1,2,4-Triazoles as Important Antibacterial Agents

Strzelecka, Małgorzata; Świątek, Piotr

doi:10.3390/ph14030224

Cited by 126 publications

(64 citation statements)

References 81 publications

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“…GC-MS analysis indicated that the chemical constituents of the most promising ME of E. desertorum snail had 3 major different peaks compared to H. aspersa; which are 3H-1,2,4-triazole-3-thione,4,5-dihydro-4,5-diphenyl followed by phthalic acid, 7-bromoheptyl ethyl ester and methyl 1,2-benzisothiazole-3-acetate. Similarly, the rst compound showed a potent antibacterial activity 29 . The second component was reported to have several biological activities 30 .…”

Section: Discussionmentioning

confidence: 98%

Evaluation and comparison of antimicrobial efficacy of snail mucus of Egyptian Eremina desertorum and Helix aspersa with novel approach of their anti-inflammatory and wound healing potencies

El-Zawawy

Mona

2021

Preprint

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Snail mucus is composed of bioactive compounds thought to have different biological properties for the treatment of some skin problems. Although Helix aspersa mucus is used in several cosmetic products, a detailed characterization of Eremina desertorum mucus composition and its biological activities is still missing. Mucus extracts (MEs) from H. aspersa and E. desertorum were prepared and tested for their antimicrobial, anti-inflammatory activities with their potencies in wound healing. Also, chemical characterization is done by GC-MS analysis. Results showed that ME of E. desertorum gave higher inhibitory activity against resistant strains related to burn wound infections compared to ME of H. aspersa. Also, it revealed a significant anti-inflammatory activity. Moreover, we found that ME of E. desertorum lacked cytotoxicity and was able to significantly induce cell proliferation and migration through up-regulation expression of TGFβ1 and VEGF genes. Our results suggested that MEs of E. desertorum have higher biological effects compared to H. aspersa, which are attributable to antimicrobial, anti-inflammatory activities, cell proliferation and pave the way for further investigating its potential effect as a human therapeutic agent.

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Section: Discussionmentioning

confidence: 98%

Evaluation and comparison of antimicrobial efficacy of snail mucus of Egyptian Eremina desertorum and Helix aspersa with novel approach of their anti-inflammatory and wound healing potencies

El-Zawawy

Mona

2021

Preprint

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show abstract

“…GC–MS analysis indicated that the chemical constituents of the most promising ME of E. desertorum snail had 3 major different peaks compared to H. aspersa ; which are 3H-1,2,4-triazole-3-thione,4,5-dihydro-4,5-diphenyl followed by phthalic acid, 7-bromoheptyl ethyl ester and methyl 1,2-benzisothiazole-3-acetate. Similarly, the first compound showed a potent antibacterial activity 29 . The second component was reported to have several biological activities 30 .…”

Section: Discussionmentioning

confidence: 99%

Antimicrobial efficacy of Egyptian Eremina desertorum and Helix aspersa snail mucus with a novel approach to their anti-inflammatory and wound healing potencies

El-Zawawy

Mona

2021

Sci Rep

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Snail mucus is composed of bioactive compounds thought to have different biological properties for the treatment of some skin problems. Although Helix aspersa mucus is used in several cosmetic products, a detailed characterization of Eremina desertorum mucus composition and its biological activities is still missing. Mucus extracts (MEs) from H. aspersa and E. desertorum were prepared and tested for their antimicrobial and anti-inflammatory activities with their potencies in wound healing. Also, chemical characterization was performed by GC–MS analysis. Results showed that ME of E. desertorum gave higher inhibitory activity against resistant strains related to burn wound infections compared to ME of H. aspersa. Additionally, it revealed a significant anti-inflammatory activity. Moreover, we found that ME of E. desertorum lacked cytotoxicity and was able to significantly induce cell proliferation and migration through up-regulation of TGF-β1 and VEGF gene expression. Our results suggested that MEs of E. desertorum have higher biological effects than H. aspersa, which are attributable to antimicrobial, anti-inflammatory activities, cell proliferation and pave the way for further investigating its potential effect as a human therapeutic agent.

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“…The second-generation 4-substituted proline analogues were designed using the 1,2,3-triazole substituent at Cγ of the P2 proline residue. The triazole moiety is found in diverse bioactive compounds that act as potential new drugs to treat bacterial, fungal, viral and malarial infections [32][33][34][35][36][37][38][39][40]. Triazoles were synthesized by azide-alkyne cycloaddition click chemistry using ruthenium-and copper-based catalysts allowing regioselective 1,5-and 1,4-substitutions of various functional groups.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and biological evaluation of P2-modified proline analogues targeting the HtrA serine protease in Chlamydia

Hwang

Strange

Mazraani

et al. 2022

European Journal of Medicinal Chemistry

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High temperature requirement A (HtrA) serine proteases have emerged as a novel class of antibacterial target, which are crucial in protein quality control and are involved in the pathogenesis of a wide array of bacterial infections. Previously, we demonstrated that HtrA in Chlamydia is essential for bacterial survival, replication and virulence. Here, we report a new series of proline (P2)-modified inhibitors of Chlamydia trachomatis HtrA (CtHtrA) developed by proline ring expansion and Cγ-substitutions. The structure-based drug optimization process was guided by molecular modelling and in vitro pharmacological evaluation of inhibitory potency, selectivity and cytotoxicity. Compound 25 from the first-generation 4-substituted proline analogues increased antiCtHtrA potency and selectivity over human neutrophil elastase (HNE) by approximately 6-and 12-fold, respectively, relative to the peptidic lead compound 1. Based on this compound, second-generation substituted proline residues containing 1,2,3triazole moieties were synthesized by regioselective azide-alkyne click chemistry. Compound 49 demonstrated significantly improved antichlamydial activity in whole cell assays, diminishing the bacterial infectious progeny below the detection limit at the lowest dose tested. Compound 49 resulted in approximately 9-and 22-fold improvement in the inhibitory potency and selectivity relative to 1, respectively. To date, compound 49 is the most potent HtrA inhibitor developed against Chlamydia spp. a Relative inhibition against CtHtrA is the ratio of IC50 CtHtrA(1) to IC50 CtHtrA (compound).b Relative inhibition against HNE is the ratio of IC50 HNE (1) to IC50 HNE (compound).

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1,2,4-Triazoles as Important Antibacterial Agents

Cited by 126 publications

References 81 publications

Evaluation and comparison of antimicrobial efficacy of snail mucus of Egyptian Eremina desertorum and Helix aspersa with novel approach of their anti-inflammatory and wound healing potencies

Evaluation and comparison of antimicrobial efficacy of snail mucus of Egyptian Eremina desertorum and Helix aspersa with novel approach of their anti-inflammatory and wound healing potencies

Antimicrobial efficacy of Egyptian Eremina desertorum and Helix aspersa snail mucus with a novel approach to their anti-inflammatory and wound healing potencies

Design, synthesis and biological evaluation of P2-modified proline analogues targeting the HtrA serine protease in Chlamydia

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