The Experts below are selected from a list of 750 Experts worldwide ranked by ideXlab platform
Gonzalez Calderon Davir - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and antifungal activity of novel oxazolidin-2-one linked-1,2,3-triazole derivatives
MedChemComm, 2017Co-Authors: Ramirez Villalva Alejandra, Gonzalez Calderon Davir, Rojas García Roxana, Gonzalez Romero Carlos, Tamariz Mascarua Joaquin, Morales Rodriguez Macario, Zavala Segovia, MarÍa De Las Nieves, Fuentes Benites, Maria Paulina Aydee GraciaAbstract:Artículo IndizadoNovel oxazolidin-2-one-linked 1,2,3-triazole derivatives (4a–k) were synthesized by straightforward and versatile azide–enolate (3 + 2) cycloaddition. The series of compounds was screened for antifungal activity against four filamentous fungi as well as six yeast species of Candida spp. According to their efficiency and breadth of scope, they can be ordered as 4k > 4d > 4h > 4a, especially in relation to the activity displayed against Candida glabrata ATCC-34138, Trichosporon Cutaneum ATCC-28592 and Mucor hiemalis ATCC-8690, i.e. compounds 4d, 4h and 4k showed excellent activity against C. glabrata (MIC 0.12, 0.25 and 0.12 μg mL−1, respectively), better than that of itraconazole (MIC 1 μg ml−1). The activity of compound 4d (MIC = 2 μg mL− 1) was higher than that observed for the standard antifungal drug (MIC = 8 μg mL−1) against Trichosporon Cutaneum, while compound 4k displayed an excellent antimycotic activity against Mucor hiemalis (MIC = 2 μg mL−1 vs. 4 μg mL−1 for itraconazole). In addition, we describe herein a novel mild and eco-friendly synthetic protocol for obtaining β-ketosulfones (adducts to afford compounds 4a–k) from α-brominated carbonyls in an aqueous nanomicellar medium at room temperature.CONACYT, Secretaría de Investigación de Estudios Avanzados de la UAE
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Antifungal activity of 10-homo-N-1,2,3-triazol-bicyclic carbonucleosides: A novel type of compound afforded by azide-enolate (3+2) cycloaddition
T.D.H. Bugg, 2016Co-Authors: Gonzalez Romero Carlos, Ramirez Villalva Alejandra, Morales Rodriguez Macario, Fuentes-benítes Aydee, Aguirre De Paz, José Guadalupe, Morales-reza, Marco Antonio, Mejía-dionicio, María Guadalupe, Gonzalez Calderon DavirAbstract:The first report of 1′-homo-N-1,2,3-triazol-bicyclic carbonucleosides (7a and 7b) is described herein. Azide-enolate (3+2) cycloaddition afforded the synthesis of this novel type of compound. Antifungal activity was evaluated in vitro against four filamentous fungi (Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae and Mucor hiemalis) as well as nine species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 7a and 7b are promising candidates for complementary biological studies due to their good activity against Candida spp.Secretaria de Investigación y Estudios Avanzados (SIEA) de la Universidad autónoma del Estado de México (UAEMex
Carlos Gonzalezromero - One of the best experts on this subject based on the ideXlab platform.
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antifungal activity of 1 homo n 1 2 3 triazol bicyclic carbonucleosides a novel type of compound afforded by azide enolate 3 2 cycloaddition
Bioorganic Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Jose Aguirrede G Paz, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Aydee Fuentesbenites, Carlos GonzalezromeroAbstract:The first report of 1'-homo-N-1,2,3-triazol-bicyclic carbonucleosides (7a and 7b) is described herein. Azide-enolate (3+2) cycloaddition afforded the synthesis of this novel type of compound. Antifungal activity was evaluated in vitro against four filamentous fungi (Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae and Mucor hiemalis) as well as nine species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 7a and 7b are promising candidates for complementary biological studies due to their good activity against Candida spp.
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azide enolate 1 3 dipolar cycloaddition in the synthesis of novel triazole based miconazole analogues as promising antifungal agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Eduardo Diaztorres, Aydee FuentesbenitesAbstract:Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.
