Displaying publications 1 - 20 of 238 in total

Abstract:
Sort:
  1. Aziman N, Abdullah N, Noor ZM, Kamarudin WS, Zulkifli KS
    J Food Sci, 2014 Apr;79(4):M583-92.
    PMID: 24666004 DOI: 10.1111/1750-3841.12419
    Preliminary phytochemical and flavonoid compounds of aqueous and ethanolic extracts of 6 aromatic Malaysian herbs were screened and quantified using Reverse-Phase High Performance Liquid Chromatography (RP-HPLC). The herbal extracts were tested for their antimicrobial activity against 10 food-borne pathogenic and food spoilage microorganisms using disk diffusion assay. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC)/minimum fungicidal concentration (MFC) of herbal extracts were determined. In the phytochemical screening process, both aqueous and ethanolic extracts of P. hydropiper exhibited presence of all 7 tested phytochemical compounds. Among all herbal extracts, the aqueous P. hydropiper and E. elatior extracts demonstrated the highest antibacterial activity against 7 tested Gram-positive and Gram-negative bacteria with diameter ranging from 7.0 to 18.5 mm and 6.5 to 19 mm, respectively. The MIC values for aqueous and ethanolic extracts ranged from 18.75 to 175 mg/mL and 0.391 to 200 mg/mL, respectively while the MBC/MFC values for aqueous and ethanolic extracts ranged from 25 to 200 mg/mL and 3.125 to 50 mg/mL, respectively. Major types of bioactive compounds in aqueous P. hydropiper and E. elatior extracts were identified using RP-HPLC instrument. Flavonoids found in these plants were epi-catechin, quercetin, and kaempferol. The ability of aqueous Persicaria hydropiper (L.) H. Gross and Etlingera elatior (Jack) R.M. Sm. extracts to inhibit the growth of bacteria is an indication of its broad spectrum antimicrobial potential. Hence these herbal extracts may be used as natural preservative to improve the safety and shelf-life of food and pharmaceutical products.
    Matched MeSH terms: Bacteria/drug effects*
  2. Jia Y, Zhao L
    Eur J Med Chem, 2021 Nov 15;224:113741.
    PMID: 34365130 DOI: 10.1016/j.ejmech.2021.113741
    Bacterial infection is amongst the most common diseases in community and hospital settings. Fluoroquinolones, exerting the antibacterial activity through binding to type II bacterial topoisomerase enzymes, DNA gyrase and topoisomerase IV, are mainstays of chemotherapy. At present, fluoroquinolones are the most valuable antibacterial agents used popularly. However, the emergence of more virulent and resistant pathogens by the development of either mutated DNA-binding proteins or efflux pump mechanism for fluoroquinolones results in an urgent demand to develop new fluoroquinolones to withstand the drug resistance and to obtain a broader spectrum of activity. This review aims to outline the recent advances of fluoroquinolone derivatives with antibacterial potential and to summarize the structure-activity relationship (SAR) so as to provide an insight for rational design of more active candidates, covering articles published between January 2018 and June 2021.
    Matched MeSH terms: Bacteria/drug effects*
  3. Yu L, Lu M, Zhang W, Alarfaj AA, Hirad AH, Zhang H
    Microb Pathog, 2020 Apr;141:103960.
    PMID: 31953224 DOI: 10.1016/j.micpath.2019.103960
    BACKGROUND: Mycoplasma pneumoniae (MP) is a common cause of community-acquired pneumonia (CAP) among the children and adults that results upper and lower respiratory tract infections.

    OBJECTIVE: This study was aimed to inspect the ameliorative action of A. chinensis synthesized ZnONPs against M. pneumoniae infected pneumonia mice model.

    MATERIALS AND METHODS: ZnO NPs was synthesized from Albizia chinensis bark extract and characterized by UV-Vis spectroscopy, Fourier Transform Infrared (FTIR), Transmission Electron Microscopy (TEM), energy dispersive X-ray (EDX) and atomic force microscope (AFM) analyses. The antibacterial effectual of synthesized ZnONPs were examined against clinical pathogens. The pneumonia was induced to BALB/c mice via injecting the M. pneumoniae and treated with synthesized ZnONPs, followed by the total protein content, total cell counts and inflammatory mediators level was assessed in the BALF of experimental animals. The Histopathological investigation was done in the lung tissues of test animals.

