Synthesis and Antimicrobial Activity of 1,2,4‐Triazoles

Roy, Ratna; Desai, A. R.; Desai, K. R.

doi:10.1155/2005/843803

Cited by 9 publications

(5 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In the case of the alkyl substituted 1,3,4-oxadiazole derivates ( 7a and 7e – g ), the benzimidazole carbohydrazide 3 was acylated with different acid chlorides followed by subsequent POCl 3 mediated cyclization of the bisacylhydrazide intermediates. The derivatives with inverse ether-, thio-ether-, or sulfone-spacer (7 b – d ), as well as the alkyl substituted 1,3,4-oxadiazoles 7h – k were accessible by direct treatment of 3 with different carboxylic acids in neat POCl 3 …”

Section: Resultsmentioning

confidence: 99%

“…The derivatives with inverse ether-, thio-ether-, or sulfone-spacer (7b−d), as well as the alkyl substituted 1,3,4-oxadiazoles 7h−k were accessible by direct treatment of 3 with different carboxylic acids in neat POCl 3 . 24 The 1,3,4-thiadiazoles (8a−d) were synthesized according to Scheme 1 by acylation of 3 with different acid chlorides followed by cyclization of the intermediates by means of Lawesson's reagent. 25 The compounds 8e and 8f−i were synthesized in a one-pot manner.…”

Section: ■ Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Structure–Activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold

et al. 2013

View full text Add to dashboard Cite

Glutaminyl cyclase (hQC) has emerged as a new potential target for the treatment of Alzheimer's disease (AD). The inhibition of hQC prevents of the formation of the Aβ3(pE)-40,42 species which were shown to be of elevated neurotoxicity and are likely to act as a seeding core, leading to an accelerated formation of Aβ-oligomers and fibrils. This work presents a new class of inhibitors of hQC, resulting from a pharmacophore-based screen. Hit molecules were identified, containing benzimidazole as the metal binding group connected to 1,3,4-oxadiazole as the central scaffold. The subsequent optimization resulted in benzimidazolyl-1,3,4-thiadiazoles and -1,2,3-triazoles with an inhibitory potency in the nanomolar range. Further investigation into the potential binding mode of the new compound classes combined molecular docking and site directed mutagenesis studies.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

Structure–Activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold

et al. 2013

View full text Add to dashboard Cite

show abstract

“…The substances containing a five member heterocyclic base are important targets in chemical synthesis because of their 2 pronounced biological activities . The chemistry of Nbridged heterocycles derived from 1, 2, 4-triazole has received considerable attention in recent years due to their usefulness in different areas of biological activities and as 3 industrial intermediates . A large number of heterocyclic compounds containing the 1, 2, 4-triazole ring and N-C-S linkage of triazole especially responsible for biological 2 3 4 activities i.e.…”

Section: Introductionmentioning

confidence: 99%

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Tirunagari¹,

Jangala²,

Nandagopal³

2014

IJPER

View full text Add to dashboard Cite

A series of potential bioactive compounds, 4-Amino-5-mercapto-3-(4-chlorophenyl)-1, 2, 4-triazole (1d), 4-Amino-5-mercapto-3-(4-nitrophenyl)-1, 2, 4-triazole (2d) , 4-Amino-5-mercapto-3-(2, 4-dichlorophenyl)-1, 2, 4-triazole (3d), 4-Amino-5-mercapto-3-(2-chlorophenyl)-1, 2, 4-triazole (4d), 4-Amino-5-mercapto-3-(2-methylphenyl)-1, 2, 4-triazole (5d), 4-Amino-5-mercapto-, 2, 4-triazole (6d) were synthesized according to the 1 literature methods. The synthesized compounds were characterized by FT-IR, H NMR spectroscopy, C H N analysis and anticancer activity was evaluated.Male Swiss albino mice has been used as test animal. Tumor cells used for anticancer activity were EAC (Ehrlich Ascites Carcinoma). Compounds were given at a dose of 25 mg/kg body weight intraperitoneally. groups were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition and non-viable cell count and increase in life span (%ILS). All the compounds exhibited the significant (P< 0.01) anticancer activity compared to control and the compound 4d is found to be the most potent one. The standard drug was used as 5-Fluorouracil (20mg/kg, body weight).Keywords: 1, 2, 4-triazole, anticancer activity, tumor cell count, tumor weight inhibition. 3-(4-methoxyophenyl)-1 Compounds treated (III-VIII)ABSTRACT

show abstract

“…Compounds including a 1,2-diazole nucleus and N-substituted derivatives are known to possess various biological activity [1]. Among these types of molecules have been shown to have various important biological activity such as antibacterial, antifungal, antiviral, diuretic, antituberculostatic, anti-HIV, antihistaminic anticancer, anticonvulsant, anti-inflammatory and analgesic properties [3][4][5][6][7]. Sulpha/substituted 1,2-diazoles may serve as the alternative sources for the development of new antiinflamatory agents due to their biological activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis And Anti-Inflammatory Activity On Sulpha/Substituted Pyrazoles(1,2-Diazole)

Malik¹

2013

iosrphr

View full text Add to dashboard Cite

Synthesis and Antimicrobial Activity of 1,2,4‐Triazoles

Cited by 9 publications

References 3 publications

Structure–Activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold

Structure–Activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold

Development and Physicochemical, In Vitro and In Vivo Evaluation of Transdermal Patches of Zaleplon

Synthesis And Anti-Inflammatory Activity On Sulpha/Substituted Pyrazoles(1,2-Diazole)

Contact Info

Product

Resources

About