Category: 59032-27-8

Ma, Chunlin published the artcileSyntheses, characterizations and crystal structures of new triorgano-tin or -germanium complexes with 1H-5-mercapto-1,2,3-triazolato, Category: triazoles, the publication is Polyhedron (2004), 23(11), 1981-1986, database is CAplus.

Triorganotin and triorganogermanium(IV) complexes with 1H-5-mercapto-1,2,3-triazolato, R₃MSC₂H₂N₃ [M = Sn, R = CH₃, (1); C₂H₅, (2); Bu, (3); C₆H₅, (4); M = Ge, R = CH₃, (5); C₂H₅, (6); Bu, (7); C₆H₅, (8)], were synthesized. All the complexes 1–8 were characterized by elemental, IR and ¹H NMR analyses. Among them complexes 4 and 8 also were characterized by x-ray crystallog. diffraction analyses, which revealed that the Sn and Ge atom environments are distorted tetrahedral coordination polyhedrons, coordinated to three Ph groups and to one S atom of the ligand. The packing of complexes 4 and 8 is stabilized into a 1-dimensional infinite chain by intermol. N-H···N H bonds.

Polyhedron published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Category: triazoles.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Wu, Fanhong published the artcileSynthesis of anhydrous sodium salt of 5-mercapto-1,2,3-triazole, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate, the publication is Zhongguo Yiyao Gongye Zazhi (2001), 32(2), 81-82, database is CAplus.

Sodium 1,2,3-triazole-3-sulfide was prepared by trans-acylating di-Et carbonate with hydrazine hydrate to obtain Et hydrazinoformate, condensing with chloroacetaldehyde to obtain Et 2-chloroethylenehydrazinoformate, cyclizing with SOCl₂ in dichloromethane in the presence of pyridine to obtain 5-chloro-1,2,3-thiadiazole, substituting with NH₃ in DMF, and rearranging in the presence of NaOH.

Zhongguo Yiyao Gongye Zazhi published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C23H28N2O4, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Dharuman, Suresh published the artcileSynthesis and Structure-Activity Relationship of Thioacetamide-Triazoles against Escherichia coli, Application In Synthesis of 59032-27-8, the publication is Molecules (2022), 27(5), 1518, database is CAplus and MEDLINE.

Infections due to Gram-neg. bacteria are increasingly dangerous due to the spread of multi-drug resistant strains, emphasizing the urgent need for new antibiotics with alternative modes of action. Authors have previously identified a novel class of antibacterial agents, thioacetamide-triazoles, using an antifolate targeted screen and determined their mode of action which is dependent on activation by cysteine synthase A. Herein, authors report a detailed examination of the anti-E. coli structure-activity relationship of the thioacetamide-triazoles. Analogs of the initial hit compounds were synthesized to study the contribution of the aryl, thioacetamide, and triazole sections. A clear structure-activity relationship was observed generating compounds with excellent inhibition values. Substitutions to the aryl ring were generally best tolerated, including the introduction of thiazole and pyridine heteroaryl systems. Substitutions to the central thioacetamide linker section were more nuanced; the introduction of a Me branch to the thioacetamide linker substantially decreased antibacterial activity, but the isomeric propionamide and N-benzamide systems retained activity. Changes to the triazole portion of the mol. dramatically decreased the antibacterial activity, further indicating that 1,2,3-triazole is critical for potency. From these studies, authors have identified new lead compounds with desirable in-vitro ADME properties and in-vivo pharmacokinetic properties.

Molecules published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application In Synthesis of 59032-27-8.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Dharuman, Suresh published the artcileSynthesis and Structure-Activity Relationship of Thioacetamide-Triazoles against Escherichia coli, Application In Synthesis of 59032-27-8, the publication is Molecules (2022), 27(5), 1518, database is CAplus and MEDLINE.

