Insa Seck - Academia.edu (original) (raw)
Papers by Insa Seck
Current Topics in Medicinal Chemistry, 2020
Background: 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biologi... more Background: 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biological activities are known. Researchers around the world are increasingly being interested in this emerging area, owing to its immense pharmacological scope. Objective: This work summarizes the synthesis of 1,2,3-triazoles and the significance of this pattern as a lead structure for new drug molecules discovery. Methods: 1,2,3-triazoles can be obtained on a multigram scale through “click chemistry” under ambient conditions. Results: Sixteen compounds were synthesized and evaluated on five microbial strains E. coli, E. faecalis, P. aeruginosa, S. aureus and C. albicans. NMR, MS and IR were used to characterize all compounds. They were evaluated with their Minimum Inhibitory Concentrations (MICs) and interesting results were obtained with compounds 12a, 12b, 3, 2a and 2c, with MIC 0.14 μM (P. aeruginosa), 1.08 μM (E. coli), 1.20 μM (E. faecalis and C. albicans), 3.5 μM (E. faecalis) and 4.24...
Results in Chemistry, 2021
The expansion of the novel coronavirus known as SARS-CoV-2 (severe acute respiratory syndrome cor... more The expansion of the novel coronavirus known as SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), COVID-19 (coronavirus disease 2019), or 2019-nCoV (2019 novel coronavirus) is a global concern over its pandemic potential. The need for therapeutic alternatives to stop this new pandemic is urgent. Nowadays, no efficacious therapy is available, and vaccines and drugs are underdeveloped to cure or prevent SARS-CoV-2 infections in many countries. Some vaccines candidates have been approved; however, a number of people are still skeptical of this coronavirus vaccines. Probably because of issues related to the quantity of the vaccine and a possible long-term side effects which are still being studied. The previous pandemics of infections caused by coronavirus, such as SARS-CoV in 2003, the Middle East respiratory syndrome coronavirus (MERS-CoV) in 2012, HCoV-229E, and HCoV-OC43 were described in the 1960 s,-HCoV-NL63 isolated in 2004, and HCoV-HKU1identified in 2005 prompted researchers to characterize many compounds against these viruses. Most of them could be potentially active against the currently emerging novel coronavirus. Five membered nitrogen heterocycles with a triazole, imidazole, and thiazole moiety are often found in many bioactive molecules such as coronavirus inhibitors. This present work summarizes to review the biological and structural studies of these compound types as coronavirus inhibitors.
Industrial & Engineering Chemistry Research
Medicinal Chemistry Research
Journal of Drug Delivery and Therapeutics
This study is part of the biological investigation of the chemical library of molecules already d... more This study is part of the biological investigation of the chemical library of molecules already described by the Laboratory of Organic Chemistry and Therapeutic Chemistry of the University of Bordeaux. The main objective was to explore the contribution of a thienyl moiety attached to the pyrimidinone nucleus, in the expression of an antimicrobial activity. The structural modifications mainly concerned the conservation or not of the benzo fragment attached to the thienyl, the saturation or not in position-1,2 of the pyrimidinone ring, the substitution on N-benzyl with more or less lipophilic units, the modification of the orientation of the thienyl fragment with, on the one hand, the compounds in which the sulfur is located near the N1 nitrogen (series of thieno[2,3-d]pyrimidin-4-ones) and on the other hand, compounds in which the sulfur is located near the ketone group (series of thieno[3,2-d]pyrimidin-4-ones). In general, thienyl fragment with sulfur located near the ketone grou...
