Synthesis, biological evaluation and in silico studies of tetrazole-heterocycle hybrids

Thiophene‐containing compounds with antimicrobial activity

“…[68] All these thiophenes were active against S. Through the reaction of thiophene-2-carboxylic monosubstituted amides with sodium azide in the presence of POCl 3 , four thiophene-tetrazole hybrids 62 (Figure 7) were prepared. [69] On the basis of the diameter of the inhibition zone, all these thiophenes were active against K. pneumoniae, but only compound 62 (R = 1-(methylsulfonyl)piperidin-4-yl) inhibited the growth of P. aeruginosa…”

“…Through the reaction of thiophene‐2‐carboxylic monosubstituted amides with sodium azide in the presence of POCl 3 , four thiophene–tetrazole hybrids 62 (Figure 7) were prepared. [ 69 ] On the basis of the diameter of the inhibition zone, all these thiophenes were active against K. pneumoniae , but only compound 62 (R = 1‐(methylsulfonyl)piperidin‐4‐yl) inhibited the growth of P. aeruginosa and S. pyogenes , while two compounds 62 (R = C 6 H 5 and 4‐FC 6 H 4 ) were active against S. aureus . With the exception of compound 62 (R = 1‐(methylsulfonyl)piperidin‐4‐yl), all others were active against C. albicans , with analog 62 (R = C 6 H 5 ) showing 75% of the diameter of the inhibition zone produced by reference drug ketoconazole under the same conditions.…”

Synthesis of substituted 5-(thiophen-2-yl)-1H-tetrazoles

“…Compounds containing of thiophene and tetrazole cycles are reported as antibacterial nonpeptide antagonists platelet aggregators, antithrombotic agents [0, 2] and nonlinear optical materials [3]. Similarly, these derivatives are well known to exhibit various activities such as anti-inflammatory [4,5], antibacterial [4][5][6], anticancer [7][8][9][10][11], antiviral [11], antifungal [12], inhibition of keratinocyte hyperproliferation [13] activities. In particular, thiophene-containing compounds are of considerable interest as anticancer drugs [7][8][9][10][11].…”

“…____________________  Shehedyn M., Barabash O., Ostapiuk M. et al, 2022 Therefore, in recent years, extensive studies of the bioactivity of compounds containing the combination of thiophene and tetrazole cycles as selective inhibitors of histone deacetylase 6 [9] and CDK8 kinase [8]. This allows it to be considered as highly effective potential anticancer agents, as well as AT2 receptor ligands [14], antiinflammatory and antibacterial agents [5]. Therefore, it is still perspective to continue studying of synthesis and reactivity of the compounds containing the thiophene and tetrazole fragments combinations.…”

Synthesis and Evaluation of Antidepressant Activities of 5-Aryl-4,5-dihydrotetrazolo [1,5-a]thieno[2,3-e]pyridine Derivatives

“…It is well-known that in compounds with a tetrazole fragment, this fragment has a great influence on the biological activity of the compound, showing, for instance, antifungal [7], antibacterial [8], antileishmanial [9], anticancer [10,11], anticonvulsant [12,13], and antidepressant effects [14]. Our group has studied a series of 7-alkyl-7 H -tetrazolo [1,5- g ]purine derivatives ( I ) (Figure 1), where most of the target compounds showed a significant antidepressant activity [15].…”