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Article ; Online: 2-Benzyl-7-(4-chlorophenyl)-3-morpholino-6-((1-phenyl-1 H -1,2,3-triazol-4-yl)methyl)-6,7-dihydro-5 H -pyrrolo[3,4- b ]pyridin-5-one

Perla Islas-Jácome / Cecilia García-Falcón / Sandra L. Castañón-Alonso / Ernesto Calderón-Jaimes / Daniel Canseco-González / Alejandro Islas-Jácome / Eduardo González-Zamora

Molbank, Vol 2023, Iss M1693, p M

2023 Volume 1693

Abstract: The new polyheterocyclic compound, 2-benzyl-7-(4-chlorophenyl)-3-morpholino-6-((1-phenyl-1 H -1,2,3-triazol-4-yl)methyl)-6,7-dihydro-5 H -pyrrolo[3,4- b ]pyridin-5-one, was synthesized by a sequential combination of 4-chlorobenzaldehyde, (1-phenyl-1 H -1, ...

Abstract	The new polyheterocyclic compound, 2-benzyl-7-(4-chlorophenyl)-3-morpholino-6-((1-phenyl-1 H -1,2,3-triazol-4-yl)methyl)-6,7-dihydro-5 H -pyrrolo[3,4- b ]pyridin-5-one, was synthesized by a sequential combination of 4-chlorobenzaldehyde, (1-phenyl-1 H -1,2,3-triazol-4-yl)methanamine, 2-isocyano-1-morpholino-3-phenylpropan-1-one, and maleic anhydride under a microwave-assisted one-pot process [Ugi-Zhu/aza Diels-Alder cycloaddition/ N -acylation/decarboxylation/dehydration] with a 28% overall yield. The synthesized compound was fully characterized by 1D ( 1 H, 13 C) and 2D (COSY, HSQC, and HMBC) NMR, FT-IR, and HRMS.
Keywords	multicomponent reactions (MCRs) ; Ugi-Zhu reaction (UZ-3CR) ; polyheterocycles ; pyrrolo[3,4- b ]pyridin-5-ones ; 1 H -1,2,3-triazoles ; Inorganic chemistry ; QD146-197
Language	English
Publishing date	2023-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of New bis -furanyl-pyrrolo[3,4- b ]pyridin-5-ones via the Ugi-Zhu Reaction and Docking Studies on the Main Protease (M Pro ) from SARS-CoV-2

Ivette Morales-Salazar / Sandra L. Castañón-Alonso / Daniel Canseco-González / Erik Díaz-Cervantes / Eduardo González-Zamora / Alejandro Islas-Jácome

Chemistry Proceedings, Vol 8, Iss 84, p

2021 Volume 84

Abstract: The synthesis of five new bis -furanyl-pyrrolo[3,4- b ]pyridin-5-ones in 30 to 40% yields through a domino sequence based on the Ugi-Zhu three-component reaction is described. Then, on the main protease M Pro (PDB: 6lu7) from the SARS-CoV-2, the ... ...

Abstract	The synthesis of five new bis -furanyl-pyrrolo[3,4- b ]pyridin-5-ones in 30 to 40% yields through a domino sequence based on the Ugi-Zhu three-component reaction is described. Then, on the main protease M Pro (PDB: 6lu7) from the SARS-CoV-2, the synthesized products and co-crystallized ligands of M Pro were in silico evaluated using the docking technique, finding moderate to good binding energies and some interesting interactions, demonstrating that the ligand 8c can be considered as a drug candidate against the SARS-CoV-2-M Pro due to its LE value (−5.96 kcal/mol), which is better than other synthesized and reported molecules in the literature. At the same time, hydrophobic interactions play a crucial role in the ligand target molecular couplings, demonstrated through a hydrophobicity surfaces analysis. Finally, 8a and 8b can also be considered as drug candidates. Thus, some synthesized bis -furanyl-pyrrolo[3,4- b ]pyridin-5-ones may be used for further in vitro assays against the virus.
Keywords	Ugi-Zhu reaction ; polyheterocycles ; docking ; COVID-19 ; SARS-CoV-2 ; main protease M Pro ; Chemistry ; QD1-999
Subject code	333
Language	English
Publishing date	2021-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of a Symmetrical tris -Tetrazole as Isostere of a Tricarboxylic Acid

Julio C. Flores-Reyes / Perla Islas-Jácome / Atilano Gutiérrez-Carrillo / Mónica A. Rincón-Guevara / Galdina V. Suárez-Moreno / Óscar Vázquez-Vera / Leticia Lomas-Romero / Eduardo González-Zamora / Alejandro Islas-Jácome

Chemistry Proceedings, Vol 8, Iss 25, p

Behind New Tridentate Ligands for MOFs

2021 Volume 25

Abstract: The synthesis and characterization of three tridentate ligands for new MOFs are described. A triple aminolysis of the 1,3,5-tribenzoyl chloride with p -aminobenzoic acid gave the tricarboxylic acid 3 in 90% yield. Moreover, the same reaction, also from ... ...