Molecules, 2021
Amaryllidaceae plants are rich in alkaloids with biological properties. Pancratium trianthum is a... more Amaryllidaceae plants are rich in alkaloids with biological properties. Pancratium trianthum is an Amaryllidaceae species widely used in African folk medicine to treat several diseases such as central nervous system disorders, tumors, and microbial infections, and it is used to heal wounds. The current investigation explored the biological properties of alkaloid extracts from bulbs of P. trianthum collected in the Senegalese flora. Alkaloid extracts were analyzed and identified by chromatography and mass spectrometry. Alkaloid extracts from P. trianthum displayed pleiotropic biological properties. Cytotoxic activity of the extracts was determined on hepatocarcinoma Huh7 cells and on acute monocytic leukemia THP-1 cells, while agar diffusion and microdilution assays were used to evaluate antibacterial activity. Antiviral activity was measured by infection of extract-treated cells with dengue virus (DENVGFP) and human immunodeficiency virus-1 (HIV-1GFP) reporter vectors. Cytotoxicity ...
Current Topics in Medicinal Chemistry, 2020
Background: Due to the rapid development of microbial resistance, finding new molecules became ur... more Background: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. Objective: The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential. Methods: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433. Results: All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginos...
International Journal of Biological and Chemical Sciences, 2016
http://indexmedicus.afro.who.int Étude in vitro de l'effet antifalcémiant des globules rouges et ... more http://indexmedicus.afro.who.int Étude in vitro de l'effet antifalcémiant des globules rouges et de l'activité antioxydante d'extraits de la poudre de racines de Maytenus senegalensis Lam (Celestraceae)
International Journal of Biological and Chemical Sciences, 2015
L'objectif de cette étude est d'évaluer l'activité antifalcémiante d'extraits de racines de Lepta... more L'objectif de cette étude est d'évaluer l'activité antifalcémiante d'extraits de racines de Leptadenia hastata sur des hémoglobines falciformes et d'identifier les principes actifs à l'origine de cette activité. La méthode employée étudie la réversibilité des drépanocytes, en fonction du temps d'incubation des extraits par rapport aux témoins (eau physiologique, phénylalanine et arginine) sur des échantillons de sang de patients drépanocytaires homozygotes. Des concentrations de 0,05; 0,5; 5 et 10 mg/ml de quatre extraits (méthanol, hexane, acétate d'éthyle et méthanol résiduel) ont été mises en contact avec des drépanocytes de type SS après avoir provoqué leur falciformation avec une solution à 2% de métabisulfite de sodium. L'évaluation a été effectuée toutes les 30 minutes pendant 120 minutes. Les différents extraits ont montré une activité dosedépendante sur la réversibilité de la falciformation des globules rouges avec plus de 80% d'inversion en 120 minutes pour l'extrait méthanolique, le plus actif. Un screening phytochimique a permis de faire une corrélation entre les flavonoïdes et l'activité antifalcémiante des extraits de Leptadenia hastata.
Synthesis
Starting from commercially available stigmasterol,an efficient preparation of a cholesterol analo... more Starting from commercially available stigmasterol,an efficient preparation of a cholesterol analogue with a triazole ring was achieved, based on a [3 + 2]-cycloaddition of a cholesterol side chain terminal azide with a terminal acetylene.
Mediterranean Journal of Chemistry, 2015
Food Chemistry, 2012
... M. Lamsal, S. Koirala; Evaluation of new WHO diagnostic criteria for diabetes on the prevalen... more ... M. Lamsal, S. Koirala; Evaluation of new WHO diagnostic criteria for diabetes on the prevalence of abnormal glucose tolerance in heterogeneous Nepali population: The implication of measuring glycated hemoglobin. Singapore Medical Journal, 41 (2000), pp. 264–267. ...