Infections due to Gram-neg. bacteria are increasingly dangerous due to the spread of multi-drug resistant strains, emphasizing the urgent need for new antibiotics with alternative modes of action. Authors have previously identified a novel class of antibacterial agents, thioacetamide-triazoles, using an antifolate targeted screen and determined their mode of action which is dependent on activation by cysteine synthase A. Herein, authors report a detailed examination of the anti-E. coli structure-activity relationship of the thioacetamide-triazoles. Analogs of the initial hit compounds were synthesized to study the contribution of the aryl, thioacetamide, and triazole sections. A clear structure-activity relationship was observed generating compounds with excellent inhibition values. Substitutions to the aryl ring were generally best tolerated, including the introduction of thiazole and pyridine heteroaryl systems. Substitutions to the central thioacetamide linker section were more nuanced; the introduction of a Me branch to the thioacetamide linker substantially decreased antibacterial activity, but the isomeric propionamide and N-benzamide systems retained activity. Changes to the triazole portion of the mol. dramatically decreased the antibacterial activity, further indicating that 1,2,3-triazole is critical for potency. From these studies, authors have identified new lead compounds with desirable in-vitro ADME properties and in-vivo pharmacokinetic properties.

Molecules published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application In Synthesis of 59032-27-8.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Monn, James A. published the artcileSynthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu₂ Receptor Agonist, Application of Sodium 1,2,3-triazole-5-thiolate, the publication is Journal of Medicinal Chemistry (2015), 58(18), 7526-7548, database is CAplus and MEDLINE.

Identification of orthosteric mGlu_2/3 receptor agonists capable of discriminating between individual mGlu₂ and mGlu₃ subtypes has been highly challenging owing to the glutamate-site sequence homol. between these proteins. Herein we detail the preparation and characterization of a series of mols. related to (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY354740) bearing C4-thiotriazole substituents. On the basis of second messenger responses in cells expressing other recombinant human mGlu_2/3 subtypes, a number of high potency and efficacy mGlu₂ receptor agonists exhibiting low potency mGlu₃ partial agonist/antagonist activity were identified. From this, (1R,2S,4R,5R,6R)-2-amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY2812223, I) was further characterized. Cocrystn. of I with the amino terminal domains of hmGlu₂ and hmGlu₃ combined with site-directed mutation studies has clarified the underlying mol. basis of this unique pharmacol. Evaluation of I in a rat model responsive to mGlu₂ receptor activation coupled with a measure of central drug disposition provides evidence that this mol. engages and activates central mGlu₂ receptors in vivo.

Journal of Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application of Sodium 1,2,3-triazole-5-thiolate.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Shchepin, Roman published the artcileInfluence of heterocyclic and oxime-containing farnesol analogs on quorum sensing and pathogenicity in Candida albicans, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate, the publication is Bioorganic & Medicinal Chemistry (2008), 16(4), 1842-1848, database is CAplus and MEDLINE.

A series of synthetic mols. combining a geranyl backbone with a heterocyclic or oxime head group are quorum-sensing mols. that block the yeast to mycelium transition in the dimorphic fungus Candida albicans. A number of the analogs have an IC₅₀ ≤ 10 μM, a level of potency essentially identical to the natural quorum sensing signal, the sesquiterpene farnesol. Two of the most potent analogs, neither toxic toward healthy mice, display remarkably different effects when co-administered with C. albicans. While neither offers protection from candidiasis, one analog mimics farnesol in acting as a virulence factor, whereas the other has no effect. The results offer the first example of highly potent synthetic fungal quorum-sensing mols., and provide the first evidence for the ability to decouple quorum sensing and virulence.

Bioorganic & Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C13H16BFO3, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Yoshida, Y. published the artcileStudies on anti-Helicobacter pylori agents. Part 2: New cephem derivatives, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate, the publication is Bioorganic & Medicinal Chemistry (2000), 8(9), 2317-2335, database is CAplus and MEDLINE.

