Journal of Medicinal and Chemical Sciences
Volume:3 Issue: 2, Apr 2020

Although studies on oxidation of triterpenoid ketones with hydrogen peroxide and selenium dioxide have been reported, literature reports on the effect of theoxidizing agent on the oxime derivative of triterpenoid ketones are scanty. Thus in continuation of our previous studies on the transformative reactions on pentacyclic triterpenoids of lupane and friedelin skeleton and in order to examine the nature of the products formed on the oxidation of oxime derivatives of 3-keto-triterpenoids having gem dimethyl group at C4 and a double bond at ring D (between C14-C15), the oxidation of keto-oximes of taraxerone with hydrogen peroxide and selenium dioxidewas taken up and characterisation of the products (A -D) along with the evaluation of their preliminary biological activitywere studied in this work. The oxime derivative of taraxerone (1a) in tertiary butanol was refluxed with selenium dioxide and hydrogen peroxide. The residue obtained after recovery of solvent by distillation was extracted with ether and separated into neutral and acid parts using usual method.

Treatment of bacterial infections with chemicals has led to drug resistance. Therefore, research to replace herbal treatments with less side effects is of a great importance. Therefore, this study aims at investigating the antimicrobial effects of methanolic extract of Rosmarinus officinalis on some gram positive and gram negative bacteria. In this research study, after collecting the plant and confirming its scientific name, R. officinalis extract was prepared using Soxhlet extractor method at the concentrations of 20-400 mg/mL and the antimicrobial effects of theextract using agar well diffusionand determination of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) from dilution method against standard bacteria of Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. Methanolic extract of R. officinalis plant has an inhibitory effect on P. aeruginosa, E. coli and S. aureus so that it has the highest sensitivity to methanolic extracts of R. officinalis in P. aeruginosa with a 19.8 mm the zone of growth inhibition and the lowest sensitivity to S. aureus with the zone of growth inhibition 14.4 mm. The results of this study showed that R. officinalis extract has a significant effect on tested bacteria, and further research is required to identify, quantify, and purify its effective compounds.

Phosphodiesterase-IV (PDE- IV) inhibitors which are effective anti-inflammatory agents have forced researchers to find new PDE-IV inhibitors with less adverse effects than conventional anti-inflammatory drugs. Some pyridazinone derivatives reduced inflammation by inhibiting PDE-IV enzyme and acted as anti-inflammatory agents. The new pyridazinone derivatives will be more suitable than the currently developed pyridazinone compounds for future studies and could be developed as more safe anti-inflammatory drugs for humans.

Phytochemical investigation of the pet-benzene extract of the leaves of Psidiumguajava was yielded the triterpenoids, olean-12(13), 15(16)-diene, olean-12(13), 15(16)-dien-3β-oland olean-15(16)-en-11α-ol. All the three compounds are reported for the first time from Psidiumguajava. The compounds were established by chemical characterized using IR, NMR, and Mass analysis by comparison with authentic sample. All the three triterpenoids showed moderate to good biocidal activity against some bacterial and fungal pathogens.

The present work aims to evaluate two native plants including, Hammada scoparia (H. scoparia) and Halocnemum Strobilaceum (H. Strobilaceum), which grow in Benghazi-Libya for soil phytoremediation purpose. Plants and soil samples were collected and analyzed for Cu, Zn, Fe and Cr concentrations at different sites in the north coastal region of Benghazi. Performance of Hammada scoparia and Halocnemum Strobilaceum was evaluated by calculating biological absorption coefficient (BAC), bioconcentration factor (BCF), and translocation  factor (TF). Both plants were found to be a moderate extractor. The tendency of the plants toward phytoextraction process and phytostabiliztion process was studied. Both plants tend to phytoextraction process except Halocnemum Strobilaceum tends strongly to phytostabiliztion process in case of Cu and Fe.

Tuberculosis (TB) has been one of the main causes of morbidity, and the emergence of multi-drug resistant (MDR) Mycobacterium tuberculosis strains has become a major concern. The decrease in activity of the major anti-TB drugsincluding, isoniazid, and rifampicin is an important threat that requires an urgent therapy. Anti-TB activity of the fluoroquinolones (FQs) has been under investigation. Many FQs are active in vitro; however, only a few such as ofloxacin, ciprofloxacin, sparfloxacin, levofloxacin, Moxifloxacin, and gatifloxacin have been clinically tested. The FQs can be used in co-therapy with the available anti-TB drugs. Molecular hybridization is a concept of drug design and development based on combination of pharmacophoric moieties of various bioactive compounds to produce a new hybrid compound with improved affinity and efficacy compared with the present drugs.