    RESULTS: The outcomes of this work revealed that the formulated ZnONPs was quasi-spherical, radial and cylindrical; the size was identified as 116.5 ± 27.45 nm in diameter. The in vitro antimicrobial potential of formulated ZnO-NPs displayed noticeable inhibitory capacity against the tested fungal and bacterial strains. The administration of synthesized ZnO-NPs in MP infected mice model has significantly reduced the levels of total protein, inflammatory cells, inflammatory cytokines such as IL-1, IL-6, IL-8, tumour necrosis factor-alpha (TNF-a) and transforming growth factor (TGF). Besides, the histopathological examination of MP infected mice lung tissue showed the cellular arrangements were effectively retained after administration of synthesized ZnO-NPs.

    CONCLUSION: In conclusion, synthesized ZnO-NPs alleviate pneumonia progression via reducing the level of inflammatory cytokines and inflammatory cells in MP infected mice model.

    Matched MeSH terms: Bacteria/drug effects
  4. Gorajana A, Venkatesan M, Vinjamuri S, Kurada BV, Peela S, Jangam P, et al.
    Microbiol Res, 2007;162(4):322-7.
    PMID: 16580188
    In our systematic screening programme for marine actinomycetes, a bioactive Streptomycete was isolated from marine sediment samples of Bay of Bengal, India. The taxonomic studies indicated that the isolate belongs to Streptomyces chibaensis and it was designated as S. chibaensis AUBN1/7. The isolate yielded a cytotoxic compound. It was obtained by solvent extraction followed by the chromatographic purification. Based on the spectral data of the pure compound, it was identified as quinone-related antibiotic, resistoflavine (1). It showed a potent cytotoxic activity against cell lines viz. HMO2 (Gastric adenocarcinoma) and HePG2 (Hepatic carcinoma) in vitro and also exhibited weak antibacterial activities against Gram-positive and Gram-negative bacteria.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  5. Goh TC, Bajuri MY, C Nadarajah S, Abdul Rashid AH, Baharuddin S, Zamri KS
    J Foot Ankle Res, 2020 Jun 16;13(1):36.
    PMID: 32546270 DOI: 10.1186/s13047-020-00406-y
    BACKGROUND: Diabetic foot infection is a worldwide health problem is commonly encountered in daily practice. This study was conducted to identify the microbiological profile and antibiotic sensitivity patterns of causative agents identified from diabetic foot infections (DFIs). In addition, the assessment included probable risk factors contributing to infection of ulcers that harbour multidrug-resistant organisms (MDROs) and their outcomes.

    METHODS: We carried out a prospective analysis based on the DFI samples collected from 2016 till 2018. Specimens were cultured with optimal techniques in addition to antibiotic susceptibility based on recommendations from The Clinical and Laboratory Standards Institute (CLSI). A total of 1040 pathogens were isolated with an average of 1.9 pathogens per lesion in 550 patients who were identified with having DFIs during this interval.

    RESULTS: A higher percentage of Gram-negative pathogens (54%) were identified as compared with Gram-positive pathogens (33%) or anaerobes (12%). A total of 85% of the patients were found to have polymicrobial infections. Pseudomonas aeruginosa (19%), Staphylococcus aureus (11%) and Bacteroides species (8%) appeared to be the predominant organisms isolated. In the management of Gram-positive bacteria, the most efficacious treatment was seen with the use of Vancomycin, while Imipenem and Amikacin proved to be effective in the treatment of Gram-negative bacteria.

    CONCLUSION: DFI's are common among Malaysians with diabetes, with a majority of cases displaying polymicrobial aetiology with multi-drug resistant isolates. The data obtained from this study will be valuable in aiding future empirical treatment guidelines in the treatment of DFIs. This study investigated the microbiology of DFIs and their resistance to antibiotics in patients with DFIs that were managed at a Tertiary Care Centre in Malaysia.

    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  6. Zaidan MR, Noor Rain A, Badrul AR, Adlin A, Norazah A, Zakiah I
    Trop Biomed, 2005 Dec;22(2):165-70.
