Journal of Medicinal and Chemical Sciences
Volume:2 Issue: 3, May-Jun 2019

Two new triterpenoid saponins, named, 3-O-β-D-glucopyranosyl (1→3)-Olean-12- ene- 19, 23-diol 1 and 3-O-{O-α-L-rhamno-pyranosyl-(1→3)-O-[-O-β-D-glucopyranosyl-(1→3)]-β-D-glucopyranosyl}-pomolic acid were isolated from the stem bark of Xeromphis nilotica through extensive chromatographic technique [TLC and CC] and their structures were elucidated on the basis of their spectral data [1D, 2D NMR and HR-ESI-MS] and chemical evidence.

In a medicinal chemistry-driven drug discovery program aimed at synthesizing new topically-acting trypanocidal chemotherapeutic agents to treat the African trypanosomiasis, our research group became interested recently in new chemical entities bearing in their center a thiohydrazide (C=S) NHNH or thiosemicarbazide NH(C=S) NHNH central template flanked on both sides by lipophilic aryl moieties. In this context, benzopinacolone was found to react as a rather unusual acylating agent via a mechanism (addition/elimination) involving addition of the nucleophile (a thiosemicarbazide derivative), formation of a resulting tetrahedral adduct, and expulsion of a trityl anion moiety as leaving group, presumably through an anchimeric assistance effect by intramolecular participation of the thioureido side-chain via hydrogen bond formation. The present incidental discovery should be considered at this level as a first inception and further work is now being directed at closely examining the detailed mechanism of this exceptional chemical pathway, in a reaction involving the unusual breaking of a carbon-carbon bond (carbon acid as leaving group) in the rate-determining step and involving the decomposition of the intermediate tetrahedral adduct to get the final unexpected N-thiobenzoyl-thiosemicarbazide.

Polluted and dirty water is very harmful for living organisms especially for health of humans. It causes many serious health problems which can lead ultimately to death if these are not treated at early stages. Water borne diseases including cholera, Dracunculiasis, Typhoid fever, Diarrhea, Ulcers, Hepatitis, Arsenicosis, Respiratory Tract Infection, Kidney Damage, and Endocrine Damages are very risky for lives of individuals and especially for humans, these can lead ultimately death. These diseases are mainly due to drinking water problems because of presence of different harmful bacteria and germs which may cause these drugs. These diseases can be cured with proper medications and treatment courses. Along the treatment, there are different ways to prevent from these diseases. So, that the lives of human beings can be protected from these water borne-disease. The water treatment can also be used so no one can drink or use dirty or untreated water and can be saved from these effects. So, in this article, causes of these diseases, factors increasing the risks, treatment and prevention ways are summarized briefly.

Trauma is a common cause of death in developed countries leading trauma related coagulopathy. In recent years, ‘new type endothelium development’ caused by trauma-induced hemorrhagic shock, have been widely understood and researchers try to figure out the effect of endothelial apoptosis on this process. New modulation of immune response may result in undesired apoptosis and give rise to programmed cell death. In experimental models, apoptosis has been shown in liver, kidney, heart and brain after the damage of ischemia/reperfusion (I/R) during trauma. Apoptosis may be an important factor for the development of serious hemorrhagic shock during trauma. In this review we aimed to reveal the possible relationship between trauma and apoptosis.

Human activities are a major factor determining the quality of surface and groundwater through atmospheric pollution, effluent discharges, use of agricultural chemicals, eroded soil and land use.The purpose of this research was to determine the physicochemical parameters of water samples collected from Sa’adatu Rimi College of Education, Kumbotso Kano and to compare with the standards given by World Health Organization (WHO) and Nigeria Standard for Drinking Water Quality (NSDWQ). Four samples were collected from different locations within the college premises for the analysis. The analyzed parameters are pH, temperature, Total dissolved solids, Total suspended solids, Suspended solid, Electrical conductivity, Alkalinity, Mg2+,Ca2+, ammonia, sulphate,Nitrate, Nitrite,Turbidity, Salinity, Total hardness, free carbon dioxide, Iron and Chloride. The results indicated that all the analyzed parameters are within the permissible limits recommended byWHO and NSDWQwith exception of turbidity level at A sampling station, pH concentration at B, C, and D sampling point and nitriteconcentrations at C and D sampling point. The results also showed that, the concentration of total hardness were slightly above the maximum permissible limit (MPL) recommended by NSDWQ. This paper also recommended that, the college management should provide a basis for the regular monitoring of water quality status.

In this paper, we describe a simplecatalyst-free protocol for the synthesis of thiazole, thiazolone integrated pyrazole derivatives, under ultra-sonication technique. Thiazolone derivatives 5a, 5e, 5i, 5d, 5h, 5l were derived from [2+3] cyclocondensation reaction between carbothioamide pyrazoline (4 a-c) as S-N bi-nucleophile with DMAD/DEAD. The target molecules 5b, 5f, 5j,5c, 5g, 5k weresynthesized by reaction of (4 a-c) with substituted bromoethanone. Formation of the products was confirmed by FT-IR, 1H-NMR, 13C-NMR, LC-MS and X-ray analysis. Docking studies were carried out against the antimicrobial target (3UDI) to know interaction of the molecules (ligands) with the docked target. Among the docked compounds thiazolone derivative 5d showed the minimum binding energy of -9.08 kJ/mol with ligand efficiency of -0.23. All the synthesized compounds were examined primarily for their in-vitro antibacterial and antioxidant activity (IC50). Compound 5g (18±0.0) and 5d (19.5±0.5) showed significant bacterial inhibition against E.coli and S.aureus. Compound 5k (16.57) were showed substantial DPPH free radical inhibition activity as compared to the reference drug Ascorbic acid.

An efficient procedure was developed for the synthesis of different derivatives of 3,4-disubstituted pyrrole using TosMIC with ethyl cinnamate in DMF using lithium hydroxide monohydrate as a base. Further, trisubstituted pyrrole was synthesized using nitrostyrene, ethyl-propiolate and benzylamine in toluene as a reaction medium. This reaction was catalysed by lewis acid FeCl3. This strategy was further modified to synthesized tetra and penta substituted pyrrole using ethanol as a reaction medium keeping other conditions intact. This method is very economical and was successfully utilized for the synthesis of its derivatives with moderate to good yields.

The main aim of the present work is theoretical studies and docking analysis on the novel small molecule irilone as a progesterone receptor (PR) effect supporter in endometrial and ovarian cancer cell lines. The quantum mechanical computations are done using B3LYP/6-31+G(d,p) level of theory on the molecule under study at room temperature. The theoretical calculations showed that irilone is a stable small molecule with high electrophilicity property. The density of states (DOS) graph indicated that the virtual orbitals of the said compound have more density than the occupied orbitals. These studied indicated that the title compound can make a complex with progesterone receptor (PR) using steric and hydrogen bond (HB) interactions. The docking analysis showed that the receptor (PR-B isoform) residues Pro-696, Gln-725, Met-759, Arg-766, Glu-695, Asp-697, Leu-758, Lys-822, Ile-699, Val-698 and Trp-755 play main role in receptor-ligand complex formation.