Abstract	The synthesis and characterization of three tridentate ligands for new MOFs are described. A triple aminolysis of the 1,3,5-tribenzoyl chloride with p -aminobenzoic acid gave the tricarboxylic acid 3 in 90% yield. Moreover, the same reaction, also from the 1,3,5-tribenzoyl chloride, but using p -aminobenzonitrile gave the new tris -benzonitrile 5 in 85% yield. Finally, this later one was treated with sodium azide and a Lewis acid to synthesize the new tris -tetrazole-based ligand 7 in 72% yield through a [3 + 2] azide-nitrile cycloaddition. It is noteworthy that the isosterism between carboxylic acids and tetrazoles may be considered to design and fabricate new MOFs with similar properties.
Keywords	metal-organic frameworks (MOFs) ; tridentate ligands ; tricarboxylic acids ; tris -benzonitriles ; tris -tetrazoles ; aminolysis ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2021-11-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of Tris-Heterocycles via a Cascade IMCR/Aza Diels-Alder + CuAAC Strategy

Manuel A. Rentería-Gómez / Alejandro Islas-Jácome / Shrikant G. Pharande / David A. Vosburg / Rocío Gámez-Montaño

Frontiers in Chemistry, Vol

2019 Volume 7

Abstract: 6-Triazolylmethyl-pyrrolo[3,4-b]pyridin-5-one tris-heterocycles were synthesized in 43–57% overall yields. The two-stage synthesis involved a cascade process (Ugi-3CR/aza Diels-Alder/N-acylation/aromatization) followed by a copper-assisted alkyne-azide [ ... ...

Abstract	6-Triazolylmethyl-pyrrolo[3,4-b]pyridin-5-one tris-heterocycles were synthesized in 43–57% overall yields. The two-stage synthesis involved a cascade process (Ugi-3CR/aza Diels-Alder/N-acylation/aromatization) followed by a copper-assisted alkyne-azide [3+2] cycloaddition (CuAAC). This efficient and convergent strategy proceeded via complex terminal alkynes functionalized with a fused bis-heterocycle at the α-position. The final products are ideal candidates for SAR studies as they possess two privileged scaffolds in medicinal chemistry: 4-substituted or 1,4-substituted 1H-1,2,3-triazoles and pyrrolo[3,4-b]pyridin-5-ones.
Keywords	nitrogen tris-heterocycles ; cascade IMCR process ; CuAAC ; Ugi-3CR ; aza Diels-Alder ; Chemistry ; QD1-999
Language	English
Publishing date	2019-08-01T00:00:00Z
Publisher	Frontiers Media S.A.
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Search for Non-Protein Protease Inhibitors Constituted with an Indole and Acetylene Core

Marco A. Almaraz-Girón / Ernesto Calderón-Jaimes / Adrián Sánchez Carrillo / Erik Díaz-Cervantes / Edith Castañón Alonso / Alejandro Islas-Jácome / Armando Domínguez-Ortiz / Sandra L. Castañón-Alonso

Molecules, Vol 26, Iss 3817, p

2021 Volume 3817

Abstract: A possible inhibitor of proteases, which contains an indole core and an aromatic polar acetylene, was designed and synthesized. This indole derivative has a molecular architecture kindred to biologically relevant species and was obtained through five ... ...

Abstract	A possible inhibitor of proteases, which contains an indole core and an aromatic polar acetylene, was designed and synthesized. This indole derivative has a molecular architecture kindred to biologically relevant species and was obtained through five synthetic steps with an overall yield of 37% from the 2,2′-(phenylazanediyl)di(ethan-1-ol). The indole derivative was evaluated through docking assays using the main protease (SARS-CoV-2-M pro ) as a molecular target, which plays a key role in the replication process of this virus. Additionally, the indole derivative was evaluated as an inhibitor of the enzyme kallikrein 5 (KLK5), which is a serine protease that can be considered as an anticancer drug target.
Keywords	synthesis ; indole derivatives ; inhibitor of proteases ; studies in silico ; docking studies ; SARS-CoV-2-M pro ; Organic chemistry ; QD241-441
Language	English
Publishing date	2021-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: A One-Pot Six-Component Reaction for the Synthesis of 1,5-Disubstituted Tetrazol-1,2,3-Triazole Hybrids and Their Cytotoxic Activity against the MCF-7 Cell Line

Cesia M. Aguilar-Morales / Jorge Gustavo Araujo-Huitrado / Yamilé López-Hernández / Claudia Contreras-Celedón / Alejandro Islas-Jácome / Angelica Judith Granados-López / Cesar R. Solorio-Alvarado / Jesús Adrián López / Luis Chacón-García / Carlos J. Cortés-García

Molecules, Vol 26, Iss 6104, p

2021 Volume 6104

Abstract: A high-order multicomponent reaction involving a six-component reaction to obtain the novel linked 1,5-disubstituted tetrazole-1,2,3-triazole hybrids in low to moderate yield is described. This one-pot reaction is carried out under a cascade process ... ...