    PMID: 16883283 MyJurnal
    Medicinal plants have many traditional claims including the treatment of ailments of infectious origin. In the evaluation of traditional claims, scientific research is important. The objective of the study was to determine the presence of antibacterial activity in the crude extracts of some of the commonly used medicinal plants in Malaysia, Andrographis paniculata, Vitex negundo, Morinda citrifolia, Piper sarmentosum, and Centella asiatica. In this preliminary investigation, the leaves were used and the crude extracts were subjected to screening against five strains of bacteria species, Methicillin Resistant Staphylococcus aureus (MRSA), Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli, using standard protocol of Disc Diffusion Method (DDM). The antibacterial activities were assessed by the presence or absence of inhibition zones and MIC values. M. citrifolia, P. sarmentosum and C. asiatica methanol extract and A. paniculata (water extract) have potential antibacterial activities to both gram positive S. aureus and Methicillin Resistant S. aureus (MRSA). None of the five plant extracts tested showed antibacterial activities to gram negative E. coli and K. pneumoniae, except for A. paniculata and P. sarmentosum which showed activity towards P. aeruginosa. A. paniculata being the most potent at MIC of 2 g/disc. This finding forms a basis for further studies on screening of local medicinal plant extracts for antibacteria properties.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects*
  7. Arshad A, Osman H, Bagley MC, Lam CK, Mohamad S, Zahariluddin AS
    Eur J Med Chem, 2011 Sep;46(9):3788-94.
    PMID: 21712145 DOI: 10.1016/j.ejmech.2011.05.044
    Two novel series of hydrazinyl thiazolyl coumarin derivatives have been synthesized and fully characterized by IR, (1)H NMR, (13)C NMR, elemental analysis and mass spectral data. The structures of some compounds were further confirmed by X-ray crystallography. All of these derivatives, 10a-d and 15a-h, were screened in vitro for antimicrobial activity against various bacteria species including Mycobacterium tuberculosis and Candida albicans. The compounds 10c, 10d and 15e exhibited very good activities against all of the tested microbial strains.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  8. Chelliapan S, Wilby T, Sallis PJ, Yuzir A
    Water Sci Technol, 2011;63(8):1599-606.
    PMID: 21866757
    Tylosin has been considered inhibiting COD removal in anaerobic digestion. In this study it is proven that this is not always the case. Accordingly, elevated concentrations of Tylosin (100-800mgL-1) could be tolerated by the anaerobic system. The influence of Tylosin concentrations on an up-flow anaerobic stage reactor (UASR) was assessed using additions of Tylosin phosphate concentrate. Results showed high efficiency for COD removal (average 93%) when Tylosin was present at concentrations ranging from 0 to 400 mg L-1. However, at Tylosin concentrations of 600 and 800 mg L-1 treatment efficiency declined to 85% and 75% removal respectively. The impact of Tylosin concentrations on archaeal activity were investigated and the analysis revealed that archaeal cells dominated the reactor, confirming that there was no detectable inhibition of the methanogens at Tylosin levels between 100 and 400mg L-1. Nevertheless, the investigation showed a slight reduction in the number of methanogens at Tylosin levels of 600 and 800 mg L-1. These results demonstrated that the methanogens were well adapted to Tylosin. It would not be expected that the process performance of the UASR would be affected, not even at a level well in excess of those appearing in real wastewater from a Tylosin production site.
    Matched MeSH terms: Bacteria/drug effects*
  9. Fathilah AR, Rahim ZH, Othman Y, Yusoff M
    Pak J Biol Sci, 2009 Mar 15;12(6):518-21.
    PMID: 19580002
    In this study, the bacteriostatic effect of Piper betle and Psidium guajava extracts on selected early dental plaque bacteria was investigated based on changes in the doubling time (g) and specific growth rates (micro). Streptococcus sanguinis, Streptococcus mitis and Actinomyces sp. were cultured in Brain Heart Infusion (BHI) in the presence and absence of the extracts. The growth of bacteria was monitored periodically every 15 min over a period of 9 h to allow for a complete growth cycle. Growth profiles of the bacteria in the presence of the extracts were compared to those in the absence and deviation in the g and micro were determined and analyzed. It was found that the g and mu were affected by both extracts. At 4 mg mL(-1) of P. betle the g-values for S. sanguinis and S. mitis were increased by 12.0- and 10.4-fold, respectively (p < 0.05). At similar concentration P. guajava increased the g-value by 1.8- and 2.6 -fold, respectively (p < 0.05). The effect on Actinomyces sp. was observed at a much lower magnitude. It appears that P. betle and P. guajava extracts have bacteriostatic effect on the plaque bacteria by creating a stressed environment that had suppressed the growth and propagation of the cells. Within the context of the dental plaque, this would ensure the attainment of thin and healthy plaque. Thus, decoctions of these plants would be suitable if used in the control of dental plaque.
