Synthesis of Novel Substituted Tetrazoles Having Antifungal Activity.

Abstract

Activity. -In an effort to find novel potent antifungal agents, a variety of tetrazoles such as (IX), (X), (XI), and (XII) (58 examples in all) are synthesized and evaluated for their antifungal activity. Some of these compounds, e.g.(IXb-d), (Xb,c), (XIa), and (XIIa) possess good antifungal activity against different fungal cultures. In general, introduction of an additional methyl group at C-3 in compounds (IX) and (X) results in significant improvements of antifungal activity. -(UPADHAYAYA, R. S.; JAIN, S.; SINHA, N.; KISHORE, N.; CHANDRA, R.; ARORA*, S. K.; Eur.

Isotopic effect on tautomeric behavior of 5‐(2,6‐disubstituted‐aryloxy)‐tetrazoles

“…5-Substituted tetrazoles are reported to possess antibacterial, [1 -3] antifungal, [4] antiviral, [5 -7] analgesic, [8 -11] antiinflammatory, [12 -15] antiulcer [16 -18] and antihypertensive [19,20] activities. The tetrazole function is metabolically stable.…”

N-(Cyanomethyl)benzamide

“…Data collection: APEX2 (Bruker, 2005); cell refinement: SAINT (Bruker, 2005); data reduction: SAINT; program(s) used to solve structure: SHELXS97 (Sheldrick, 2008); program(s) used to refine structure: SHELXL97 (Sheldrick, 2008); molecular graphics: PLATON (Spek, 2009) and ORTEP-3 for Windows (Farrugia, 1997); software used to prepare material for publication: publCIF (Westrip, 2010). Tetrazoles derivatives are an important class of compounds, which can be used in the fields of bioorganic and medicinal chemistry as antibacterials, anti-cancer, heart disease, neurodegenerative disease, and antifungal activity (Smissman et al,1976;McGuire et al, 1990;Lunn et al, 1992;Itoh et al, 1995;Upadhayaya et al, 2004;Wu et al, 2008;Rostom et al, 2009. The tetrazole moiety has long been established as a bioisostere of a carboxyl unit (Burger, 1991). A major advantage of tetrazoles over carboxylic acids is that they are resistant to many biological metabolic degradation pathways (Singh et al, 1980).…”

“…For the biological activity and medicinal properties of tetrazole derivatives, see : Smissman et al (1976); McGuire et al (1990); Lunn et al (1992); Itoh et al (1995); Upadhayaya et al (2004); Wu et al (2008); Rostom et al (2009);Burger (1991); Singh et al (1980). For the synthetic procedure, see: Adams & Langley (1941a,b).…”

Synthesis, antimicrobial and antioxidant activities of 1-(1,4-benzodioxane-2-carbonyl)piperazine derivatives

“…Piperazine is currently the most important building block used in drug discovery with a high number of positive hits encountered in biological screens of this heterocycle and its congeners. A literature survey revealed that piperazine derivatives are important pharmacophores across a number of different therapeutic areas [6] and act as antifungal [7], antibacterial, antimalarial, antipsychotic [8] and anti-HIV protease [9]. Piperazine sulfonamides are most widely used antibacterial agents [10] in the world, chiefly because of their low cost, low toxicity, and excellent activity against common bacterial disease.…”