Abstract	A high-order multicomponent reaction involving a six-component reaction to obtain the novel linked 1,5-disubstituted tetrazole-1,2,3-triazole hybrids in low to moderate yield is described. This one-pot reaction is carried out under a cascade process consisting of three sequential reactions: Ugi-azide, bimolecular nucleophilic substitution (S N 2), and copper-catalyzed alkyne–azide reaction (CuAAC), with high atom and step-economy due the formation of six new bonds (one C-C, four C-N, and one N-N). Thus, the protocol developed offers operational simplicity, mild reaction conditions, and structural diversity. Finally, to evaluate the antitumoral potential of the synthetized molecules, a proliferation study was performed in the breast cancer (BC) derived cell line MCF-7. The hybrid compounds showed several degrees of cell proliferation inhibition with a remarkable effect in those compounds with cyclohexane and halogens in their structures. These compounds represent potential drug candidates for breast cancer treatment. However, additionally assays are needed to elucidate their complete effect over the cellular hallmarks of cancer.
Keywords	Ugi-azide ; high-order multicomponent reaction ; 1,5-disubstituted tetrazole ; 1,4-disubstituted-1,2,3-triazoles ; hybrid compounds ; cytotoxic activity ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2021-10-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: Synthesis of imidazo[1,2-a]pyridin-chromones by a MW assisted Groebke–Blackburn–Bienaymé process

Kishore, Kranthi G / Alejandro Islas-Jácome / Rocío Gámez-Montaño / Unnamatla M.V. Basavanag

Tetrahedron letters. 2015 Jan. 01, v. 56, no. 1

2015

Abstract: A series of nine novel imidazo[1,2-a]pyridin-chromones and nine novel imidazo[1,2-a]pyridin-6-fluorochromones were synthesized in good to excellent yields by a MW assisted Groebke–Blackburn–Bienaymé reaction (GBB) under mild thermal and acidic conditions. ...

Abstract	A series of nine novel imidazo[1,2-a]pyridin-chromones and nine novel imidazo[1,2-a]pyridin-6-fluorochromones were synthesized in good to excellent yields by a MW assisted Groebke–Blackburn–Bienaymé reaction (GBB) under mild thermal and acidic conditions. Additionally, optimized geometries for the two non-prepared 5-bromoimidazo[1,2-a]pyridin-chromones were calculated at the TPSSh/6-311G(d) level of theory in order to understand the role of the steric strain in the GBB process.
Keywords	chemical reactions ; chemical structure ; geometry ; organic compounds
Language	English
Dates of publication	2015-0101
Size	p. 155-158.
Publishing place	Elsevier Ltd
Document type	Article
ZDB-ID	204287-3
ISSN	1873-3581 ; 0040-4039
ISSN (online)	1873-3581
ISSN	0040-4039
DOI	10.1016/j.tetlet.2014.11.047
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Synthesis of Pyrrolo[3,4- b ]pyridin-5-ones via Multicomponent Reactions and In Vitro–In Silico Studies Against SiHa, HeLa, and CaSki Human Cervical Carcinoma Cell Lines

Daniel Segura-Olvera / Ailyn N. García-González / Ivette Morales-Salazar / Alejandro Islas-Jácome / Yareli Rojas-Aguirre / Ilich A. Ibarra / Erik Díaz-Cervantes / Sofía Lizeth Alcaraz-Estrada / Eduardo González-Zamora

Molecules, Vol 24, Iss 14, p

2019 Volume 2648

Abstract: A series of 12 polysubstituted pyrrolo[3,4- b ]pyridin-5-ones were synthesized via a one-pot cascade process (Ugi−3CR/ aza Diels-Alder/ N -acylation/decarboxylation/dehydration) and studied in vitro using human epithelial cervical carcinoma SiHa, HeLa, ... ...