    Matched MeSH terms: Bacteria/drug effects*
  10. Banerjee S, Devaraja TN, Shariff M, Yusoff FM
    J Fish Dis, 2007 Jul;30(7):383-9.
    PMID: 17584435
    Use of antibiotics for the control of bacterial diseases in shrimp culture has caused several adverse impacts to the industry. This has resulted in the search for alternative environment friendly approaches to overcome bacterial infections. This study was conducted to investigate the use of beneficial bacteria as an alternative to antibiotics. Ten pathogenic bacterial species isolated from shrimp, Penaeus monodon, and Artemia cysts were tested for susceptibility to indigenous marine Bacillus subtilis AB65, Bacillus pumilus AB58, Bacillus licheniformis AB69 and compared with oxytetracycline, chloramphenicol, gentamicin and bacitracin, which are common antibiotics used in Asian aquaculture. The Bacillus spp. were isolated from the local marine environment for bioremediation use in shrimp hatcheries and were proven to reduce total ammonium nitrogen. The pathogenic bacterial isolates were 90% susceptible to B. subtilis AB65, 70% susceptible to B. pumilus AB58 and B. licheniformis AB69 and 100% susceptible to oxytetracycline, chloramphenicol and gentamicin but only 40% to bacitracin. Two representative isolates of the vibrio group, Vibrio alginolyticus VaM11 and Vibrio parahaemolyticus VpM1, when tested for competitive exclusion by a common broth method using the marine Bacillus spp., showed decreased viable counts from 10(8) to 10(2) cfu mL(-1). The results suggest that the action of the marine bacteria appears to be significant in protecting the host shrimp against pathogenic bacteria. In addition to the alternative use of antibiotics, the selected marine bacteria had additional bioremediation properties of reducing ammonia.
    Matched MeSH terms: Bacteria/drug effects*
  11. Sufian AS, Ramasamy K, Ahmat N, Zakaria ZA, Yusof MI
    J Ethnopharmacol, 2013 Mar 7;146(1):198-204.
    PMID: 23276785 DOI: 10.1016/j.jep.2012.12.032
    Muntingia calabura (Elaeocarpaceae) is one of the most common roadside trees in Malaysia. Its leaves, barks, flowers and roots have been used as a folk remedy for the treatment of fever, incipient cold, liver disease, as well as an antiseptic agent in Southeast Asia. The aim of this study is to isolate and identify the antibacterial and cytotoxic compounds from the leaves of Muntingia calabura L.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  12. Yusof MI, Yusof AH
    Med J Malaysia, 2004 Dec;59(5):574-7.
    PMID: 15889557
    Staphylococcus aureus infection remains the commonest organism causing musculoskeletal infection and antibiotic is the mainstay of treatment apart from adequate and appropriate surgical intervention. The exact figure of antibiotic resistance in orthopaedic practice is not known but it is expected to be higher than previously reported as the use of antibiotics is rampant. Its sensitivity to various antibiotics differs from one center to another making local surveillance necessary. From 66 patients with musculoskeletal infections studied in our centre, Staphylococcus aureus was cultured in 50-65% of patients, depending on the sample taken. Fifteen percent of this were methicillin resistant Staphylococcus aureus (MRSA). Staphylococcus aureus was found to be sensitive to cloxacillin in 95% of patients' sample. MRSA remained highly sensitive to vancomycin, clindamycin and fucidic acid.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects*; Gram-Positive Bacteria/drug effects*
  13. Hossain MI, El-Harbawi M, Alitheen NB, Noaman YA, Lévêque JM, Yin CY
    Ecotoxicol Environ Saf, 2013 Jan;87:65-9.
