Synthesis of Thio Analogues of Quinolone Antibacterials

A facile and rapid synthesis of thio compounds, analogues to ciprofloxacin, and norfloxacin is described.     

Catalyst-free,aqueous and highly diastereoselective synthesis of new 5-substituted 1H-tetrazoles via a multi-component domino Knoevenagel condensation/1,3 dipolar cycloaddition reaction

An approach for the synthesis of new 5-substituted-tetrazoles via multi-component domino Knoevenagel condensation/1,3 dipolar cycloaddition reaction of carbonyl compounds, malononitrile and sodium azide in water without assistance of any catalyst has been reported. This general protocol provides a wide variety of 5-substituted 1H-tetrazoles in good yields under mild reaction conditions.     

One-pot efficient synthesis of disulfides from alkyl halides and alkyl tosylates using thiourea and elemental sulfur without contamination by higher polysulfides

An efficient and odorless synthesis of disulfides from alkyl halides using thiourea and elemental sulfur in the presence of sodium carbonate in wet polyethylene glycol (PEG 200) at 40 °C without contamination by higher polysulfides has been developed. This procedure was then extended to preparation of disulfides from alkyl tosylates at 70 °C.     

Morphology and Size Distribution Characterization of Precipitated Asphaltene from Live Oil During Pressure Depletion

The size and morphology of asphaltene aggregates, precipitated from live oil by pressure depletion at the reservoir temperature was studied using scanning electron microscopy and atomic force microscopy. The experimental studies showed that the mean size of aggregates increased when pressure decreased. The results indicate that the morphology of aggregates was changed from amorphous spherical and elliptical shapes to irregular. A bimodal distribution function was able to describe the size distribution in pressure range of 500 to 3500 psi. At higher pressure, the unimodel was able to represent the size distribution. The results showed reduction in live oil stability and asphaltene aggregation with pressure drop.     

Phytochemical and Biological Evaluation of a Newly Designed Nutraceutical Self-Nanoemulsifying Self-Nanosuspension for Protection and Treatment of Cisplatin Induced Testicular Toxicity in Male Rats

The incorporation of cisplatin (CP) as a cytotoxic antineoplastic agent in most chemotherapeutic protocols is a challenge due to its toxic effect on testicular tissues. Natural compounds present a promising trend in research, so a new nutraceutical formulation (NCF) was designed to diminish CP spermatotoxicity. A combination of three nutraceutical materials, 250 mg Spirulina platensis powder (SP), 25 mg Tribulus terrestris L. extract (TT), and 100 mg fish oil (FO) were formulated in self-nanoemulsifying self-nanosuspension (SNESNS). SP was loaded into the optimized self-nanoemulsifying system (30% FO, 50% span 80/cremophor EL and 20% isopropanol) and mixed with TT aqueous solution to form SNESNS. For the SP, phytochemical profiling revealed the presence of valuable amounts of fatty acids (FAs), amino acids, flavonoids, polyphenols, vitamins, and minerals. Transmission electron microscopy (TEM) and particle size analysis confirmed the formation of nanoemulsion-based nanosuspension upon dilution. Method validation of the phytochemical constituents in NCF has been developed. Furthermore, NCF was biologically evaluated on male Wistar rats and revealed the improvement of spermatozoa, histopathological features, and biochemical markers over the CP and each ingredient group. Our findings suggest the potential of NCF with SNESNS as a delivery system against CP-induced testicular toxicity in male rats.     

Green synthesis of bis-coumarin derivatives using Fe(SD)3 as a catalyst and investigation of their biological activities

A convenient, practical, green, and environmentally friendly method was developed for the synthesis of biscoumarins and corresponding tetrakis products from the reaction of 4-hydroxycoumarin and various aldehydes. The bis-coumarins were synthesized in high yield under mild reaction conditions. Products were obtained in the presence of in situ prepared Fe(SD)₃ [Iron(III) dodecyl sulfate] as a combined Lewis acid–surfactant catalyst (LASC) in water in short reaction times. Also, the antibacterial activity of compounds was screened against Pseudomonas aeruginosa and Escherichia coli as Gram-negative bacteria and Micrococcus luteus and Staphylococcus aureus as Gram-positive bacterial strains. Products 3g , 3k–l were most active than cefotaxime against E. coli and also compounds 3c and 3g were most active than cefotaxime against S. aureus.     

