A comparative study of the behavior of cyanothioformamide and oxazolidine (thiones or iminothiones) towards some binucleophiles

Reactions of cyanothioformamides ( I ) with o‐phenylenediamines, o‐aminophenol, and anthranilic acids furnished benzimidazole ( II,III ), benzoxazole ( VII ), and quinazoline ( IX ) derivatives, respectively. Oxazolidine (thiones or iminothiones) ( IV ) were reacted with the same binucleophiles to produce quinoxaline ( V ), benzimidazole ( VI ), and quinazoline ( XI ) derivatives. © 2002 Wiley Periodicals, Inc. Heteroatom Chem 13:291–298, 2002; Published online in Wiley Interscience (www.interscience.wiley.com). DOI 10.1002/hc.10031     

Reaction with hydrazonoyl halides XXIII [1]: Synthesis and reactions of C‐coumarinoyl‐N‐arylformohydrazonoyl bromides

C‐Coumarinoyl‐N‐arylformohydrazonoyl bromides ( 3 ) were synthesized by reaction of N‐nitrosoarylacetamides with an appropriate sulfonium bromide in ethanol at room temperature. The reactions of potassium thiocyanate, potassium selenocyanate, thiourea, methyl phenylthiocarbomate, and methyl phenylhydrazinedithioate with hydrazonoyl bromide 3a were examined. © 1999 John Wiley & Sons, Inc. Heteroatom Chem 10: 355–362, 1999     

Transport of Carbamazepine,Ciprofloxacin and Sulfamethoxazole in Activated Carbon: Solubility and Relationships between Structure and Diffusional Parameters

The transport of carbamazepine, ciprofloxacin and sulfamethoxazole in the different pores of activated carbon in an aqueous solution is a dynamic process that is entirely dependent on the intrinsic parameters of these molecules and of the adsorbent. The macroscopic processes that take place are analyzed by interfacial diffusion and reaction models. Modeling of the experimental kinetic curves obtained following batch treatment of each solute at 2 µg/L in tap water showed (i) that the transport and sorption rates were controlled by external diffusion and intraparticle diffusion and (ii) that the effective diffusion coefficient for each solute, with the surface and pore diffusion coefficients, were linked by a linear relationship. A statistical analysis of the experimental data established correlations between the diffusional parameters and some geometrical parameters of these three molecules. Given the major discontinuities observed in the adsorption kinetics, the modeling of the experimental data required the use of traditional kinetic models, as well as a new kinetic model composed of the pseudo first or second order model and a sigmoidal expression. The predictions of this model were excellent. The solubility of each molecule below 60 °C was formulated by an empirical expression.     

The Multifaceted Role of Curcumin in Advanced Nanocurcumin Form in the Treatment and Management of Chronic Disorders

Curcumin is the primary polyphenol in turmeric’s curcuminoid class. It has a wide range of therapeutic applications, such as anti-inflammatory, antioxidant, antidiabetic, hepatoprotective, antibacterial, and anticancer effects against various cancers, but has poor solubility and low bioavailability. Objective: To improve curcumin’s bioavailability, plasma concentration, and cellular permeability processes. The nanocurcumin approach over curcumin has been proven appropriate for encapsulating or loading curcumin (nanocurcumin) to increase its therapeutic potential. Conclusion: Though incorporating curcumin into nanocurcumin form may be a viable method for overcoming its intrinsic limitations, and there are reasonable concerns regarding its toxicological safety once it enters biological pathways. This review article mainly highlights the therapeutic benefits of nanocurcumin over curcumin.     

Ginsenoside Rb1 Mitigates Escherichia coli Lipopolysaccharide-Induced Endometritis through TLR4-Mediated NF-κB Pathway

Endometritis is the inflammatory response of the endometrial lining of the uterus and is associated with low conception rates, early embryonic mortality, and prolonged inter-calving intervals, and thus poses huge economic losses to the dairy industry worldwide. Ginsenoside Rb1 (GnRb1) is a natural compound obtained from the roots of Panax ginseng, having several pharmacological and biological properties. However, the anti-inflammatory properties of GnRb1 in lipopolysaccharide (LPS)-challenged endometritis through the TLR4-mediated NF-κB signaling pathway has not yet been researched. This study was planned to evaluate the mechanisms of how GnRb1 rescues LPS-induced endometritis. In the present research, histopathological findings revealed that GnRb1 ameliorated LPS-triggered uterine injury. The ELISA and RT-qPCR assay findings indicated that GnRb1 suppressed the expression level of pro-inflammatory molecules (TNF-α, IL-1β and IL-6) and boosted the level of anti-inflammatory (IL-10) cytokine. Furthermore, the molecular study suggested that GnRb1 attenuated TLR4-mediated NF-κB signaling. The results demonstrated the therapeutic efficacy of GnRb1 in the mouse model of LPS-triggered endometritis via the inhibition of the TLR4-associated NF-κB pathway. Taken together, this study provides a baseline for the protective effect of GnRb1 to treat endometritis in both humans and animals.     

Synthesis and cytotoxic activity of some novel benzocoumarin derivatives under solvent free conditions

In the present study, a rapid, less expensive, clean and environmental friendly route to synthesis new pyrazoles, pyrazolopyridazines and condensed pyrimidines was developed via grinding of 2-(3-(dimethylamino)acryloyl)-3H-benzo[f]chromen-3-one (1) with different reagents. All the new compounds were characterized and established using elemental analysis and spectral data. Eight compounds were selected for in vitro antiproliferative against different human cancer cell lines entitled melanoma, cancers of the lung, leukemia, breast, brain, colon, prostate, ovary and kidney by the USA NCI.