    PMID: 23107478 DOI: 10.1016/j.ecoenv.2012.09.020
    Three 1-(2-hydroxyethyl)-3-alkylimidazolium chloride room temperature ionic liquids (ILs) [2OHimC(n)][Cl]; (n=0, 1, 4) have been synthesized from the appropriate imidazole precursors and characterized by IR and NMR spectroscopies and elemental analysis. Their anti-microbial activities were investigated using the well-diffusion method. The viabilities of Escherichia coli, Aeromonas hydrophila, Listeria monocytogenes and Salmonella enterica as a function of IL concentrations were studied. The minimal inhibitory concentrations (MICs) and EC₅₀ values for the present ILs were within the concentration range from 60 to 125 mM and 23 to 73 mM. The anti-microbial potencies of the present ILs were compared to a standard antibiotic, gentamicin. The finding affords additional perspective on the level of ILs toxicity to aquatic lifeforms and yet, this characteristic can be readily harnessed to detect microbial growth and activity.
    Matched MeSH terms: Bacteria/drug effects*
  14. Othman N, Pan L, Mejin M, Voong JC, Chai HB, Pannell CM, et al.
    J Nat Prod, 2016 Apr 22;79(4):784-91.
    PMID: 26974604 DOI: 10.1021/acs.jnatprod.5b00810
    Four new 2,3-secodammarane triterpenoids, stellatonins A-D (3-6), together with a new 3,4-secodammarane triterpenoid, stellatonin E (7), and the known silvestrol (1), 5‴-episilvestrol (2), and β-sitosterol, were isolated from a methanol extract of the stems of Aglaia stellatopilosa through bioassay-guided fractionation. The structures of the new compounds were elucidated using spectroscopic and chemical methods. The compounds were evaluated for their cytotoxic activity against three human cancer cell lines and for their antimicrobial activity using a microtiter plate assay against a panel of Gram-positive and Gram-negative bacteria and fungi.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  15. Matin MM, Nath AR, Saad O, Bhuiyan MM, Kadir FA, Abd Hamid SB, et al.
    Int J Mol Sci, 2016 Aug 27;17(9).
    PMID: 27618893 DOI: 10.3390/ijms17091412
    Benzyl α-l-rhamnopyranoside 4, obtained by both conventional and microwave assisted glycosidation techniques, was subjected to 2,3-O-isopropylidene protection to yield compound 5 which on benzoylation and subsequent deprotection of isopropylidene group gave the desired 4-O-benzoylrhamnopyranoside 7 in reasonable yield. Di-O-acetyl derivative of benzoate 7 was prepared to get newer rhamnopyranoside. The structure activity relationship (SAR) of the designed compounds was performed along with the prediction of activity spectra for substances (PASS) training set. Experimental studies based on antimicrobial activities verified the predictions obtained by the PASS software. Protected rhamnopyranosides 5 and 6 exhibited slight distortion from regular ¹C₄ conformation, probably due to the fusion of pyranose and isopropylidene ring. Synthesized rhamnopyranosides 4-8 were employed as test chemicals for in vitro antimicrobial evaluation against eight human pathogenic bacteria and two fungi. Antimicrobial and SAR study showed that the rhamnopyranosides were prone against fungal organisms as compared to that of the bacterial pathogens. Interestingly, PASS prediction of the rhamnopyranoside derivatives 4-8 were 0.49 < Pa < 0.60 (where Pa is probability 'to be active') as antibacterial and 0.65 < Pa < 0.73 as antifungal activities, which showed significant agreement with experimental data, suggesting rhamnopyranoside derivatives 4-8 were more active against pathogenic fungi as compared to human pathogenic bacteria thus, there is a more than 50% chance that the rhamnopyranoside derivative structures 4-8 have not been reported with antimicrobial activity, making it a possible valuable lead compound.
    Matched MeSH terms: Bacteria/drug effects
  16. Perveen S, Safdar N, Chaudhry GE, Yasmin A
    World J Microbiol Biotechnol, 2018 Jul 14;34(8):118.
