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1,2,4-Triazole synthesis - Organic chemistry

SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF SOME NEWLY 1, 2, 4-TRIAZOLE DERIVATIVES

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1-Benzyl-4-phenyl-1H-1,2,3-triazole | C15H13N3 | …

Antimicrobial activity: All the newly synthesized compounds 3a-3h, 4a-4h and 5a-5h were tested for their antimicrobial activity. The effects of unknown compounds were compared with the standard drug; gatifloxacin and ciprofloxacin for bacteria and fluconazole for fungi. The antimicrobial activity was assayed by using cup plate method Chuinkshank et al 17 by using the inhibition zones in mm. Antibacterial activity was performed against Staphyloccus aureus, Escherischia coli, Proteus vulgaris, Klebsiella pneumoniae and antifungal activity against Aspergillus fumigatus, Candida albicans, Candida albicans ATCC and Candida krusei.

Categories: Synthesis of N-Heterocycles > Synthesis of 1,2,4-triazoles

INTRODUCTION:The triazole ring is an important pharmacophore in modern drug discovery. The chemistry and pharmacology of triazoles have been of great interest to medicinal chemistry because its derivatives possessed various biological activities such as antimicrobial 1-3, anti-inflammatory 4, anticancer 5, anti-histaminic 6

Synthesis of 3,5-DINITRO-1,2,4-TRIAZOLE - …

ABSTRACT: A series of 1-(2-(4H-1,2,4-triazol-4-yl)ethylamino)-3-chloro-4-(5-methoxy/ehthoxy-2-substituted alkyl/aryl-1H-indol-3-yl)azetidinones (4a-4h) and 1-(2-(4H-1,2,4-triazol-4-yl) ethylamino)-3-chloro-4-(5-methoxy/ethoxy-2-substituted alkyl/aryl-1H-indol-3-yl)thiazolidinones (5a-5h) have been synthesized by the reaction of 3-((2-(2-(4H-1,2,4-triazol-4-yl)ethyl)hydrazono)methyl)-5-methoxy/ethoxy-2-substituted-1H-indoles (3a-3h) with chloroacetyl chloride and thioglycolic acid respectively. All the newly synthesized compounds were screened for their antibacterial activity against S. aureus, E. coli, P. vulgaris, K. pneumoniae and antifungal activity against A. fumigatus, C. albicans, C. albicans ATCC and C. Krusei G03. The antibacterial activity of newly synthesized compounds compared with standard drug gattifloxacin and ciprofloxacin against different bacteria and antifungal activity of newly compounds compared with standard drug fluconazole against different fungi. The compounds 5d, 5e, 5g and 5h exhibited good antibacterial activity while compounds 4g, 5g and 5h also showed notable antifungal activity. The purity of the newly synthesized compounds was checked by thin layer chromatography (TLC) on silica gel-G coated plates using different solvent systems. The structure of all the compounds were established by the elemental (C, H, N) and spectral (IR, 1HNMR and mass) analysis.

Azetidinone derivatives have been reported to show a variety of antimicrobial 11-12, antituberculocis 13. Thiazolidinone moiety with triazole ring increases the antimicrobial activity 14-16. These all activities showed that the minor change in the substitution batter activities of azetidine and thiazolidine derivatives have enhanced dramatically so our research group decide to synthesized a new series azeti/thiazolidine derivatives with several substitutions.

Synthesis description for preparation of 3,5-DINITRO-1,2,4-TRIAZOLE


1. R.P. Iyer, W. Egan, J.B. Regan, and S.L. Beaucage, J. Amer. Chem. Soc., 1990, 112, 1253-1254.
2. M. Overhoff and G. Sczakiel, EMBO Rep, 2005, 6, 1176-81.
3. J. Krutzfeldt, et al., Nature, 2005, 438, 685-9.
4. B.A. Kraynack and B.F. Baker, RNA, 2006, 12, 163-76.
5. B.J. Bergot and W. Egan, Journal of Chromatography, 1992, 599, 35-42.

Chemistry: All reagents and solvents were of analytical grade and used directly. Reactions were routinely performed in oven-dried borosil glassware. The melting points of compounds were determined in open capillaries with the help of thermonic melting point apparatus and were uncorrected. The homogeneity of all newly synthesized compounds was routinely checked by thin layer chromatography (TLC) on silica gel G plates and spots were located by using iodine chamber. Elemental analysis (C, H, N) of all the synthesized compounds were determined by perkin-Elmer 2400 elemental analyzer, and results were found within the ± 0.4% of theoretical values. The IR spectra were recorded on a Beckman Acculab-10 spectrometer (ν max in cm-1) and the 1H NMR spectra were recorded by Brucker DPX-300 MHz using CDCl3 as solvent. Mass spectra were determined on VG-70-S instrument.

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1H-1,2,4-Triazole | C2H3N3 - PubChem

Our experiments demonstrate that a 0.05 M solution of Sulfurizing Reagent II is recommended for the synthesis of RNA phosphorothioates. A sulfurizing time of 2-4 minutes generated oligophosphorothioates of high quality. This was true for both TOM-RNA and TBDMS-RNA monomers. As shown in Figure 2, Beaucage Reagent was significantly more sluggish than Sulfurizing Reagent II. Representative HPLC analyses5 of RNA oligos are shown in Figure 3. The chromatogram on the left was obtained from sulfurizing U-TOM-RNA linkages for 60 seconds with Beaucage Reagent. The large n-1 peak is due to incomplete stepwise sulfurization and accumulation of deletions. The chromatogram on the right was an identical synthesis except using Sulfurizing Reagent II. Individual RNA sequences, especially those containing stretches of purine nucleoside residues are more difficult to sulfurize irrespective of the reagent used. To obtain a high degree of sulfurization with those oligonucleotides, a 0.1 M solution of Sulfurizing Reagent II and/or extended contact time may be required.

Carbazole is an aromatic heterocyclic organic compound

All the newly synthesized compounds 3a-3h, 4a-4h and 5a-5h were tested for their antimicrobial activity. The pharmacological data of all the compounds have been reported in table 1. The results revealed that the majority of the synthesized compounds showed varying degree of inhibition against the tested microorganism. The alkyl, phenyl and chlorophenyl substitution is beneficial for the antibacterial as well as antifungal activities. The methoxy and ethoxy substituent’s on indole nucleus increase the antimicrobial activity. Compounds having azetidinone and thiazolidinone moiety exhibited better antimicrobial activities. It can be seen in table 1, although all the compounds are not as active as standard drugs. Compounds 5g was found more potent antibacterial agents against different bacteria with standard drug gatifloxacin and ciprofloxacin. Compounds 4e, 4g, 5a, 5b, 5d, 5e, 5f and 5h showed moderate activity and rest compounds showed less activity against all the strains. Compounds 5g (against C. albicans), 5h (against C. albicans ATCC), 4g, 5g and 5h (against C. krusei GO3) showed good antifungal activity compared with fluconazole.

SULFURIZING REAGENT II - STABLE IN SOLUTION AND …

A new sulfurizing reagent must, therefore, exhibit all the good properties of Beaucage Reagent while adding good stability in solution on the synthesizer AND offering strong ability to sulfurize RNA linkages. We are happy to offer Sulfurizing Reagent II, 3-((Dimethylamino-methylidene)amino)-3H-1,2,4-dithiazole-3-thione, DDTT (2). Use of Sulfurizing Reagent II in RNA Synthesis

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