South African Journal of Botany
Total phenolic, flavonoid and tannin contents together with antioxidant and pro-oxidant activitie... more Total phenolic, flavonoid and tannin contents together with antioxidant and pro-oxidant activities of Carapa procera were investigated. The antioxidant activity of Carapa procera was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, ferric reducing/ antioxidant power (FRAP) method and 2,2 0-azino bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assay. The study of pro-oxidant activity was based on the power producing of iron ion in the Fenton reaction. The total phenolic content (TPC) of the extract was exhibiting high value of 8.2 mg gallic acid equivalents (GAE)/ g of dried Carapa. The study revealed a low percentage of flavonoids 0.04% in the extract and 0.24 mg of tannic acid equivalents (TAE)/g of dried Carapa for the tannin content (TC). Proanthocyanidins were less represented among the tannins 6.80% of the extract. The chromatographic fingerprints showed the presence of tannins and acid, like (+)-catechin, epicatechin, trans-4-hyroxicinnamic, 3,4-dihydroxicinnamic and acid chlorogenic. Carapa procera exhibited high antioxidant activity in the both DPPH and ABTS assays, being 10.45 mg Vitamin C equivalents/g of dried Carapa and 500 mmol Trolox/g of dried Carapa, respectively. The FRAP gave a good result 2.45 mg Vitamin C equivalents /g of dried Carapa. The pro-oxidant activity was 24.25 mg/ml of Carapa extract. The phytochemical screening was the subject of intensive investigations in order to identify the chemical constituents present in medicinal plants, such as Carapa procera and to evaluate their potential biological activities.
![Research paper thumbnail of Syntheses and crystal structure of 4-[(pyridin-3-yl)diazenyl]morpholine and 1-[(pyridin-3-yl)diazenyl]-1,2,3,4-tetrahydroquinoline](https://attachments.academia-assets.com/100304653/thumbnails/1.jpg)
](Acta Crystallographica Section E: Crystallographic Communications, Jan 10, 2023
Two new heterocyclic 1,2,3-triazenes were synthesized by diazotation of 3-aminopyridine following... more Two new heterocyclic 1,2,3-triazenes were synthesized by diazotation of 3-aminopyridine following respectively by coupling with morpholine or 1,2,3,4-tetrahydroquinoline. 4-[(Pyridin-3-yl)diazenyl]morpholine (I), C 9 H 12 N 4 O, has monoclinic P2 1 /c symmetry at 100 K, while 1-[(pyridin-3-yl)diazenyl]-1,2,3,4tetrahydroquinoline (II), C 14 H 14 N 4 , has monoclinic P2 1 /n symmetry at 100 K. These 1,2,3-triazene derivatives were synthesized by the organic medium method by coupling reactions of 3-aminopyridine with morpholine and 1,2,3,4tetrahydroquinoline, respectively, and characterized by 1 H NMR, 13 C NMR, IR, mass spectrometry, and single-crystal X-ray diffraction. The molecule of compound I consists of pyridine and morpholine rings connected by an azo moiety (-N N-). In the molecule of II, the pyridine ring and the 1,2,3,4tetrahydroquinoline unit are also connected by an azo moiety. The double-and single-bond distances in the triazene chain are comparable for the two compounds. In both crystal structures, the molecules are connected by C-HÁ Á ÁN interactions, forming infinite chains for I and layers parallel to the bc plane for II.
Click chemistry approach to ionic liquids (ILs) supported organic synthesis
Tetrahedron Letters, 2015
ABSTRACT A series of 1,3,4-trialkyl-1,2,3-triazolium ionic liquids were synthesized via click che... more ABSTRACT A series of 1,3,4-trialkyl-1,2,3-triazolium ionic liquids were synthesized via click chemistry and used as reaction media for the Morita-Baylis-Hillman (MBH) reaction.
Current Topics in Medicinal Chemistry
Background: Due to the rapid development of microbial resistance, finding new molecules became ur... more Background: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. Objective: The objective of this work is to access to 1,2,3-triazene-1,3-disubstituted, a class of molecule with a high therapeutic potential. Method: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: three gram (-): Escherichia coli ATCC 25921, Enterococcus faecalis ATCC 29212 and Pseudomonas aeruginosa ATCC 27253; one gram (+) strain: Staphylococcus aureus ATCC 38213; and one fungi: Candida albicans ATCC 24433. Results: All strains were sensitive and the best MIC, 0.28 μM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with very good MIC 0.32 μM against Escherichia coli and Pseudomonas aer...