    PMID: 30008019 DOI: 10.1007/s11274-018-2500-1
    This paper describes the extracellular synthesis of silver nanoparticles from waste part of lychee fruit (peel) and their conjugation with selected antibiotics (amoxicillin, cefixim, and streptomycin). FTIR studies revealed the reduction of metallic silver and stabilization of silver nanoparticles and their conjugates due to the presence of CO (carboxyl), OH (hydroxyl) and CH (alkanes) groups. The size of conjugated nanoparticles varied ranging from 3 to 10 nm as shown by XRD. TEM image revealed the spherical shape of biosynthesized silver nanoparticles. Conjugates of amoxicillin and cefixim showed highest antibacterial activity (147.43 and 107.95%, respectively) against Gram-negative bacteria i.e. Alcaligenes faecalis in comparison with their control counterparts. The highest reduction in MIC was noted against Gram-positive strains i.e. Enterococcus faecium (75%) and Microbacterium oxydans (75%) for amoxicillin conjugates. Anova two factor followed by two-tailed t test showed non-significant results both in case of cell leakage and protein estimation between nanoparticles and conjugates of amoxicillin, cefixime and streptomycin. In case of MDA release, non-significant difference among the test samples against the selected strains. Our study found green-synthesized silver nanoparticles as effective antibacterial bullet against both Gram positive and Gram negative bacteria, but they showed a more promising effect on conjugation with selected antibiotics against Gram negative type.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects; Gram-Positive Bacteria/drug effects
  17. Yan LP, Gopinath SCB, Anbu P, Kasim FH, Zulhaimi HI, Yaakub ARW
    Prep Biochem Biotechnol, 2020;50(10):1053-1062.
    PMID: 32597353 DOI: 10.1080/10826068.2020.1783678
    This research comprehends iron-oxide nanoparticle (IONP) production, the apparent metallic nanostructure with unique superparamagnetic properties. Durian-rind-extract was utilized to synthesize IONP and the color of reaction mixture becomes dark brown, indicated the formation of IONPs and the peak was observed at ∼330 nm under UV-visible spectroscopy. The morphological observation under high-resolution microscopies has revealed the spherical shape and the average size (∼10 nm) of IONP. The further support was rendered by EDX-analysis showing apparent iron and oxygen peaks. XRD results displayed the crystalline planes with (110) and (300) planes at 2θ of 35.73° and 63.53°, respectively. XPS-data has clearly demonstrated the presence of Fe2P and O1s peaks. The IONPs were successfully capped by the polyphenol compounds from durian-rind-extract as evidenced by the representative peaks between 1633 and 595 cm-1 from FTIR analysis. The antimicrobial potentials of IONPs were evidenced by the disk-diffusion assay. The obtained results have abundant attention and being actively explored owing to their beneficial applications.
    Matched MeSH terms: Bacteria/drug effects
  18. Rahman ZA, Harun A, Hasan H, Mohamed Z, Noor SS, Deris ZZ, et al.
    Eye Contact Lens, 2013 Sep;39(5):355-60.
    PMID: 23982472 DOI: 10.1097/ICL.0b013e3182a3026b
    Ocular surface infections that include infections of conjunctiva, adnexa, and cornea have the potential risk of causing blindness within a given population. Empirical antibiotic therapy is usually initiated based on epidemiological data of common causative agents. Thus, the aims of this study were to determine the bacterial agents and their susceptibility patterns of isolates from ocular surface specimens in our hospital.
    Matched MeSH terms: Gram-Negative Bacteria/drug effects*; Gram-Positive Bacteria/drug effects*
  19. Al-Adiwish WM, Tahir MI, Siti-Noor-Adnalizawati A, Hashim SF, Ibrahim N, Yaacob WA
    Eur J Med Chem, 2013 Jun;64:464-76.
    PMID: 23669354 DOI: 10.1016/j.ejmech.2013.04.029
    New 5-aminopyrazoles 2a-c were prepared in high yields from the reaction of known α,α-dicyanoketene-N,S-acetals 1a-c with hydrazine hydrate under reflux in ethanol. These compounds were utilized as intermediates to synthesize pyrazolo[1,5-a]-pyrimidines 3a-c, 4a-d, 5a-c, and 6a-c, as well as pyrazolo[5,1-c][1,2,4]triazines 7a-c and 8a-c, by the reaction of 2-[bis(methylthio)methylene]malononitrile, α,α-dicyanoketene-N,S-acetals 1a-b, acetylacetone, acetoacetanilide as well as acetylacetone, and malononitrile, respectively. Furthermore, cyclization of 2a-c with pentan-2,5-dione yielded the corresponding 5-pyrrolylpyrazoles 9a-c. Moreover, fusion of 2a-c with acetic anhydride resulted in the corresponding 1-acetyl-1H-pyrazoles 10a-c. The antibacterial activity and cytotoxicity against Vero cells of several selected compounds are also reported.
    Matched MeSH terms: Bacteria/drug effects*
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links