Abstract	A series of 12 polysubstituted pyrrolo[3,4- b ]pyridin-5-ones were synthesized via a one-pot cascade process (Ugi−3CR/ aza Diels-Alder/ N -acylation/decarboxylation/dehydration) and studied in vitro using human epithelial cervical carcinoma SiHa, HeLa, and CaSki cell line cultures. Three compounds of the series exhibited significative cytotoxicity against the three cell lines, with HeLa being the most sensitive one. Then, based on these results, in silico studies by docking techniques were performed using Paclitaxel as a reference and αβ-tubulin as the selected biological target. Worth highlighting is that strong hydrophobic interactions were observed between the three active molecules and the reference drug Paclitaxel, to the αβ-tubulin. In consequence, it was determined that hydrophobic−aromatic moieties of bioactive compounds and Paclitaxel play a key role in making stronger interactions to the ligand−target complex. A quantitative structure activity relationship (QSAR) study revealed that the six membered rings are the most significant molecular frameworks, being present in all proposed models for the in vitro-studied cell lines. Finally, also from the docking interpretation, a ligand-based pharmacophore model is proposed in order to find further potential polyheterocyclic candidates to bind stronger to the αβ-tubulin.
Keywords	pyrrolo[3,4- b ]pyridin-5-ones ; paclitaxel ; αβ-tubulin ; cervical cancer ; SiHa ; HeLa ; Caski ; molecular docking ; QSAR ; pharmacophore model ; Organic chemistry ; QD241-441
Subject code	540 ; 500
Language	English
Publishing date	2019-07-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Synthesis of New bis 1- and 5-Substituted 1 H -Tetrazoles via Huisgen-Type 1,3-Dipolar Cycloadditions

Roberto E. Blanco-Carapia / Julio C. Flores-Reyes / Yizrell Medina-Martínez / Perla Islas-Jácome / Diego Pérez-Martínez / Leticia Lomas-Romero / Ilich A. Ibarra / Alejandro Islas-Jácome / Eduardo González-Zamora

Proceedings, Vol 9, Iss 1, p

2019 Volume 32

Abstract: The synthesis and characterization of one symmetrical bis -1-substituted-1 H -tetrazole (69%) via a Huisgen-type 1,3-dipolar cycloaddition, as well as, one symmetrical aza -linked bis -5-substituted-1 H -tetrazole (57%) via a classic Huisgen 1,3-dipolar ... ...

Abstract	The synthesis and characterization of one symmetrical bis -1-substituted-1 H -tetrazole (69%) via a Huisgen-type 1,3-dipolar cycloaddition, as well as, one symmetrical aza -linked bis -5-substituted-1 H -tetrazole (57%) via a classic Huisgen 1,3-dipolar cycloaddition followed by a reductive aza -coupling under greener reaction conditions are described. The main reason behind these tetrazole-based ligands is to construct novel Metal-Organic Framework (MOF) architectures to evaluate their CO 2 capture properties under relative humidity conditions. It is worthy to note that both herein reported products have not been synthesized nor isolated, anywhere. Besides, the synthesis of new ligands to fabricate novel MOFs with potential application in environmental remediation has become a highly valued field of opportunity for synthetic chemists and materials engineers.
Keywords	Symmetrical bis-tetrazole-based ligands ; Huisgen 1,3-dipolar cycloadditions ; MOFs chemistry ; CO2 capture properties ; General Works ; A
Subject code	540
Language	English
Publishing date	2019-04-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
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Article ; Online: Quadratic Non-Linear Optical Properties of the poly(2,5- bis (but-2-ynyloxy) Benzoate Containing the 2-(ethyl(4-((4-nitrophenyl)buta-1,3-diynyl)phenyl)amino)ethanol) Chromophore

Sandra L. Castañón-Alonso / Omar G. Morales-Saavedra / Marco A. Almaraz-Girón / Sandro Báez-Pimiento / Alejandro Islas-Jácome / L. M. Rocha-Ramírez / Armando Domínguez-Ortiz / Marcos Esparza-Schulz / Adolfo Romero-Galarza / María E. Hernández-Rojas

Polymers, Vol 12, Iss 1, p

2020 Volume 241

Abstract: Excellent quadratic non-linear optical (ONL-2) properties of the poly(2,5- bis (but-2-ynyloxy) benzoate, containing a polar diacetylene as a chromophore, were found. According with the Maker fringes method, oriented polymer films showing an order ... ...

Abstract	Excellent quadratic non-linear optical (ONL-2) properties of the poly(2,5- bis (but-2-ynyloxy) benzoate, containing a polar diacetylene as a chromophore, were found. According with the Maker fringes method, oriented polymer films showing an order parameter of ∼0.23 can display outstanding and stable Second Harmonic Generation (SHG) effects under off-resonant conditions (SHG-532 nm). Also, the macroscopic non-linear optical (NLO)-coefficients were evaluated under the rod-like molecular approximation, obtaining: χ zzz (2) and χ zxx (2) in the order of 280 ± 10 and 100 ± 10 pm V −1 , respectively. The mechanical and chemical properties, in addition to the large ONL-2 coefficients exhibited by this polymer, make it a promising organic material in the development of optoelectronic/photonic devices.
Keywords	diacetylenes ; push-pull polymers ; non-linear optics ; optical materials ; organic films ; Organic chemistry ; QD241-441
Subject code	535
Language	English
Publishing date	2020-01-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
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