Ultrasound assisted eco-friendly synthesis of 3-cinnamoyl coumarins using N,N'-(1,2-phenylene)bis(2-aminobenzamide) dichloro cobalt immobilized on mesoporous Al-SBA-15 as a new and recyclable catalyst

ABSTRACT

A novel mesoporous Al-SBA-15 modified by N,N'-(1,2-phenylene)bis(2-aminobenzamide) dichloro cobalt has been prepared and applied as a reusable catalyst in the 3-cinnamoyl coumarins synthesis via three-component reaction between benzaldehydes, salicylaldehydes and ethyl acetoacetate by the assist of ultrasonic irradiation. By using of the nanocatalyst and also ultrasound irradiation, the easiness and velocity of the abovementioned reaction were enhanced and an environment friendly condition was provided to synthesis of various 3-cinnamoyl coumarin compounds. The properties and structure of nanocatalyst have been specified by methods including powder X-ray diffraction (XRD), energy dispersive spectroscopy (EDS), Fourier transform infrared spectroscopy (FT-IR), transmission electron microscopy (TEM), nitrogen adsorption–desorption analysis and scanning electronic microscopy (SEM). Superiority of this novel and viable method is due to mild reaction condition, short reaction times, high yields of 3-cinnamoyl coumarins, environmentally benign, recoverability of the CoCl₂N,N'-(1,2-phenylene)bis(2-aminobenzamide)/Al-SBA-15 catalyst and reusability with important preservation in its catalytic activity.     

Green and one‐pot surface coating of iron oxide magnetic nanoparticles with natural amino acids and biocompatibility investigation

We report the synthesis of iron oxide magnetic nanoparticles (IONPs) coated with various natural amino acids (AAs) using a one‐pot reaction in an aqueous medium. Several AAs, which contained hydrophilic and hydrophobic groups, were selected to study their effects on size, morphology and toxicity of IONPs. Functionalized IONPs were characterized using X‐ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, and scanning and transmission electron microscopies. Furthermore, vibrating sample magnetometry analysis shows these nanoparticles have excellent magnetic properties. Cellular toxicity of IONPs was also investigated on HFF2 cell lines. The AA‐coated IONPs are non‐toxic and biocompatible. Natural AA‐coated IONPs show a potential for their development in in vitro and in vivo biomedical fields due to their non‐toxicity, good ζ‐potential and related small size and narrow size distribution.     

Green synthesis and chemical characterization of Thymus vulgaris leaf aqueous extract conjugated gold nanoparticles for the treatment of acute myeloid leukemia in comparison to doxorubicin in a leukemic mouse model

Recently, metallic nanoparticles have been used for the treatment of several disorders, such as cancer. Indeed, finding the chemotherapeutic drug of nanoparticles is in researching the priority of both developed and developing countries. The present study confirms the ability of aqueous extract of Thymus vulgaris grown under in vitro condition for the biosynthesis of gold nanoparticles (AuNPs). Also, in this study, we indicated the antioxidant, cytotoxicity, and anti-acute myeloid leukemia properties of AuNPs compared to doxorubicin in a leukemic mouse model. The synthesized AuNPs were characterized using different techniques including X-ray diffraction (XRD), energy Dispersive X-ray Spectrometry (EDS), fourier-transform infrared spectroscopy (FT-IR) spectroscopy, ultraviolet–visible spectroscopy (UV–Vis.), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). In vivo design, induction of acute myeloid leukemia was done by 7,12-Dimethylbenz[a]anthracene (DMBA) in 75 mice. Then, the animals were randomly divided into six subgroups, including control, untreated, doxorubicin, AuNPs, T. vulgaris, and HAuCl₄. By quantitative real-time PCR, sphingosine-1-phosphate receptor-1 and sphingosine-1-phosphate receptor-5 mRNA expression in lymphocytes were significantly (P ≤ 0.01) raised by treating the leukemic mice with the AuNPs and doxorubicin. Also, AuNPs similar to doxorubicin, significantly (P ≤ 0.01) enhanced the anti-inflammatory cytokines (IL4, IL5, IL10, IL13, and IFNα) and the platelet, lymphocyte, and red blood cell (RBC) parameters and reduced the pro-inflammatory cytokines (IL1, IL6, IL12, IL18, IFNY, and TNFα), and the total white blood cell (WBC), blast, monocyte, neutrophil, eosinophil, and basophil counts as compared to the untreated mice. In vitro design, 2,2-diphenyl-1-picrylhydrazyl (DPPH) test revealed similar antioxidant potentials for doxorubicin and AuNPs. Furthermore, AuNPs similar to doxorubicin had low cell viability dose-dependently against 32D-FLT3-ITD, Human HL-60/vcr, and Murine C1498 cell lines without any cytotoxicity on HUVEC cell line. Above results confirm the excellent antioxidant, cytotoxicity, and anti-acute myeloid leukemia effects of AuNPs compared to doxorubicin. After confirming these results in clinical trial studies, AuNPs can be used as a chemotherapeutic drug for the treatment of acute myeloid leukemia in human.