This work was conducted to evaluate catalytic efficiency of red clay of Adrar-Algeria zone as an effective green catalyst on the Aza Michael reaction. The Aza-Michael reaction is the addition of amine to α, β-unsaturated alkene was carried out using raw red clay from the Adrar-Algeria area as a catalyst to synthesize the new carbon-carbon or carbon-heteroatom bond containing products. The reaction was carried out with favorable conditions, ambient temperature, without solvent, and the protocol likes the environment, so-that the synthesized products provide high yields and excellent chemo selectivity.

Design of novel antipsoriatic drugs based on the medicinal compound Tazarotene is the main purpose of the present study. Firstly, the molecular structures of Tazarotene and its derivatives (F, Cl, CH3, OCH3, COOH, OH, NH2 and CF3) were optimized using density functional theory (DFT) at B3LYP/6-311++G (d, p) computational method. Then, the optimized molecules were docked into the active site of the retinoic acid receptors. The molecular docking analyses revealed that, the Tazarotene derivatives with COOH, CF3 and OCH3 substituents can make strongest complexes with RAR-alpha, RAR-beta and RAR-gamma, respectively. Based on the physicochemical properties calculations, it was cleared that the CF3 derivative of Tazarotene has better properties (receptor-ligand interaction efficiency, lipophilicity and skin permeation) compared with that of the Tazarotene.

In this research study, two Schiff base compounds AP-DHPDB (1) synthesized from the reaction of 2-aminophenol (AP) with 3, 3ʹ-dihydroxy-4, 4ʹ-(propane-1, 2-dieloxy)-dibenzaldehyde (DHPDB) and FA-DHEDB (2) synthesized from the reaction of furfuryl amine (FA) with 3, 3ʹ-dihydroxy-4, 4ʹ-(ethane-1, 2-dieloxy)-dibenzaldehyde (DHEDB) by reflux in methanol as solvent for 2 h. Suitable crystals of 1 and 2 get by slow evaporation of solvent after few days and characterized by elemental analysis. Crystal structures of the title compounds 1 and 2 were determined using the single crystal X-ray diffraction analysis. The title compounds 1 and 2 were found to be in monoclinic and orthorhombic with the space group of C2/c and Pnca, respectively. The unit cell parameter of 1 were a=29/8994(10), b=4.86618(7), c=21.7214(4) Å, b=124.4901(17)° and V=2604.85(12) Å3, and the unit cell parameter of 2 were a=22/3513(7), b=26.0250(7), c=4.6681(9) Å and V=2715(12) Å3. The C-N bond distances around the iminic nitrogen of compound 1 are 1.418 and 1.268 Å, and in compound 2 are 1.467 and 1.269 Å, indicated the single and double bonds, respectively. Also, the bond angles around the iminic nitrogen are distorted from 120° corresponding to sp2 hybrid (N1-C7-C8 = 122.5° and C6-N1-C7 = 119.3° for 1 and N7-C8-C9 = 123.9° and C6-N7-C8 = 116.12° for 2).

Acetaminophen overdose is one of severe global health challenges. In this study, adsorption technique was used to reduce acetaminophen overdose. Carbo tablets derived by wet granulation technique, coded as formulated carbo tablet (FCT) and alginated formulated carbo tablets (FCT-Alg), were characterized using the pharmaceutical drug procedures (hardness, disintegration time, tablet strength, friability) and instrumental techniques including, FTIR, SEM, and DSC analysis. DSC thermogram revealed that, the excipients were compatible with the active pharmaceutical ingredient (API). Batch adsorption experiments were carried out in the simulated gastric fluid (SGF) to monitor the role of some parametric factors (pH, concentration, carbo dosages, and PCM dosages). The tablet displayed favorable hardness and disintegration time (3.40 min). Optimum adsorption was observed at pH 1.2 for FCT in SGF (RE of 92.80%); FCT-Alg in SGF (RE of 99.17%). The results depicted that, the adsorption of the acetaminophen in SGF gave up to 99.65% removal efficiency, and compared with the commercial carbo tablet (CCT) with adsorption efficiency of 96.44%.