Synthesis, characterization, molecular docking and in vitro antimalarial properties of new carboxamides bearing sulphonamide.

Sulphonamides and carboxamides have shown large number of pharmacological properties against different types of diseases among which is malaria. Twenty four new carboxamide derivatives bearing benzenesulphonamoyl alkanamides were synthesized and investigated for their in silico and in vitro antimalarial and antioxidant properties. The substituted benzenesulphonyl chlorides (1a-c) were treated with various amino acids (2a-h) to obtain the benzenesulphonamoyl alkanamides (3a-x) which were subsequently treated with benzoyl chloride to obtain the N-benzoylated derivatives (5a-f, i-n and q-v). Further reactions of the N-benzoylated derivatives or proline derivatives with 4-aminoacetophenone (6) using boric acid as a catalyst gave the sulphonamide carboxamide derivatives (7a-x) in excellent yields. The in vitro antimalarial studies showed that all synthesized compounds had antimalarial property. Compound 7k, 7c, 7l, 7s, and 7j had mean MIC value of 0.02, 0.03, 0.05, 0.06 and 0.08 µM respectively comparable with chloroquine 0.06 µM. Compound 7c was the most potent antioxidant agent with IC50 value of 0.045 mM comparable with 0.34 mM for ascorbic acid. In addition to the successful synthesis of the target molecules using boric acid catalysis, the compounds were found to have antimalarial and antioxidant activities comparable with known antimalarial and antioxidant drugs. The class of compounds reported herein have the potential of reducing oxidative stress arising from malaria parasite and chemotherapeutic agent used in the treatment of malaria.

Ecological and human health risk assessment of heavy metal contamination in soil of a municipal solid waste dump in Uyo, Nigeria.

The study assessed the levels of some heavy metals in soils in the vicinity of a municipal solid waste dumpsite with a view to providing information on the extent of contamination, ecological risk of metals in the soils and human health risk to the residents in Uyo. Soil samples were collected in rainy and dry seasons and analyzed for metals (Pb, Cd, Zn, Mn, Cr, Ni and Fe) using atomic absorption spectrometry. The concentrations of heavy metals (mg/kg) at the dumpsite in rainy season were Pb (9.90), Zn (137), Ni (12.56), Cr (3.60), Cd (9.05) and Mn (94.00), while in dry season, the concentrations were Pb (11.80), Zn (146), Ni (11.82), Cr (4.05), Cd (12.20) and Mn (91.20). The concentrations of metals in the studied sites were higher than that of the control site (P < 0.05). Pollution indices studies revealed that soil samples from dumpsite and distances from 10 and 20 m east of the dumpsite were highly polluted with cadmium. Ecological risk assessment carried out showed that cadmium contributed 98-99 % of the total potentially ecological risk. No probable health risk was observed as the total hazard index of all the metals was less than one. However, children were found to be more susceptible to heavy metal contamination than adult.

Analysis and Sources of Polycyclic Aromatic Hydrocarbons in Soil and Plant Samples of a Coal Mining Area in Nigeria.

This study analysed coal, plant and soil samples collected from the vicinity of Okobo coal mine in Nigeria for Polycyclic aromatic hydrocarbons (PAHs) and evaluated the sources of the PAH contamination in the environmental samples. The environmental samples were extracted by sonication using a ternary solvent system and analysed for 16 PAHs by gas chromatography-mass spectrometry (GC-MS). The results of the analysis of the samples identified some of the target PAHs. The ranges of total concentrations (in mg/kg) of PAHs in the coal, plant and soil samples were, 0.00-0.04, 0.00-0.16 and 0.00-0.01 respectively. The evaluation of the results of the PAH analysis of the environmental samples using diagnostic ratios revealed that the PAHs in the soil samples were mainly of petrogenic origin, while those in plant samples indicated mixture of petrogenic and pyrolytic origins.

Relationship between Sonographic Placental Thickness and Gestational Age in Normal Singleton Fetuses in Enugu, Southeast Nigeria.

BACKGROUND: The accuracy of common ultrasound parameters for the estimation of gestational age (GA) decreases as pregnancy advances in age. Hence, there is need to explore other parameters that may complement the established fetal biometric parameters in predicting GA in late pregnancy. AIM: The aim of this study is to determine the relationship between the sonographic placental thickness (PT) and GA in the second and third trimesters. SUBJECTS AND METHODS: A cross-sectional study of 627 normal pregnant women with GA between 14 and 40 weeks was conducted at the University of Nigeria Teaching Hospital Ituku-Ozalla, Enugu from May 2013 to February 2014 by sonography. Anteroposterior diameter of the placenta was measured at the level of the umbilical cord insertion. The last menstrual period of the women, femur length, biparietal diameter, head circumference, and abdominal circumference of the fetus were measured for GA estimation. Descriptive statistics, regression analysis, and independent sample t-test were used in statistical analysis. RESULTS: Mean PT was 23.2 (2.8) mm in the second trimester and 36.1 (3.6) mm in the third trimester. There was a significant difference between the values in the present study and values from similar studies in other populations (P < 0.04). There was a strong relationship between GA and PT and the following mathematical relationships for the second and third trimesters were obtained in the GA = 0.982 (PT) + 3.614 and GA = 0.977 (PT) + 3.354, respectively. CONCLUSION: Population-specific charts for PT may be used to estimate GA in the second and third trimesters.