Design, Synthesis of Pyrimidinothiazoles and Pyrimidinobenzimidazoles N-ethyl Carboxylic Acid Derivatives Analogs of 4-Quinolone
Molou Kouassi Yves Guillaume,
Timotou Adeyole,
Coulibaly Souleymane,
Camara Tchambaga Etienne,
Kablan Ahmont Landry Claude,
Coulibali Siomenan,
Sissouma Drissa
Issue:
Volume 10, Issue 4, December 2022
Pages:
106-112
Received:
6 October 2022
Accepted:
25 October 2022
Published:
4 November 2022
DOI:
10.11648/j.mc.20221004.11
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Abstract: Heterocycles containing pyrimidine and pyridine moieties are of great interest because they represent an important class of natural products such as nucleic acid, cytosine, and thymine. In addition, structural thiazole and benzimidazole subunits are present in various synthetic compounds, many of them have beneficial biological activities. The combination of these structures could beneficial in the discovery of new bioactive molecules and drugs. In this article, the synthesis of two series of new molecules derived from both pyrimidinothiazole (7a, 7b) and pyrimidinobenzimidazole carboxylic acids (9a-c) was presented. Structurally, these compounds are 4-quinolone analogs, which also possess medicinal properties. These compounds were synthesized by first developing ethyl pyrimidinothiazoles carboxylate (6a, 6b) and pyrimidinobenzimidazoles N-ethyl carboxylate (8a-c). Ethyl pyrimidinothiazoles carboxylate (6a, 6b) were synthesized by condensing ethyl ethoxymethylenemalonate with 2-amino-1,3-thiazoles (2a-b) at ethanol reflux. Pyrimidinobenzimidazoles carboxylate N-ethyl (8a-c) were obtained by an interaction between 2-aminobenzimidazoles (4a-c) and ethyl ethoxymethylenemalonate (5) followed by N-alkylation by the action of ethyl iodide in the presence of potassium carbonate. Obtained esters (6a, 6b) and (8a-c) were converted to the corresponding acids (7a, 7b) and (9a-c) by saponification with sodium hydroxide followed by neutralization with acetic acid. The structure of the compounds was confirmed by spectroscopic analysis of 1H, 13C-NMR and mass spectrometry.
Abstract: Heterocycles containing pyrimidine and pyridine moieties are of great interest because they represent an important class of natural products such as nucleic acid, cytosine, and thymine. In addition, structural thiazole and benzimidazole subunits are present in various synthetic compounds, many of them have beneficial biological activities. The comb...
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Syntheses, Antioxidant Activity and Crystal Structures of 1-Nicotinoyl-4-Phenylthiosemicarbazide and Its Derivative N-Phenyl-5-(Pyridin-3-yl)-1,3,4-Oxadiazol-2-amine
Ndama Faye,
Aissatou Alioune Gaye,
Alioune Fall,
Cheikh Ndoye,
Mayoro Diop,
Gregory Excoffier,
Mohamed Gaye
Issue:
Volume 10, Issue 4, December 2022
Pages:
113-120
Received:
23 November 2022
Accepted:
7 December 2022
Published:
15 December 2022
DOI:
10.11648/j.mc.20221004.12
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Abstract: The title compound C13H12N4OS (I) is synthetized from nicotinic hydrazide and isothiocynate. Compound C13H10N4O (II) is obtained upon reaction of (I) with Mn (II) salt. Compound I crystallizes in the triclinic space group Pī with the following unit cell parameters: a = 9.5667 (2) Å, b = 11.5464 (2) Å, c = 12.6658 (2) Å, a = 78.320 (1)°, b = 83.319 (1)°, g = 88.079 (2)°, V = 1360.73 (4) Å3, Z = 4, R1 = 0.040 and wR2 = 0.112 and compound II crystallizes in the monoclinic space group P21/n with the following unit cell parameters: a = 5.4055 (2) Å, b = 19.686 (1) Å, c = 10.5015 (4) Å, b = 92.402 (2)°, V = 1116.51 (8) Å3, Z = 4, R1 = 0.070 and wR2 = 0.212. The asymmetric unit contains two molecules of I. For both molecules, the carbonyl oxygen atom and the sulfur atom are, respectively, in syn and trans conformation with respect to their related amino nitrogen atoms. Strong intermolecular bonds of type N—H···N, N—H···S, and N—H···O, and weak intermolecular bonds of type C—H···O and C—H···S form chains superimposed on each other which are linked, resulting in a three-dimensional network architecture. The heterocyclic compound (II) 1,3,4-oxadiazol derivative is not planar with dihedral angle of 17.725 (14)° and 4.550 (15)° between 1,3,4-oxadiazole ring and phenyl and pyridine rings respectively. The dihedral angle between the phenyl and pyridine rings is 22.260 (12)°. In the compound II, intramolecular hydrogen bonds of type C—H···N resulting in S(6) ring stabilize the structure. One intermolecular hydrogen bonds of type N—H···N links the molecules thus forming a chain parallel to the c-axis.
