Synthesis and Bio-Evaluation of Novel Salicylic Acid-Oriented Thiourea Derivatives with Potential Applications in Agriculture

Li, Shaowei; Li, Huangyong; Cao, Xiufang; Chen, Changshui

doi:10.2174/15701808113109990045

Cited by 5 publications

(2 citation statements)

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“…Thiourea derivatives have been reported in the literature for their multiple biological activities, including antibacterial [1][2][3][4], antifungal [5,6], antitubercular [7][8][9], anthelmintic [10], antiviral [11,12], anticancer [4,13,14], analgesic [15][16][17], anti-inflammatory [1,18], anti-diabetic [19,20], anticonvulsant [21], antithyroid [22,23], antioxidant [24], insecticidal [25], herbicidal [26], and rodenticidal [27] effects. Thiourea derivatives are also versatile intermediates for the synthesis of heterocyclic compounds such as 1,3-thiazoles, pyrimidines, 1,2,4-triazines and 1,3-quinazolines [28].…”

Section: Introductionmentioning

confidence: 99%

New N-acyl Thiourea Derivatives: Synthesis, Standardized Quantification Method and In Vitro Evaluation of Potential Biological Activities

Roman

Pintilie

Cãproiu³

et al. 2023

Antibiotics

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New N-acyl thiourea derivatives with heterocyclic rings have been synthesized by first obtaining isothiocyanate, which further reacted with a heterocyclic amine, characterized by (FT-IR, NMR spectroscopy and FT-ICR) and tested for their in vitro antimicrobial, anti-biofilm and antioxidant activities to obtain a drug candidate in a lead-optimization process. From the tested compounds, those bearing benzothiazole (1b) and 6-methylpyridine (1d) moieties revealed anti-biofilm activity against E. coli ATCC 25922 at MBIC values of 625 µg/mL. Compound 1d exhibited the highest antioxidant capacity (~43%) in the in vitro assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Considering the in vitro results, the highest anti-biofilm and antioxidant activities were obtained for compound 1d. Therefore, a reversed-phase high-performance liquid chromatography (RP-HPLC) method has been optimized and validated for the quantitative determination of compound 1d. The detection and quantitation limits were 0.0174 μg/mL and 0.0521 μg/mL, respectively. The R2 correlation coefficient of the LOQ and linearity curves were greater than 0.99, over the concentration range of 0.05 μg/mL–40 μg/mL. The precision and accuracy of the analytical method were within 98–102%, confirming that the method is suitable for the quantitative determination of compound 1d in routine quality control analyses. Evaluating the results, the promising potential of the new N-acyl thiourea derivatives bearing 6-methylpyridine moiety will be further investigated for developing agents with anti-biofilm and antioxidant activities.

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Section: Introductionmentioning

confidence: 99%

New N-acyl Thiourea Derivatives: Synthesis, Standardized Quantification Method and In Vitro Evaluation of Potential Biological Activities

Roman

Pintilie

Cãproiu³

et al. 2023

Antibiotics

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“…Various synthetic analogs of SA have been developed and used for crop protection against microbial pathogens [ 18 ]. Currently SA-oriented thiourea derivatives are being developed as potential herbicidal as well as plant growth promoting compounds [ 19 ].…”

Section: Introductionmentioning

confidence: 99%

Hormone Signaling: Current Perspectives on the Roles of Salicylic Acid and Its Derivatives in Plants

Kumar

Haq

Chapagai

et al. 2015

The Formation, Structure and Activity of Phytochemicals

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Salicylic acid (SA) is an important plant hormone with a wide range of effects on plant growth and metabolism. Plants lacking SA exhibit enhanced susceptibility to pathogens. SA plays important signaling roles in resistance against biotrophic and hemi-biotrophic phytopathogens. It is synthesized in plastids along two pathways, one involving phenylalanine ammonia lyase (PAL) and the other isochorismate synthase (ICS). In Arabidopsis , during immune response most SA is synthesized through the ICS-dependent pathway, but clearly an ICS-independent pathway also exists. Several SA effector proteins have been identifi ed and characterized which mediate downstream SA signaling. This includes SABP, a catalase, SABP2, a methyl salicylate esterase, SABP3, a carbonic anhydrase, NPR1 (nonexpressor of pathogenesis-related 1), NPR3 (a NPR1 paralog), and NPR4 (another NPR1 paralog). NPR3 and NPR4 regulate the turnover of NPR1, a process which plays a key role in activating defense gene expression. The role of SA in abiotic stress signaling is gradually becoming clearer. Various components of SA signaling in biotic stress also appear to impact abiotic stress signaling.

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Antifungal activity of volatile organic compounds from Trichoderma virens

Inayati¹,

Sulistyowati²,

Aini³

et al. 2019

AIP Conference Proceedings

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Synthesis and Bio-Evaluation of Novel Salicylic Acid-Oriented Thiourea Derivatives with Potential Applications in Agriculture

Cited by 5 publications

References 0 publications

New N-acyl Thiourea Derivatives: Synthesis, Standardized Quantification Method and In Vitro Evaluation of Potential Biological Activities

New N-acyl Thiourea Derivatives: Synthesis, Standardized Quantification Method and In Vitro Evaluation of Potential Biological Activities

Hormone Signaling: Current Perspectives on the Roles of Salicylic Acid and Its Derivatives in Plants

Antifungal activity of volatile organic compounds from Trichoderma virens

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