Data on the synthetic routes to substituted 1,2,3-triazoles, including those containing functional groups, based on cyclisation of various nitrogen compounds published during the last 15 years are described. Examples of using new triazole derivatives in agrochemistry, medicine and engineering are given.

https://iopscience.iop.org/article/10.1070/RC2005v074n04ABEH000893/pdf

1,2,3-Triazole and its derivatives. Development of methods for the formation of the triazole ring

2.3. Amides and Lactams 3435 2.4. Imides 3448 2.5. Thiophenes 3451 2.6. Thiazolines, Thiazoles, and Thiazines 3454 2.7. Dithiazoles 3456 2.8. Thiadiazoles 3456 2.9. Imidazolines and Pyrimidines 3456 2.10. Alcohols 3458 2.11. PdO to PdS 3461 2.12. Reduction 3462 2.13. Nucleotides, Purines, and Pyrimidines 3463 2.14. Miscellaneous 3467 2.15. P4S10 vs Lawesson’s Reagent (LR) 3473 3. Conclusion 3473 4. Acknowledgments 3473 5. References 3473

A Berzelius Reagent, Phosphorus Decasulfide (P4S10), in Organic Syntheses

Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents

A novel compound having excellent JNK inhibitory activity. It is a compound represented by the following general formula or a salt thereof. (I) In the formula, R1 represents -(CO)h-(NRa)j-(CRb=CRc)k-Ar (wherein Ra, Rb, and Rc each independently represents hydrogen, halogeno, hydroxy, optionally substituted C1-6 alkyl, etc.); Cy means a 5- or 6-membered aromatic heterocycle; and V's each independently means -L-X-Y [wherein L means a single bond, optionally substituted C1-6 alkylene, etc.; X means a single bond, -A- (wherein A represents NR2, O, CO, S, SO, or SO2), etc.; and Y means hydrogen, halogeno, nitro, etc.].

Pyrazole compound and medicinal composition containing the same

Design, synthesis, characterization, in vitro and in silico evaluation of novel imidazo[2,1-b][1,3,4]thiadiazoles as highly potent acetylcholinesterase and non-classical carbonic anhydrase inhibitors.

2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation of the respective 6-aryl-2-(2-aryl-2H-1,2,3-triazol-4-yl)imidazo[2,1-b]-1,3,4-thiadiazoles 5. Reactivity of the latter fused ring towards reaction with different electrophilic reagents afforded the corresponding 5-substituted derivatives 6-8. The structure of the above compounds was confirmed from their spectral characteristics. Some of these compounds were found to possess slight to moderate activity against the microorganisms Staphylococcus aureus, Candida albicans, Pseudomonas aeruginosa, and Escherichia coli.

https://www.mdpi.com/1420-3049/16/7/5496/pdf?origin=publicationDetail

Synthesis and Antibacterial Activities of Novel Imidazo(2,1-b)-1,3,4-thiadiazoles

Synthesis of acetylenic β-diketones and their conversion into 4H-pyran-4-ones, pyrazoles, and 1-hydroxy-4-pyridones

5-Aryl-2-phenylpyrazolo[1,5-c]pyrimidine-7(6H)-thiones have been synthesized by the reaction of 1,5-diaryl-4-pentyne-1,3-diones with thiosemicarbazide and their reactions were studied. The pyrazolopyrimidinethiones give with certain electrophiles the respective 3-substituted 7-thiones. Their oxidation affords the corresponding disulfide. Moreover, they can be converted to the corresponding pyrazolopyrimidinones on reaction with alkaline hydrogen peroxide. The structure of the above compounds was confirmed from their spectral characteristics.

A new synthesis of pyrazolo[1,5-c]pyrimidines from acetylenic β-diketones

Aim: A new series of pyrazolo[1,5-c]pyrimidines were synthesized by different hybridization strategies. Methodology: All structures were confirmed by IR, 1H, 13C, 1H-13C heteronuclear multiple-quantum correlation (HMQC) spectra and microanalysis. They were evaluated for their in vitro antileishmanial activity against miltefosine and amphotericin B deoxycholate as reference drugs. Results: The most active compounds 2a and 9a demonstrated superior potencies to miltefosine by ten- and six-fold, respectively, for the promastigote form, and by 5.5-fold for the amastigote form. Their binding scenario to Leishmania major pteridine reductase was rationalized by docking experiments. In addition, all compounds were safe for the experimental animals orally up to 150 mg/kg and parenterally up to 75 mg/kg. Conclusion: This study provides novel chemotype class for antileishmanial activity.

M. G. Marei

Papers

Synthesis and Antibacterial Activities of Novel Imidazo(2,1-b)-1,3,4-thiadiazoles

Synthesis of acetylenic β-diketones and their conversion into 4H-pyran-4-ones, pyrazoles, and 1-hydroxy-4-pyridones

A new synthesis of pyrazolo[1,5-c]pyrimidines from acetylenic β-diketones

Synthesis, modeling and biological evaluation of hybrids from pyrazolo[1,5c]pyrimidine as antileishmanial agents.

Synthesis and reactions of 3‐iodo‐4H‐pyran‐4‐ones