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a facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity
European Journal of Medicinal Chemistry, 2015Co-Authors: Alejandra Ramirezvillalva, Davir Gonzalezcalderon, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Erick Cuevasyanez, Aydee FuentesbenitesAbstract:Abstract Four novel miconazole analogues ( 8 – 11 ) were synthetized and evaluated for activity against four filamentous fungi ( Mucor hiemalis , Aspergillus fumigatus , Trichosporon Cutaneum , and Rhizopus oryzae ) and eight species of Candida as yeast specimens. Compounds 9 and 10 showed very good activity when evaluated in yeast (MIC 0.112 and 0.163 μg/mL) compared to the reference compound, itraconazole (MIC 0.067 μg/mL). The best antifungal activity in filamentous strains was shown by compound 9 . Hence compounds 9 and 10 represent new leads for further pharmacomodulation in this series.
Davir Gonzalezcalderon - One of the best experts on this subject based on the ideXlab platform.
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antifungal activity of 1 homo n 1 2 3 triazol bicyclic carbonucleosides a novel type of compound afforded by azide enolate 3 2 cycloaddition
Bioorganic Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Jose Aguirrede G Paz, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Aydee Fuentesbenites, Carlos GonzalezromeroAbstract:The first report of 1'-homo-N-1,2,3-triazol-bicyclic carbonucleosides (7a and 7b) is described herein. Azide-enolate (3+2) cycloaddition afforded the synthesis of this novel type of compound. Antifungal activity was evaluated in vitro against four filamentous fungi (Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae and Mucor hiemalis) as well as nine species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 7a and 7b are promising candidates for complementary biological studies due to their good activity against Candida spp.
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azide enolate 1 3 dipolar cycloaddition in the synthesis of novel triazole based miconazole analogues as promising antifungal agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Eduardo Diaztorres, Aydee FuentesbenitesAbstract:Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.
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a facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity
European Journal of Medicinal Chemistry, 2015Co-Authors: Alejandra Ramirezvillalva, Davir Gonzalezcalderon, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Erick Cuevasyanez, Aydee FuentesbenitesAbstract:Abstract Four novel miconazole analogues ( 8 – 11 ) were synthetized and evaluated for activity against four filamentous fungi ( Mucor hiemalis , Aspergillus fumigatus , Trichosporon Cutaneum , and Rhizopus oryzae ) and eight species of Candida as yeast specimens. Compounds 9 and 10 showed very good activity when evaluated in yeast (MIC 0.112 and 0.163 μg/mL) compared to the reference compound, itraconazole (MIC 0.067 μg/mL). The best antifungal activity in filamentous strains was shown by compound 9 . Hence compounds 9 and 10 represent new leads for further pharmacomodulation in this series.
Ramirez Villalva Alejandra - One of the best experts on this subject based on the ideXlab platform.
