Molecular hybridization approach for phenothiazine incorporated 1,2,3-triazole hybrids as promising antimicrobial agents: Design, synthesis, molecular docking and in silico ADME studies

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications

“…Furthermore, the strong dipole properties of the triazole unit increased its importance in the field of medicinal chemistry, as it binds to the biological target with high affinity. Phenothiazine conjugates 5 and 6 with a 1,2,3-triazole linker were developed and the conjugates screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain [57]. All the Phenothiazine conjugates 5 and 6 with a 1,2,3-triazole linker were developed and the conjugates screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain [57].…”

“…Phenothiazine conjugates 5 and 6 with a 1,2,3-triazole linker were developed and the conjugates screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain [57]. All the Phenothiazine conjugates 5 and 6 with a 1,2,3-triazole linker were developed and the conjugates screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain [57]. All the compounds exhibited relatively good in vitro anti-tubercular activity as demonstrated by the compound 5a bearing a 4-nitro group that showed significant anti-tubercular activity with a MIC value of 2.44 µM against M.tb H37Rv (Figure 8).…”

1,2,3-Triazole Nucleus as a Versatile Tool for the Obtainment of Novel Biologically Active Compounds: an Overview

“…As vantagens oferecidas por esta técnica englobam poder: (i) sintetizar compostos capazes de sobrepujar resistências Neste cenário, núcleos 1,2,3-triazólicos tornamse especialmente úteis como escolha para linkers devido a sua atuação como farmacóforos de diferentes atividades biológicas. [48][49][50][51][52] Dentro deste contexto, Campos e colaboradores hibridizaram a juglona (14) com a D-ribose e com a D-galactose, em suas formas protegidas, formando os híbridos 15a e 15b respectivamente (Esquema 1). 53 A proposta envolveu explorar a demanda energética super expressa das células tumorais, consequência dos processos de divisão celular desregulados, transformando os compostos híbridos 15a-b em "Cavalos de Tróia" para as células tumorais.…”

Anti-Tubercular Properties of 4-Amino-5-(4-Fluoro-3- Phenoxyphenyl)-4H-1,2,4-Triazole-3-Thiol and Its Schiff Bases: Computational Input and Molecular Dynamics

“…Based on the last 40 years of academic and pharmaceutical industry inventions, only bedaquiline was the first novel anti-TB drug permitted by the United States Food and Drug Administration (US FDA) authority in December 2012, for the treatment of MDR-TB, [6] while delamanid was the second anti-TB agent to be approved by the European Medicines Agency in late 2013 [7] and pretomanid was the third drug to be approved by the US FDA in August 2019 [8,9] (Figure 1). Triazole pharmacophore with various functional groups/substitutions has been reported for its promising anti-TB [10][11][12][13][14][15][16][17][18][19][20][21], antiviral [22], antibacterial [23,24], antifungal [25,26], antioxidant [27][28][29][30], and antiglycation properties [31]. In addition, it also serves as an opener of Ca( 2+ )-activated potassium (maxi-K) channels [32] and demonstrates molluscicidal [33], hypoglycemic [34], antihypertensive and blood platelet aggregation inhibition [35] activities.…”

“…Triazole pharmacophore with various functional groups/substitutions has been reported for its promising anti-TB [ 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 ], antiviral [ 22 ], antibacterial [ 23 , 24 ], antifungal [ 25 , 26 ], antioxidant [ 27 , 28 , 29 , 30 ], and antiglycation properties [ 31 ]. In addition, it also serves as an opener of Ca( 2+ )-activated potassium (maxi-K) channels [ 32 ] and demonstrates molluscicidal [ 33 ], hypoglycemic [ 34 ], antihypertensive and blood platelet aggregation inhibition [ 35 ] activities.…”