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3. Synthesis, Characterization and Theoretical Investigations on the Molecular Structure, Electronic Property and anti-Trypanosomal Activity of Benzenesulphonamide-Based Carboxamide and Its Derivatives.

Author

Asogwa, Fredrick C., Izuchukwu, Ugwu D., Louis, Hitler, Eze, Cosmas C., Ekeleme, Chinedu M., Ezugwu, James A., Benjamin, Innocent, Attah, Solomon I., Agwamba, Ernest C., Ekoh, Ogechi C., and Adeyinka, Adedapo S.

Subjects
ACETAMIDE derivatives, ACETAMIDE, MOLECULAR structure, CARBOXAMIDES, DRUG discovery, PHARMACEUTICAL chemistry, BINDING energy
Abstract

Sulfonamide-based carboxamide drugs have multiple active sites that confers them with a variety of chemical and pharmacological activities. The combination of structural functionalities has been established to be vital in the drug discovery process. The synthesis of novel, nontoxic, cheap and effective anti-parasitic analogues is a trending aspect of pharmaceutical and medicinal chemistry research. In this research, the synthesis, characterization, and density functional theory (DFT) investigation of the reactivity and anti-trypanosomal simulation of benzenesulphonamide-based carboxamide derivatives was carried out for 2-[N-(benzenesulfonyl)-1-phenylformamido]-N-(4-nitrophenyl)acetamide(BPNA), 2-[N-(benzenesulfonyl)-1-phenylformamido]-N-(4-nitrophenyl)-3-phenylpropanamide (BPNPP), 2-[N-(benzenesulfonyl)-1-phenylformamido]-3-(1H-indol-2-yl)-N-(4-nitrophenyl)propenamide (BPINP) and 2-[N-(benzenesulfonyl)-1-phenylformamido]-4-methyl-N-(4-nitrophenyl)pentanamide (BPMNP) following an environmentally friendly zinc chloride catalyst mediated synthesis. The lower value of the HOMO-LUMO energy gap (2.9756 eV) observed for BPMNP indicated its higher chemical and biological activity. The global electrophilicity index (ω), which is related to chemical hardness and chemical potential in line with other global descriptors showed that the order of reactivity is BPMNP > BPINP > BPNPP > BPNA. The NBO analysis showed that σ → σ*, σ* →π*, π → π*, and π* → π* transitions were observed in all the compounds while σ → σ* and π* → π* showed the lowest and the highest stabilization energy, respectively. From the molecular docking analysis, BPMNP again, showed the most stable binding energy of − 9.6 kcal/mol and bond length of 1.99 Å, evidently performing better than the standard drug with binding energy and bond length of −7.6 kcal/mol and 2.89 Å, respectively. The binding energy obtained was observed to follow a decreasing order as thus; BPMNP > BPINP > BPNA > BPNPP which strongly indicates alkane-substituted benzenesulphonamide carboxamides especially BPINP and BPMNP possess potent curative properties against trypanosomiasis. [ABSTRACT FROM AUTHOR]

Published
2023
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4. Novel Cholinesterase Inhibitors:Synthesis, in silico and in vitro Studies

Author

Ekerendu, Effiong E., Okoro, Uchechukwu C., Eze, Cosmas C., Khanye, David S., Omeje, Kingsley O., Mishra, Narendra K., Ugwu, David I., Ekerendu, Effiong E., Okoro, Uchechukwu C., Eze, Cosmas C., Khanye, David S., Omeje, Kingsley O., Mishra, Narendra K., and Ugwu, David I.

Abstract

The synthesis of new functionalized linear diaza and triaza phenothiazine and phenoxazines and their in silico and in vitro anti-Alzheimer activity is reported. Fifteen new amide derivatives (8-11 & 13-24) were synthesized by the reactions of phenothiazines/phenoxazine (6 or 12) and various aliphatic and aromatic primary amides (7) in the presence of nickel catalyst and anhydrous potassium carbonate under nitrogen atmosphere. The FTIR, 1H NMR, 13C NMR and HR-MS spectra of the synthesized compounds were in agreement with the assigned structures. All the 15 new derivatives were screened for their in silico and in vitro anti-Alzheimer's activity using the inhibition of acetylcholinesterase and butyrylcholinesterase. The results of the in silico experiment showed that most of the synthesized derivatives had good binding energies, binding interaction and bond distances. The most active derivatives in the in silico studies was compounds 18 (-12.5 and -11.5 kcal/mol) against acetylcholinesterase and butyrylcholinesterase, respectively. In addition, compound 18 had the best in vitro inhibitory activity against acetylcholinesterase and butyrylcholinesterase (99.37% and 82.35%). The results of in silico experiment were greatly in agreement with the results of in vitro studies. The structure-activity relationship studies revealed that the phenothiazine derivatives had better in silico and in vitro activities. Furthermore, 2-substitutted phenothiazines had better activity than the unsubstituted phenothiazines. The synthesized compounds showed promising in silico and in vitro activities against acetylcholinesterase and butyrylcholinesterase and as such could be further developed for the treatment of Alzheimer's disease.

Published
2023

5. Synthesis, Characterization and Theoretical Investigations on the Molecular Structure, Electronic Property and anti-Trypanosomal Activity of Benzenesulphonamide-Based Carboxamide and Its Derivatives

Author

Asogwa, Fredrick C., primary, Izuchukwu, Ugwu D., additional, Louis, Hitler, additional, Eze, Cosmas C., additional, Ekeleme, Chinedu M., additional, Ezugwu, James A., additional, Benjamin, Innocent, additional, Attah, Solomon I., additional, Agwamba, Ernest C., additional, Ekoh, Ogechi C., additional, and Adeyinka, Adedapo S., additional

Published
2022
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6. Synthesis and Biological Properties of some New Lead Sulphonamide and Carboxamide Scaffolds Bearing Coumarin Moieties

Author

Eze, Cosmas C., Ezeokonkwo, Mercy Amarachukwu, Ezema, Benjamin Ebere, Onoabedje, Abraham Efeturi, and Ugwu, David Izuchukwu

Abstract

Coumarin, sulphonamide, and amide scaffolds exhibit diverse pharmacological features and constitute an important class of therapeutic agents. In this review, we have discussed the synthesis, biological properties, and SAR of coumarins containing sulphonamide or amide group in the last seven years. Many reviews on the therapeutic activities of coumarins, sulphonamides, and amides have been published. Hence the authors focused on coumarin-linked sulphonamide or amide scaffolds. The review provides information on the synthetic route to new coumarins containing sulphonamide or amide groups with improved pharmacological properties.

Published
2021
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7. One-Pot Multicomponent Synthesis of Imidazole Rings in Acidic Ionic Liquids: A Review

Author

Eze, Cosmas C., Ezeokonkwo, Mercy Amarachi, Ezema, Benjamin Ebere, Onoabedje, Abraham Efeturi, Ibeanu, Fidelia Ngozika, Ugwu, David Izuchukwu, Onyeyilim, Leonard Ebuka, and Ezugwu, James Anayochwkwu

Abstract

The design of the environmentally friendly approach to the synthesis of biologically important compounds without compromising the yield has been the focus of many chemists in recent years. The development of the one-pot synthesis of heterocycles in the presence of Ionic Liquids (ILs), used as both environmental media and catalysts, is efficient and environmentally sustainable. This review highlights the one-pot synthesis of imidazoles in acidic ILs in the past decade. Some reviews have been conducted on imidazoles, such as their pharmacological importance. Hence, we decided to focus on their synthesis in acidic ionic liquids, which the authors are not aware of any published literature.

Published
2020
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