Synthesis of New Heterocyclic Compounds with Biological Activity against Pathogenic Microbes in the Albaha Area

Abstract

Several new heterocyclic derivatives containing fused pyrazoloxazine moieties were synthesized via cycloaddition reactions of binucleophilic dentates, including hydrazine hydrate and its derivatives as well as active methylene compounds and aniline derivatives, resulting in novel five-, six-and seven-membered heterocyclic compounds. Due to increased microbial resistance to currently available drugs accentuate a real problem, so novel antimicrobial drugs are needed. Pyrazoles are good candidate as antimicrobial agents, where they have low-molecularweight compounds, nonvolatile and chemically stable. The novel synthesized five-, six-and seven-membered heterocyclic compounds were tested for their antimicrobial activity against different pathogenic microorganisms inside Albaha area. Bacterial species included Staphylococcus aureus, Staphylococcus epidermidis, Salmonella enteritidis, Streptococcus faecalis, Streptococcus agalactiae, Klebsiella pneumonia, Proteus mirabilis, Pseudomonas aeruginosa, Acinetobacter baumannii, and Enterobacter aerogenes. However, the following fungi were tested: Aspergillus niger, Aspergillus fumigates, Penicillium chrysogenium, Trichophyton rubrum and Candida albicans 157 and Candida albicans causes candidiasis. Staphylococcus aureus 119 was largely inhibited were observed after contact with synthesized pyrazoloxazine derivatives 1, 5, 8, 10, 13 and 24. Of the susceptible bacteria, Klebsiella pneumonia and Enterobacter aerogens 157 were the least affected, with inhibition zones between 10 and 12 mm. The pyrazoloxazine derivatives 3, 4, 25, 2Y, Ox1 and Ox2 inhibited all the fungi tested, including Aspergillus niger, Aspergillus fumigatus, Penicillium chrysogenium and Trichophyton rubrum. The zones of inhibition ranged from 40 to 14 mm/disc for these organisms. The current study demonstrates that the newly synthesized pyrazoloxazine derivatives have a good inhibition capacity against most tested pathogenic bacterial and fungal species.