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Synthesis and antifungal activity of novel oxazolidin-2-one linked-1,2,3-triazole derivatives
MedChemComm, 2017Co-Authors: Ramirez Villalva Alejandra, Gonzalez Calderon Davir, Rojas García Roxana, Gonzalez Romero Carlos, Tamariz Mascarua Joaquin, Morales Rodriguez Macario, Zavala Segovia, MarÍa De Las Nieves, Fuentes Benites, Maria Paulina Aydee GraciaAbstract:Artículo IndizadoNovel oxazolidin-2-one-linked 1,2,3-triazole derivatives (4a–k) were synthesized by straightforward and versatile azide–enolate (3 + 2) cycloaddition. The series of compounds was screened for antifungal activity against four filamentous fungi as well as six yeast species of Candida spp. According to their efficiency and breadth of scope, they can be ordered as 4k > 4d > 4h > 4a, especially in relation to the activity displayed against Candida glabrata ATCC-34138, Trichosporon Cutaneum ATCC-28592 and Mucor hiemalis ATCC-8690, i.e. compounds 4d, 4h and 4k showed excellent activity against C. glabrata (MIC 0.12, 0.25 and 0.12 μg mL−1, respectively), better than that of itraconazole (MIC 1 μg ml−1). The activity of compound 4d (MIC = 2 μg mL− 1) was higher than that observed for the standard antifungal drug (MIC = 8 μg mL−1) against Trichosporon Cutaneum, while compound 4k displayed an excellent antimycotic activity against Mucor hiemalis (MIC = 2 μg mL−1 vs. 4 μg mL−1 for itraconazole). In addition, we describe herein a novel mild and eco-friendly synthetic protocol for obtaining β-ketosulfones (adducts to afford compounds 4a–k) from α-brominated carbonyls in an aqueous nanomicellar medium at room temperature.CONACYT, Secretaría de Investigación de Estudios Avanzados de la UAE
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Antifungal activity of 10-homo-N-1,2,3-triazol-bicyclic carbonucleosides: A novel type of compound afforded by azide-enolate (3+2) cycloaddition
T.D.H. Bugg, 2016Co-Authors: Gonzalez Romero Carlos, Ramirez Villalva Alejandra, Morales Rodriguez Macario, Fuentes-benítes Aydee, Aguirre De Paz, José Guadalupe, Morales-reza, Marco Antonio, Mejía-dionicio, María Guadalupe, Gonzalez Calderon DavirAbstract:The first report of 1′-homo-N-1,2,3-triazol-bicyclic carbonucleosides (7a and 7b) is described herein. Azide-enolate (3+2) cycloaddition afforded the synthesis of this novel type of compound. Antifungal activity was evaluated in vitro against four filamentous fungi (Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae and Mucor hiemalis) as well as nine species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 7a and 7b are promising candidates for complementary biological studies due to their good activity against Candida spp.Secretaria de Investigación y Estudios Avanzados (SIEA) de la Universidad autónoma del Estado de México (UAEMex
Aydee Fuentesbenites - One of the best experts on this subject based on the ideXlab platform.
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antifungal activity of 1 homo n 1 2 3 triazol bicyclic carbonucleosides a novel type of compound afforded by azide enolate 3 2 cycloaddition
Bioorganic Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Jose Aguirrede G Paz, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Aydee Fuentesbenites, Carlos GonzalezromeroAbstract:The first report of 1'-homo-N-1,2,3-triazol-bicyclic carbonucleosides (7a and 7b) is described herein. Azide-enolate (3+2) cycloaddition afforded the synthesis of this novel type of compound. Antifungal activity was evaluated in vitro against four filamentous fungi (Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae and Mucor hiemalis) as well as nine species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 7a and 7b are promising candidates for complementary biological studies due to their good activity against Candida spp.
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azide enolate 1 3 dipolar cycloaddition in the synthesis of novel triazole based miconazole analogues as promising antifungal agents
European Journal of Medicinal Chemistry, 2016Co-Authors: Davir Gonzalezcalderon, Maria G Mejiadionicio, Marco A Moralesreza, Alejandra Ramirezvillalva, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Eduardo Diaztorres, Aydee FuentesbenitesAbstract:Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon Cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.
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a facile synthesis of novel miconazole analogues and the evaluation of their antifungal activity
European Journal of Medicinal Chemistry, 2015Co-Authors: Alejandra Ramirezvillalva, Davir Gonzalezcalderon, Macario Moralesrodriguez, Carlos Gonzalezromero, Bertha Jaureguirodriguez, Erick Cuevasyanez, Aydee FuentesbenitesAbstract:Abstract Four novel miconazole analogues ( 8 – 11 ) were synthetized and evaluated for activity against four filamentous fungi ( Mucor hiemalis , Aspergillus fumigatus , Trichosporon Cutaneum , and Rhizopus oryzae ) and eight species of Candida as yeast specimens. Compounds 9 and 10 showed very good activity when evaluated in yeast (MIC 0.112 and 0.163 μg/mL) compared to the reference compound, itraconazole (MIC 0.067 μg/mL). The best antifungal activity in filamentous strains was shown by compound 9 . Hence compounds 9 and 10 represent new leads for further pharmacomodulation in this series.