British Journal of Applied Science & Technology, 2017
Current Topics in Medicinal Chemistry, 2020
Background: 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biologi... more Background: 1,2,3-triazoles are five-membered heterocyclic scaffold; their broad-spectrum biological activities are known. Researchers around the world are increasingly being interested in this emerging area, owing to its immense pharmacological scope. Objective: This work summarizes the synthesis of 1,2,3-triazoles and the significance of this pattern as a lead structure for new drug molecules discovery. Methods: 1,2,3-triazoles can be obtained on a multigram scale through “click chemistry” under ambient conditions. Results: Sixteen compounds were synthesized and evaluated on five microbial strains E. coli, E. faecalis, P. aeruginosa, S. aureus and C. albicans. NMR, MS and IR were used to characterize all compounds. They were evaluated with their Minimum Inhibitory Concentrations (MICs) and interesting results were obtained with compounds 12a, 12b, 3, 2a and 2c, with MIC 0.14 μM (P. aeruginosa), 1.08 μM (E. coli), 1.20 μM (E. faecalis and C. albicans), 3.5 μM (E. faecalis) and 4.24...
Results in Chemistry, 2021
The expansion of the novel coronavirus known as SARS-CoV-2 (severe acute respiratory syndrome cor... more The expansion of the novel coronavirus known as SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2), COVID-19 (coronavirus disease 2019), or 2019-nCoV (2019 novel coronavirus) is a global concern over its pandemic potential. The need for therapeutic alternatives to stop this new pandemic is urgent. Nowadays, no efficacious therapy is available, and vaccines and drugs are underdeveloped to cure or prevent SARS-CoV-2 infections in many countries. Some vaccines candidates have been approved; however, a number of people are still skeptical of this coronavirus vaccines. Probably because of issues related to the quantity of the vaccine and a possible long-term side effects which are still being studied. The previous pandemics of infections caused by coronavirus, such as SARS-CoV in 2003, the Middle East respiratory syndrome coronavirus (MERS-CoV) in 2012, HCoV-229E, and HCoV-OC43 were described in the 1960 s,-HCoV-NL63 isolated in 2004, and HCoV-HKU1identified in 2005 prompted researchers to characterize many compounds against these viruses. Most of them could be potentially active against the currently emerging novel coronavirus. Five membered nitrogen heterocycles with a triazole, imidazole, and thiazole moiety are often found in many bioactive molecules such as coronavirus inhibitors. This present work summarizes to review the biological and structural studies of these compound types as coronavirus inhibitors.
Industrial & Engineering Chemistry Research
Medicinal Chemistry Research
Journal of Drug Delivery and Therapeutics
This study is part of the biological investigation of the chemical library of molecules already d... more This study is part of the biological investigation of the chemical library of molecules already described by the Laboratory of Organic Chemistry and Therapeutic Chemistry of the University of Bordeaux. The main objective was to explore the contribution of a thienyl moiety attached to the pyrimidinone nucleus, in the expression of an antimicrobial activity. The structural modifications mainly concerned the conservation or not of the benzo fragment attached to the thienyl, the saturation or not in position-1,2 of the pyrimidinone ring, the substitution on N-benzyl with more or less lipophilic units, the modification of the orientation of the thienyl fragment with, on the one hand, the compounds in which the sulfur is located near the N1 nitrogen (series of thieno[2,3-d]pyrimidin-4-ones) and on the other hand, compounds in which the sulfur is located near the ketone group (series of thieno[3,2-d]pyrimidin-4-ones). In general, thienyl fragment with sulfur located near the ketone grou...
