Synthesis and Biological Evaluation of 3-Biphenyl-4-yl-4-phenyl-4<i>H</i>-1,2,4-triazoles as Novel Glycine Transporter 1 Inhibitors

Sugane, Takashi; Tobe, Takahiko; Hamaguchi, Wataru; Shimada, Ichio; Maeno, Kyoichi; Miyata, Junji; Suzuki, Takeshi; Kimizuka, Tetsuya; Kohara, Atsuyuki; Morita, Tomoyo; Doihara, Hitoshi; Saita, Kyouko; Aota, Masaki; Furutani, Masako; Shimada, Yoshiaki; Hamada, Naoko; Sakamoto, Shuichi; Tsukamoto, Shin‐ichi

doi:10.1021/jm101031u

Cited by 42 publications

(16 citation statements)

References 18 publications

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“…Aryltriazole 30 showed very potent binding affinity (Ki = 0.0027 μmol/L) to CRF1 receptors with an IC50 of 0.049 μmol/L (Lowe et al, 2005). Several findings suggest that medications aimed at inhibiting the activity of glycine transporter 1 (GlyT1) may be useful as therapeutic agents for schizophrenia, dementia, and related disorders (Sugane et al, 2011). A series of 3biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles were evaluated as novel GlyT1 inhibitors and found that fluorophenylsubstituted triazole derivative 31 was the most potent one, which had improved GlyT1 inhibitory activity and selectivity against GlyT2.…”

Section: Anti-neuropathic Activity Of Triazole Derivativesmentioning

confidence: 99%

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Asif¹

2019

Preprint

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Various heterocyclic compounds along their derivatives were evaluated for their biological activities as antiviral, antitumor, anticonvulsant, antibacterial, antifungal, antituberculosis, analgesic, anti-inflammatory, antidiabetic, antihistamine and other biological activities. The triazole moiety seems to be very small, but in the biological profile has attracted the attention of many researchers to explore this skeleton to its multiple potential against several activities. The triazole derivatives possess a great importance in medicinal chemistry and can be used for the synthesis of numerous heterocyclic compounds with different biological activities. This review article covers the information of triazoles derivatives having different psychopharmacological actions. Thus triazole acts as a promising medicinal agent for the scientists working over this field. This review can be helpful to develop various more new compounds possessing triazoles moiety that could be better in terms of efficacy and lesser toxicity.

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Section: Anti-neuropathic Activity Of Triazole Derivativesmentioning

confidence: 99%

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Asif¹

2019

Preprint

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“…An HTS hit (Figure 11.9, A) from a GlyT1 screen was found to be a low micromolar inhibitor of GlyT1 but displayed no selectivity over the closely related GlyT2 [51]. It was noted that increasing the steric bulk at either the 3-or 4-position on the triazole ring increased the selectivity for GlyT1.…”

Section: Glycine Transporter 1 (Glyt1) Inhibitorsmentioning

confidence: 99%

Conformational Restriction and Steric Hindrance in Medicinal Chemistry

Wipf

Skoda

Mann

2015

The Practice of Medicinal Chemistry

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“…Oxadiazoles, including 1,2,4-oxadiazoles and 1,3,4-oxadiazoles which possess various bioactivities like antibacterial, antifungal and antitumor potencies [178], have relatively high reactivity due to the inductive effect of oxygen atom in the oxadiazole ring, and they have been investigated very well to transform into more stable heterocycles, especially 1,2,4-triazole derivatives [179][180][181][182][183][184][185][186][187]. In recent years, the prepared triazoles via rearrangement of oxadiazoles usually exhibited wide applications in medicinal chemistry especially as antitubercular [188] and antiproliferative agents [189], and also in supramolecular chemistry as progesterone receptors and ligands of coordination polymers [64,190,191].…”

Section: Transformations Of Five-membered Heterocyclic Compoundsmentioning

confidence: 99%

Current Developments in the Syntheses of 1,2,4-Triazole Compounds

Zhang¹,

Damu²,

Cai³

et al. 2014

COC

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Heterocyclic 1,2,4-triazole derivatives possess unusually spacious potentiality as medicinal agents, agricultural chemicals, functional materials, ionic liquids, supramolecular catalysts as well as artificial enzymes and receptors for supramolecular recognition and biomimetic catalysis, and their various researches and developments have been being a quite rapidly developing and active highlight topic with an infinite space. Numerous efforts have been directed toward various types of possible applications of 1,2,4-triazole-based compounds and a lot of important progress has been made, especially their preparations have attracted increasing attention. This review systematically summarized the recent advances in the syntheses of 1,2,4-triazole derivatives, including: (1) Cyclizations to form triazole ring; (2) Transformations of heterocyclic compounds to construct triazole ring; (3) Substitutions on 1,2,4-triazole ring; (4) Structural modifications in side chains of 1,2,4-triazole ring. It was hoped that this review would be helpful for the design and development of highly efficient preparation of 1,2,4-triazole derivatives with various sorts and varieties of extensively potential applications in medicine, agriculture, chemistry, materials, supramolecular sciences and so on.

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Synthesis and Biological Evaluation of 3-Biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as Novel Glycine Transporter 1 Inhibitors

Cited by 42 publications

References 18 publications

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Anti-neuropathic and anticonvulsant activities of various substituted triazoles analogues

Conformational Restriction and Steric Hindrance in Medicinal Chemistry

Current Developments in the Syntheses of 1,2,4-Triazole Compounds

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