Abstract: The title compound C13H12N4OS (I) is synthetized from nicotinic hydrazide and isothiocynate. Compound C13H10N4O (II) is obtained upon reaction of (I) with Mn (II) salt. Compound I crystallizes in the triclinic space group Pī with the following unit cell parameters: a = 9.5667 (2) Å, b = 11.5464 (2) Å, c = 12.6658 (2) Å, a = 78.320 (1)°, b = 83.319 ...
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Impact of Coal Fly Ash on the Concentration of Heavy Metals in Water, Soil and Plant Samples in Gansari, Around Cement Company of Northern Nigeria
Jibrin Noah Akoji,
Gidado Muhammad Junaid,
Ovurevu Oyiza Dorcas
Issue:
Volume 10, Issue 4, December 2022
Pages:
121-127
Received:
18 July 2022
Accepted:
30 September 2022
Published:
23 December 2022
DOI:
10.11648/j.mc.20221004.13
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Abstract: This study assessed the impact of Coal Fly Ash on the concentration of Heavy metals in water, soil, and vegetables (moringa and spinach) from Gansari village nearby Cement Company of Northern Nigeria in Sokoto State, Nigeria. Thesamples collected were digested, and analysed for heavy metals concentration using Atomic Absorption Spectroscopy. The results obtained from this study indicate that the concentrations of heavy metals Pb, Cd, Se, Ni, Fe in water samples are higher than the WHO/SON permissible limit, while the concentrations of Cu and Zn are below the WHO/SON standard limits, Mn in water is higher than the SON but lower than the WHO standards. In plants samples, the heavy metals accumulate in plant organs at different concentrations depending on the antioxidants defense mechanism developed by the plant cells and the level of their metal tolerance. The average concentrations of Pb, Mn, Cd, and Ni in all plant samples are higher than the permissible limit, while Cd is higher only in spinach sample. The bioaccumulation of the plant samples differs and the heavy metals are distributed in all parts of the plants samples, the roots of the spinach accumulates higher concentrations of heavy metals than the leaves and stem, while in moringa the leaves accumulates higher than the roots and stem. The concentrations of heavy metals in soil sample are below the targeted values proposed by World Health Organization (WHO). The heavy metals concentrations in water, soil, and plants samples were compared and it was shown that the plants samples have the highest concentrations of heavy metals than the water and soil samples. This shows that the water and plant samples from the study area have heavy metals concentrations above the permissible limit. These maybe due to the effect of the coal fly ash from Cement Company of Northern Nigeria, Sokoto that is nearby the study area, and with this it canbe concluded that the water and plants from the study area are not fit for human and animal consumption.
Abstract: This study assessed the impact of Coal Fly Ash on the concentration of Heavy metals in water, soil, and vegetables (moringa and spinach) from Gansari village nearby Cement Company of Northern Nigeria in Sokoto State, Nigeria. Thesamples collected were digested, and analysed for heavy metals concentration using Atomic Absorption Spectroscopy. The re...
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