 =Mn, Co, Ni, Cu, Zn, Cd and Hg),the proposed geometrical structure for all complexes were octahedral.
Sheep are considered as an important part of livestock in the worldwide, particularly in Iraq, as they provide meat, milk, leather, wool, and manure. The present study aim is isolation and identification of staphylococci, enteric bacteria and Pseudomonas spp. Totally, 115 samples were collected from sheep (100 samples were collected from the nasal cavity of local sheep suffering from respiratory infections, and 15 samples were collected from apparently healthy local sheep). All the samples were collected from seven flocks located in Abu Ghraib and Al-Radwaniyah, Baghdad governorate, Iraq. The samples were taken during the period from October 2020 to February 2021. Staphylococcus spp., Pseudomonas spp., and enteric bacteria were detected fi
... Show MoreThe present study was carried out to determine the bacterial isolates and study their antimicrobial susceptibility in case of burned wound infections. 70 burn wound swabs were taken from patients, who presented invasive burn wound infection from both sex and average age of 3-58 years, admitted to teaching medical Al- Kendi hospital from October 2007 to June 2008. Pseudomonas aeruginosa was found to be the most common isolate (48.9%) followed by Staphylococcus aureus (24.4%), Citrobacter braakii (13.3%), Enterobacter spp. (11.1%), Coagulase-negative Staphylococci (11.1%), Proteus vulgaris (6.66%), Corynebacterium spp. (6.66%), Micrococcus (6.66%), Proteus mirabilis (4.44%), Enterococcus faecalis (4.44%), E.coli (4.44%), Klebsiella spp. (2.22
... Show MoreThe present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTI
... Show MoreDrug nanocrystals are nanoscopic crystals of the parent compound with dimensions less than 1 µm. A decrease in particle size will lead to an increase in effective surface area in the diffusion layer, which, in turn, increases the drug dissolution rate. Drug nanocrystals are one of the most important strategies to enhance the oral bioavailability of hydrophobic drugs.
Cefixime is the first member of what is generally termed the third generation orally active cephalosporins. These third generation cephalosporins are distinct from the older β-lactam antibiotics in their intensive antibacterial activity against a wide range of gram-negative bacteria.
The aim of this study is to prepare nanocrystals of cefixime as a caps
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