Molecules, 2021
Amaryllidaceae plants are rich in alkaloids with biological properties. Pancratium trianthum is a... more Amaryllidaceae plants are rich in alkaloids with biological properties. Pancratium trianthum is an Amaryllidaceae species widely used in African folk medicine to treat several diseases such as central nervous system disorders, tumors, and microbial infections, and it is used to heal wounds. The current investigation explored the biological properties of alkaloid extracts from bulbs of P. trianthum collected in the Senegalese flora. Alkaloid extracts were analyzed and identified by chromatography and mass spectrometry. Alkaloid extracts from P. trianthum displayed pleiotropic biological properties. Cytotoxic activity of the extracts was determined on hepatocarcinoma Huh7 cells and on acute monocytic leukemia THP-1 cells, while agar diffusion and microdilution assays were used to evaluate antibacterial activity. Antiviral activity was measured by infection of extract-treated cells with dengue virus (DENVGFP) and human immunodeficiency virus-1 (HIV-1GFP) reporter vectors. Cytotoxicity ...
Current Topics in Medicinal Chemistry, 2020
Background: Due to the rapid development of microbial resistance, finding new molecules became ur... more Background: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. Objective: The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential. Methods: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433. Results: All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginos...
International Journal of Biological and Chemical Sciences, 2016
http://indexmedicus.afro.who.int Étude in vitro de l'effet antifalcémiant des globules rouges et ... more http://indexmedicus.afro.who.int Étude in vitro de l'effet antifalcémiant des globules rouges et de l'activité antioxydante d'extraits de la poudre de racines de Maytenus senegalensis Lam (Celestraceae)
International Journal of Biological and Chemical Sciences, 2015
L'objectif de cette étude est d'évaluer l'activité antifalcémiante d'extraits de racines de Lepta... more L'objectif de cette étude est d'évaluer l'activité antifalcémiante d'extraits de racines de Leptadenia hastata sur des hémoglobines falciformes et d'identifier les principes actifs à l'origine de cette activité. La méthode employée étudie la réversibilité des drépanocytes, en fonction du temps d'incubation des extraits par rapport aux témoins (eau physiologique, phénylalanine et arginine) sur des échantillons de sang de patients drépanocytaires homozygotes. Des concentrations de 0,05; 0,5; 5 et 10 mg/ml de quatre extraits (méthanol, hexane, acétate d'éthyle et méthanol résiduel) ont été mises en contact avec des drépanocytes de type SS après avoir provoqué leur falciformation avec une solution à 2% de métabisulfite de sodium. L'évaluation a été effectuée toutes les 30 minutes pendant 120 minutes. Les différents extraits ont montré une activité dosedépendante sur la réversibilité de la falciformation des globules rouges avec plus de 80% d'inversion en 120 minutes pour l'extrait méthanolique, le plus actif. Un screening phytochimique a permis de faire une corrélation entre les flavonoïdes et l'activité antifalcémiante des extraits de Leptadenia hastata.
Synthesis
Starting from commercially available stigmasterol,an efficient preparation of a cholesterol analo... more Starting from commercially available stigmasterol,an efficient preparation of a cholesterol analogue with a triazole ring was achieved, based on a [3 + 2]-cycloaddition of a cholesterol side chain terminal azide with a terminal acetylene.
Mediterranean Journal of Chemistry, 2015
Food Chemistry, 2012
... M. Lamsal, S. Koirala; Evaluation of new WHO diagnostic criteria for diabetes on the prevalen... more ... M. Lamsal, S. Koirala; Evaluation of new WHO diagnostic criteria for diabetes on the prevalence of abnormal glucose tolerance in heterogeneous Nepali population: The implication of measuring glycated hemoglobin. Singapore Medical Journal, 41 (2000), pp. 264–267. ...
South African Journal of Botany
Total phenolic, flavonoid and tannin contents together with antioxidant and pro-oxidant activitie... more Total phenolic, flavonoid and tannin contents together with antioxidant and pro-oxidant activities of Carapa procera were investigated. The antioxidant activity of Carapa procera was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, ferric reducing/ antioxidant power (FRAP) method and 2,2 0-azino bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assay. The study of pro-oxidant activity was based on the power producing of iron ion in the Fenton reaction. The total phenolic content (TPC) of the extract was exhibiting high value of 8.2 mg gallic acid equivalents (GAE)/ g of dried Carapa. The study revealed a low percentage of flavonoids 0.04% in the extract and 0.24 mg of tannic acid equivalents (TAE)/g of dried Carapa for the tannin content (TC). Proanthocyanidins were less represented among the tannins 6.80% of the extract. The chromatographic fingerprints showed the presence of tannins and acid, like (+)-catechin, epicatechin, trans-4-hyroxicinnamic, 3,4-dihydroxicinnamic and acid chlorogenic. Carapa procera exhibited high antioxidant activity in the both DPPH and ABTS assays, being 10.45 mg Vitamin C equivalents/g of dried Carapa and 500 mmol Trolox/g of dried Carapa, respectively. The FRAP gave a good result 2.45 mg Vitamin C equivalents /g of dried Carapa. The pro-oxidant activity was 24.25 mg/ml of Carapa extract. The phytochemical screening was the subject of intensive investigations in order to identify the chemical constituents present in medicinal plants, such as Carapa procera and to evaluate their potential biological activities.
Acta Crystallographica Section E: Crystallographic Communications, Jan 10, 2023
Two new heterocyclic 1,2,3-triazenes were synthesized by diazotation of 3-aminopyridine following... more Two new heterocyclic 1,2,3-triazenes were synthesized by diazotation of 3-aminopyridine following respectively by coupling with morpholine or 1,2,3,4-tetrahydroquinoline. 4-[(Pyridin-3-yl)diazenyl]morpholine (I), C 9 H 12 N 4 O, has monoclinic P2 1 /c symmetry at 100 K, while 1-[(pyridin-3-yl)diazenyl]-1,2,3,4tetrahydroquinoline (II), C 14 H 14 N 4 , has monoclinic P2 1 /n symmetry at 100 K. These 1,2,3-triazene derivatives were synthesized by the organic medium method by coupling reactions of 3-aminopyridine with morpholine and 1,2,3,4tetrahydroquinoline, respectively, and characterized by 1 H NMR, 13 C NMR, IR, mass spectrometry, and single-crystal X-ray diffraction. The molecule of compound I consists of pyridine and morpholine rings connected by an azo moiety (-N N-). In the molecule of II, the pyridine ring and the 1,2,3,4tetrahydroquinoline unit are also connected by an azo moiety. The double-and single-bond distances in the triazene chain are comparable for the two compounds. In both crystal structures, the molecules are connected by C-HÁ Á ÁN interactions, forming infinite chains for I and layers parallel to the bc plane for II.
Click chemistry approach to ionic liquids (ILs) supported organic synthesis
Tetrahedron Letters, 2015
ABSTRACT A series of 1,3,4-trialkyl-1,2,3-triazolium ionic liquids were synthesized via click che... more ABSTRACT A series of 1,3,4-trialkyl-1,2,3-triazolium ionic liquids were synthesized via click chemistry and used as reaction media for the Morita-Baylis-Hillman (MBH) reaction.
Current Topics in Medicinal Chemistry
Background: Due to the rapid development of microbial resistance, finding new molecules became ur... more Background: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. Objective: The objective of this work is to access to 1,2,3-triazene-1,3-disubstituted, a class of molecule with a high therapeutic potential. Method: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: three gram (-): Escherichia coli ATCC 25921, Enterococcus faecalis ATCC 29212 and Pseudomonas aeruginosa ATCC 27253; one gram (+) strain: Staphylococcus aureus ATCC 38213; and one fungi: Candida albicans ATCC 24433. Results: All strains were sensitive and the best MIC, 0.28 μM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with very good MIC 0.32 μM against Escherichia coli and Pseudomonas aer...
British Journal of Applied Science & Technology, 2017