The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of cephem derivatives are described. Introduction of thio-heterocyclic groups containing N- and S-atoms to the 3-position and Ph or thienyl acetamido groups to the 7-position of the cephem nucleus dramatically improved the activity. From this series of derivatives, . 7β-(2-phenylacetamido)-3-(5-methyl-1,3,4-thiadiazol-2-yl)thio-3-cephem-4-carboxylic acid was found to have extremely potent in vitro anti-H. pylori activity, superior therapeutic efficacy compared to AMPC and CAM, no cross-resistance between CAM or MNZ and low potential for causing diarrhea due to instability to β-lactamase.

Bioorganic & Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C18H23OP, Recommanded Product: Sodium 1,2,3-triazole-5-thiolate.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Cioffi, Christopher L. published the artcileSynthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1, COA of Formula: C2H2N3NaS, the publication is Journal of Medicinal Chemistry (2016), 59(18), 8473-8494, database is CAplus and MEDLINE.

The authors previously disclosed the discovery of rationally designed N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1), represented by analogs 10 and 11. The authors describe herein further structure-activity relationship exploration of this series via an optimization strategy that primarily focused on the sulfonamide and benzamide appendages of the scaffold. These efforts led to the identification of advanced leads possessing a desirable balance of excellent in vitro GlyT-1 potency and selectivity, favorable ADME and in vitro pharmacol. profiles, and suitable pharmacokinetic and safety characteristics. Representative analog I exhibited robust in vivo activity in the cerebral spinal fluid glycine biomarker model in both rodents and nonhuman primates. Furthermore, rodent microdialysis experiments also demonstrated that oral administration of I significantly elevated extracellular glycine levels within the medial prefrontal cortex (mPFC).

Journal of Medicinal Chemistry published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, COA of Formula: C2H2N3NaS.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Kume, Masaharu published the artcileOrally active cephalosporins. II. Synthesis and structure-activity relationships of new 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]cephalosporins with 1,2,3-triazole in C-3 side chain, Application In Synthesis of 59032-27-8, the publication is Journal of Antibiotics (1993), 46(1), 177-92, database is CAplus and MEDLINE.

The synthesis, antibacterial activity and oral absorbability of the title compounds I (X = CH₂S(CH₂)_n, S(CH₂)_m, SCH₂S(CH₂)_x, CH₂SCH₂S, S(CH₂)₂S, S(CH₂)₂O, S(CH₂)₂NH; n, m = 1-3, x = 0-2) are described. Their oral absorbability was influenced by the spacer length between C-3 of a cephem nucleus and C-4′ of 1,2,3-triazole. The SCH₂S structure was also found to contribute to their good oral absorption. The quant. relationship between the bioavailability and the spacer length of cephalosporins is discussed.

Journal of Antibiotics published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Application In Synthesis of 59032-27-8.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics

Kume, Masaharu published the artcileOrally active cephalosporins. III. Synthesis and structure-activity relationships of new 3-heterocyclicthiomethylthio-7β-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-cephem-4-carboxylic acids, Related Products of triazoles, the publication is Journal of Antibiotics (1993), 46(2), 316-30, database is CAplus and MEDLINE.

Title compounds I (R = triazolyl, tetrazolyl, thiadiazolyl, 2-pyridyl) were synthesized. Their antibacterial activity and oral absorbability were much influenced by the structure of R. I (R = 1,2,3-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 5-methyl-1,3,4-thiadiazol-2-yl) exhibited potent antibacterial activity against both Gram-pos. and Gram-neg. bacteria, whereas I (R = 2-methyl-1,2,3-triazol-4-yl, 2-pyridyl) showed better oral absorption in mice than the other cephalosporins prepared

Journal of Antibiotics published new progress about 59032-27-8. 59032-27-8 belongs to triazoles, auxiliary class Triazoles, name is Sodium 1,2,3-triazole-5-thiolate, and the molecular formula is C2H2N3NaS, Related Products of triazoles.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics