Displaying publications 1 - 20 of 51 in total

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  1. Fulltext 4-(4-Bromophenyl)-thiazol-2-amine derivatives: synthesis, biological activity and molecular docking study with ADME profile
    Sharma D, Kumar S, Narasimhan B, Ramasamy K, Lim SM, Shah SAA, et al.
    BMC Chem, 2019 Dec;13(1):60.
    PMID: 31384808 DOI: 10.1186/s13065-019-0575-x
    In order to overcome the challenges of microbial resistance as well as to improve the effectiveness and selectivity of chemotherapeutic agents against cancer, a novel series of 4-(4-bromophenyl)-thiazol-2-amine derivatives was synthesized and its molecular structures were confirmed by physicochemical and spectral characteristics. The synthesized compounds were further evaluated for their in vitro antimicrobial activity using turbidimetric method and anticancer activity against oestrogen receptor positive human breast adenocarcinoma cancer cell line (MCF7) by Sulforhodamine B (SRB) assay. The antimicrobial activity results revealed that compound p2, p3, p4 and p6 exhibited promising antimicrobial activity that are comparable to standard norfloxacin (antibacterial) and fluconazole (antifungal). Anticancer screening results demonstrated that compound p2 was found to be the most active one against cancer cell line when compared to the rest of the compounds and comparable to the standard drug (5-fluorouracil). The molecular docking study demonstrated that compounds, p2, p3, p4 and p6 displayed good docking score within binding pocket of the selected PDB ID (1JIJ, 4WMZ and 3ERT) and showed promising ADME properties.
    Matched MeSH terms: Fluconazole
  2. Fulltext A catheter-related bloodstream infection caused by the yeast Kodamaea ohmeri
    Ding, C.H., Tzar M.N., Biswas S., Muttaqillah N.A.S., Wahab A.A.
    International Medical Journal Malaysia, 2018;17(2):135-138.
    MyJurnal
    Catheter-related bloodstream infections caused by Kodamaea ohmeri are generally not considered due to the relative scarcity of reported cases. This is a case of an 85-year-old man with poorly controlled diabetes mellitus who was initially admitted to our hospital for diabetic ketoacidosis. An internal jugular catheter was inserted as part of the initial management. A week later the patient developed a temperature spike and a yeast identified as Kodamaea ohmeri by ID 32 C (bioMérieux, France) was isolated from both his central and peripheral blood cultures. The catheter was removed and the patient was treated with fluconazole despite the organism’s relatively high minimum inhibitory concentration (2 μg/mL) to this antifungal. The fungemia resolved following a 2-weeks course of fluconazole.
    Matched MeSH terms: Fluconazole
  3. Fulltext A fatal case of rhinocerebral mucormycosis
    Nurul Suhaili Kamarudin, Rosni Ibrahim, Nur Hanani Ahmad, Siti Norbaya Masri
    Malaysian Journal of Medicine and Health Sciences, 2020;16(2):329-331.
    MyJurnal
    Rhinocerebral mucormycosis is a potentially fatal and progressive angioinvasive fungal infection. It is classically described in patients with uncontrolled diabetes mellitus and hematological malignancies. This report describes a case of progressive rhinocerebral mucormycosis in a patient with poorly controlled diabetes who was on prolonged prednisolone therapy for autoimmune kidney disease. The patient, who was a female, presented to hospital with headache, orbital pain and nasal bridge swelling. Black eschar on nasal mucosae was present on admission. Later, she was started on intravenous fluconazole for the diagnosis of fungal sinusitis. Subsequently, she developed intra- cerebral haemorrhage complicated with transtentorial herniation. Diagnosis of rhinocerebral mucormycosis was later observed by a laboratory finding and the treatment was changed to intravenous amphotericin B. However, the patient succumbed to her illness on the 6th day of hospitalisation. This report discusses the risk factors associated with rhinocerebral mucormycosis as well as the underlying pathogenesis. This report will also highlight the importance of early diagnosis and appropriate treatment for mucormycosis to improve prognosis in patients.
    Matched MeSH terms: Fluconazole
  4. Fulltext An unusual cause of haemoptysis and headache: cryptococcosis
    How SH, Kuan YC, Ng TH, Ramachandram K, Fauzi AR
    Malays J Pathol, 2008 Dec;30(2):129-32.
    PMID: 19291924 MyJurnal
    Pulmonary cryptococcosis can be clinically silent in non-HIV infected patients but can also present as nodules and masses on the chest radiograph, which can be mistaken for tuberculosis or lung cancer. Common symptoms include fever and cough, and uncommonly haemoptysis. This report illustrates a non-HIV infected patient whose main complaint was haemoptysis and headache. He was diagnosed with pulmonary cryptococcosis from biopsy of an endobronchial mass found on flexible bronchoscopy. Disseminated cryptoccoccal infection should be considered as a differential diagnosis in non-HIV infected patients presenting with haemoptysis and headache. Early recognition and administration of appropriate therapy will improve clinical outcome in these patients.
    Matched MeSH terms: Fluconazole/therapeutic use
  5. Anti-Candida albicans biofilm activity by Cassia spectabilis standardized methanol extract: an ultrastructural study
    Torey A, Sasidharan S
    Eur Rev Med Pharmacol Sci, 2011 Aug;15(8):875-82.
    PMID: 21845797
    Candida (C.) albicans infection in its biofilm mode of growth has taken centre point with the increasing recognition of its role in human infections due to the development of resistance to the commonly used antibiotic or phenotypic adaptation within the biofilm. Hence, in this study the inhibitory effect of methanol extract of Cassia (C.) spectabilis leaves was evaluated against biofilm forming C. albicans.
    Matched MeSH terms: Fluconazole/pharmacology
  6. Antifungal agents in preventing oral candidiasis in clinical oncology: A network meta-analysis
    Shen Loo Y, Yee Wong T, Veettil SK, Se Wong P, Gopinath D, Mooi Ching S, et al.
    Oral Dis, 2021 Oct;27(7):1631-1643.
    PMID: 32762108 DOI: 10.1111/odi.13588
    OBJECTIVE: This review examined the comparative efficacy and safety of antifungal agents in preventing oral candidiasis among patients on cancer treatment.

    METHODS: We performed a systematic review and network meta-analysis based on randomised controlled trials that compared antifungal agents to placebo or other antifungal agents used in patients undergoing cancer treatment. Relative ranking of antifungal agents was evaluated with surface under the cumulative ranking (SUCRA) probability score. A total of 20 randomised controlled trials (3,215 participants) comparing 11 interventions were included.

    RESULTS: Compared with placebo, clotrimazole was ranked the best agent for preventing the incidence of oral candidiasis (risk ratio (RR), 0.21 [95% CI 0.08 to 0.55]; SUCRA = 0.89). Fluconazole was ranked the safest among other antifungal agents (SUCRA = 0.80), whereas clotrimazole (SUCRA = 0.36) and amphotericin B (SUCRA = 0.18) were ranked low for safety. Amphotericin B was associated with highest risk of adverse events (RR, 3.52 [95% CI 1.27 to 9.75]).

    CONCLUSION: Clotrimazole is the most effective in preventing oral candidiasis, whereas fluconazole has the most favourable risk-benefit profile in patients undergoing cancer treatment. However, we are unable to recommend clotrimazole as the best choice to prevent oral candidiasis due to unavailability of studies comparing clotrimazole with other antifungal agents.

    Matched MeSH terms: Fluconazole/therapeutic use
  7. Fulltext Biofilm architecture of Candida rugosa and effect of amphotericin b, caspofungin, fluconazole and voriconazole on its structure
    Sri Raja Rajeswari Mahalingam, Priya Madhavan, Chong, Pei Pei
    Malaysian Journal of Medicine and Health Sciences, 2019;15(102):2-2.
    MyJurnal
    Introduction: One of the most common aetiology of opportunistic fungal infections in humans is Candida species. The virulence of Candida species is due to repertoire of factors, specifically, the ability to form biofilms. Medical devices such as intravenous catheters, prosthetic heart valves and surgical interventions provide pathogenic microorganisms with a surface to adhere to form biofilm. Fungi present as biofilms are often resistant to antifungal treatment because these biofilms offer a protective barrier that prohibits the drugs to get to the active site of the fungi. The objective of this study is to investigate the biofilm architecture of Candida rugosa (C.rugosa) at different developmental phases and to identify Sessile Minimum Inhibition Concentrations (SMICs) of amphotericin B, caspofungin, fluconazole, and voriconazole for the biofilm of C. rugosa. Methods: Confocal scanning laser microscopy (CSLM) and scanning electron microscopy (SEM) were used to visualize C. rugosa biofilms at different developmental phases. The antifungal susceptibility test was performed using serial doubling dilution. The growth kinetics of Candida biofilms was quantified using XTT reduction assay and crystal violet assay. Results: From the antifungal susceptibility test, the biofilms had SMIC of >16μg/mL for amphotericin B, 6µg/mL for caspofungin, >64μg/mL for fluconazole and >16μg/ mL for voriconazole. From the SEM micrographs, C. rugosa biofilm have a structure composed of an adherent yeast cells and blastopores with hyphal elements. There were significant alterations in the morphology after exposure to antifungal agents. The quantitative measurement of the matrix thickness of embedded yeast cells were obtained from CLSM micrographs. Conclusion: In conclusion, the ability of C. rugosa to form biofilms may attribute to one of the virulence factors that causes reduced susceptibility to antifungal agents.
    Matched MeSH terms: Fluconazole
  8. Brain-Eating Amoebae: Silver Nanoparticle Conjugation Enhanced Efficacy of Anti-Amoebic Drugs against Naegleria fowleri
    Rajendran K, Anwar A, Khan NA, Siddiqui R
    ACS Chem Neurosci, 2017 12 20;8(12):2626-2630.
    PMID: 29206032 DOI: 10.1021/acschemneuro.7b00430
    The overall aim of this study was to determine whether conjugation with silver nanoparticles enhances effects of available drugs against primary amoebic meningoencephalitis due to Naegleria fowleri. Amphotericin B, Nystatin, and Fluconazole were conjugated with silver nanoparticles, and synthesis was confirmed using UV-visible spectrophotometry. Atomic force microscopy determined their size in range of 20-100 nm. To determine amoebicidal effects, N. fowleri were incubated with drugs-conjugated silver nanoparticles, silver nanoparticles alone, and drugs alone. The findings revealed that silver nanoparticles conjugation significantly enhanced antiamoebic effects of Nystatin and Amphotericin B but not Fluconazole at micromolar concentrations, compared with the drugs alone. For the first time, our findings showed that silver nanoparticle conjugation enhances efficacy of antiamoebic drugs against N. fowleri. Given the rarity of the disease and challenges in developing new drugs, it is hoped that modifying existing drugs to enhance their antiamoebic effects is a useful avenue that holds promise in improving the treatment of brain-eating amoebae infection due to N. fowleri.
    Matched MeSH terms: Fluconazole/administration & dosage
  9. Fulltext Bruton's agammaglobulinaemia in a child presenting with cryptococcal empyema thoracis and periauricular pyogenic abscess
    Wahab JA, Hanifah MJ, Choo KE
    Singapore Med J, 1995 Dec;36(6):686-9.
    PMID: 8781652
    We describe here a case of cryptococcal empyema thoracis and periauricular pyogenic abscess in a child with Bruton's agammaglobulinaemia. The cryptococcal empyema thoracis was treated with intravenous amphotericin B and intravenous fluconazole for six weeks followed by oral fluconazole. The pyogenic periauricular abscess was surgically drained and treated with intravenous ceftazidime and cloxacillin for two weeks. He also received monthly intravenous immunoglobulin.
    Matched MeSH terms: Fluconazole/administration & dosage
  10. Fulltext Candida albicans infection of a prosthetic knee replacement: a case report
    Badrul B, Ruslan G
    Med J Malaysia, 2000 Sep;55 Suppl C:93-6.
    PMID: 11200051
    We report a 64 year old man who developed Candida albicans infection following total knee arthroplasty. A two-stage exchange arthroplasty was performed after an initial swab culture grew Acinobacter sp. A scanty growth of yeast was also found from the tissue culture. Intravenous cefuroxime was instituted for six weeks followed by reimplantation four months after the removal. Three weeks after that revision, the prosthesis became infected and a culture of knee aspirate established the diagnosis of Candida albicans infection. Treatment consisted of thorough debridement of the involved joint and oral fluconazole for a year. Infection was never totally resolved and a secondary infection with methicillin resistant staphylococcus aureus then developed. Excision arthroplasty was done at two and a half years after the initial infection. At five years follow-up the infection was quiescent and he had a range of movement of 30 degrees to 70 degrees. Knee brace was used to control the valgus-varus stability.
    Matched MeSH terms: Fluconazole/therapeutic use
  11. Combination Therapy of Clinically Approved Antifungal Drugs Is Enhanced by Conjugation with Silver Nanoparticles
    Hussain MA, Ahmed D, Anwar A, Perveen S, Ahmed S, Anis I, et al.
    Int Microbiol, 2019 Jun;22(2):239-246.
    PMID: 30810990 DOI: 10.1007/s10123-018-00043-3
    Silver nanoparticles (SN) have been recently developed as a new class of antimicrobial agents against numerous pathogenic microorganisms. SN have also been used as efficient drug delivery systems and have been linked with increasing drug potency. Here, we demonstrated the enhanced antifungal efficacy of nystatin (NYT) and fluconazole (FLU) after conjugation with SN. The antifungal bioactivity of NYT- and FLU-coated SN was evaluated against Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404 by the agar tube dilution method. The aim of this study was to determine and compare the antifungal efficacy of NYT and FLU with their SN and, finally, the combination of both nanoparticles as NYT-SN + FLU-SN against pathogenic fungi. The results indicated that all test samples showed a dose-dependent response against tested fungi. SN significantly enhanced the antifungal effects of NYT and FLU as compared to drugs alone. We observed a remarkable increase in the percent inhibition of both fungi (90-100%) when treated with a combination of both nanoparticles NYT-SN + FLU-SN at 200 μg/mL only. Furthermore, the morphological modifications occurred at the surface of fungal species were also analyzed by atomic force microscopy (AFM) and scanning electron microscopy (SEM). While tested against primary human cell line, all SN showed negligible cytotoxicity. Hence, these results suggest that the combination of SN with NYT and FLU may have clinical implications in the treatment of fungal infections. However, in vivo studies are needed before recommending the use of these nanoparticles safely in clinical situations.
    Matched MeSH terms: Fluconazole/pharmacology*
  12. Comparative Study of the Effects of Fluconazole and Voriconazole on Candida glabrata, Candida parapsilosis and Candida rugosa Biofilms
    Madhavan P, Jamal F, Pei CP, Othman F, Karunanidhi A, Ng KP
    Mycopathologia, 2018 Jun;183(3):499-511.
    PMID: 29380188 DOI: 10.1007/s11046-018-0243-z
    Infections by non-albicans Candida species are a life-threatening condition, and formation of biofilms can lead to treatment failure in a clinical setting. This study was aimed to demonstrate the in vitro antibiofilm activity of fluconazole (FLU) and voriconazole (VOR) against C. glabrata, C. parapsilosis and C. rugosa with diverse antifungal susceptibilities to FLU and VOR. The antibiofilm activities of FLU and VOR in the form of suspension as well as pre-coatings were assessed by XTT [2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] reduction assay. Morphological and intracellular changes exerted by the antifungal drugs on Candida cells were examined by scanning electron microscope (SEM) and transmission electron microscope (TEM). The results of the antibiofilm activities showed that FLU drug suspension was capable of killing C. parapsilosis and C. rugosa at minimum inhibitory concentrations (MICs) of 4× MIC FLU and 256× MIC FLU, respectively. While VOR MICs ranging from 2× to 32× were capable of killing the biofilms of all Candida spp tested. The antibiofilm activities of pre-coated FLU were able to kill the biofilms at ¼× MIC FLU and ½× MIC FLU for C. parapsilosis and C. rugosa strains, respectively. While pre-coated VOR was able to kill the biofilms, all three Candida sp at ½× MIC VOR. SEM and TEM examinations showed that FLU and VOR treatments exerted significant impact on Candida cell with various degrees of morphological changes. In conclusion, a fourfold reduction in MIC50 of FLU and VOR towards ATCC strains of C. glabrata, C. rugosa and C. rugosa clinical strain was observed in this study.
    Matched MeSH terms: Fluconazole/pharmacology*
  13. Fulltext Comparison between efficacy of allicin and fluconazole against Candida albicans in vitro and in a systemic candidiasis mouse model
    Khodavandi A, Alizadeh F, Harmal NS, Sidik SM, Othman F, Sekawi Z, et al.
    FEMS Microbiol Lett, 2011 Feb;315(2):87-93.
    PMID: 21204918 DOI: 10.1111/j.1574-6968.2010.02170.x
    The efficacy of allicin compared with fluconazole in alleviating systemic Candida albicans infections was evaluated both in vitro and in vivo through a systemic candidiasis mouse model. Determination of in vitro minimum inhibitory concentrations (MICs) for different C. albicans isolates revealed that both allicin and fluconazole showed different MICs that ranged from 0.05 to 12.5 μg mL(-1) and 0.25 to 16 μg mL(-1) , respectively. A time-kill study showed a significant effect of allicin (P<0.01) against C. albicans, comparable to that of fluconazole. Scanning electron microscopy observation revealed that, similar to fluconazole, allicin produced structural destruction of C. albicans cell surface at low MIC and lysis or puncture at high MIC concentrations. Treatment of BALB/c mice systemically infected with C. albicans showed that although the allicin treatment (at 5 mg kg(-1) day(-1) ) was slightly less efficacious than fluconazole treatment in terms of the fungal load reduction and host survival time, it was still effective against C. albicans in terms of mean survival time, which increased from 8.4 to 15.8 days. These results demonstrate the efficacy of anticandidal effects of allicin both in vitro and in an animal model of candidiasis and affirm the potential of allicin as an adjuvant therapy to fluconazole.
    Matched MeSH terms: Fluconazole/pharmacology*; Fluconazole/therapeutic use*
  14. Cost-effectiveness analysis of anidulafungin vs fluconazole for the treatment of invasive candidiasis (IC) in Turkey
    Neoh CF, Senol E, Kara A, Dinleyici EC, Turner SJ, Kong DCM
    Mycoses, 2017 Nov;60(11):714-722.
    PMID: 28699297 DOI: 10.1111/myc.12651
    Anidulafungin has been shown to be non-inferior to, and possibly more efficacious, than fluconazole in treating patients with invasive candidiasis (IC). This study aimed to determine the cost-effectiveness of anidulafungin vs fluconazole for treatment of IC in the Turkish setting. A decision analytic model was constructed to depict downstream economic consequences of using anidulafungin or fluconazole for treatment of IC in the Turkish hospitals. Transition probabilities (ie treatment success, observed or indeterminate treatment failures) were obtained from a published randomised clinical trial. Cost inputs were from the latest Turkish resources. Data not available in the literature were estimated by expert panels. Sensitivity analyses were performed to assess the robustness of the model outcome. While anidulafungin [TL 17 171 (USD 4589)] incurred a higher total cost than fluconazole [TL 8233 (USD 2200) per treated patient, treatment with anidulafungin was estimated to save an additional 0.58 life-years, with an incremental cost-effectiveness ratio of TL 15 410 (USD 4118) per life-years saved. Drug acquisition cost and hospitalisation were the main cost drivers for anidulafungin and fluconazole arms respectively. The model findings were robust over a wide range of input variables except for anidulafungin drug cost. Anidulafungin appears to be a cost-effective therapy in treating IC from the Turkish hospital perspective.
    Matched MeSH terms: Fluconazole/economics; Fluconazole/therapeutic use*
  15. Fulltext Cryptococcal Meningitis in an immunocompetent Swiftlet Rancher – first reported case
    Tan, Sin Nee, Lim, Thiam Seong Christopher
    Malaysian Journal of Medicine and Health Sciences, 2019;15(1):82-84.
    MyJurnal
    Cryptococcal meningitis is a central nervous system infection cause by Cryptococcus neoformans. Although Cryptococcus is found in bird droppings, it has never been reported for those ranchers involved in the niche swiftlet ranching industry despite having close proximity with the bird droppings. We present here a case of a 41-year-old healthy swiftlet rancher who presents with a history of prolonged fever, headache and altered behaviour of a month duration. Cerebral spinal fluid analysis revealed the presence of Cryptococcus. He was treated with intravenous amphotericin B and flucytosine and discharged well with fluconazole consolidation therapy for 8 weeks, followed by maintenance therapy for 1 year. We believe this is the first reported case of Cryptococcal meningitis (CM) occurring in an immunocompetent swiftlet rancher. This case should highlight the needs to wear a proper personal protective equipment inside a swiftlet ranch due to the constant exposure to the potential cryptococcal-rich environment. A high index of suspicion, careful history taking and physical examination focusing on neurologic assessment is key to early diagnosis and timely management of CM.
    Matched MeSH terms: Fluconazole
  16. Fulltext Cryptococcal meningitis in an immunocompetent child: a case report and literature review
    Othman N, Abdullah NA, Wahab ZA
    Southeast Asian J. Trop. Med. Public Health, 2004 Dec;35(4):930-4.
    PMID: 15916093
    An immunocompetent 5 year-old girl presented with pyrexia of unknown origin associated with headache. Initial investigations showed leukocytosis and an increased erythrocyte sedimentation rate. A Widal-Weil Felix test, blood film for malarial parasites, mycoplasma IgM antibody, cultures from blood and urine, full blood picture, Mantoux test, and chest x-ray were all negative. A lumbar puncture was done as part of a work-up for pyrexia of unknown origin. Cryptococcus neoformans was seen on India ink examination and confirmed on culture. She was treated with 10 weeks of intravenous amphotericin B and 8 weeks of fluconazole. Further immunological tests did not reveal any defect in the cell-mediated immune system. C. neoformans meningitis may present with non-specific symptoms and should be considered in a work-up for pyrexia of unknown origin.
    Matched MeSH terms: Fluconazole/therapeutic use
  17. Cryptococcus humicolus meningitis: first case report in Malaysia
    Ramli SR, Leong MC, Khaithir TM, Aziz MN, Loons LC, Rafia MH
    Southeast Asian J. Trop. Med. Public Health, 2012 Sep;43(5):1212-7.
    PMID: 23431829
    We report a case of Cryptococcus humicolus meningitis complicated by communicating hydrocephalus in an apparently immunocompetent 49-year-old psychiatric patient from a nursing home. He presented with a history of poor oral intake, weight loss, headache, vomiting, blurred vision, frequent falls and unsteady gait for the previous three months. He had a history of chronic cough, productive of whitish sputum for the previous month but no hemoptysis. Cerebrospinal fluid culture was positive for Cryptococcus humicolus. He was treated with intravenous amphotericin B and oral fluconazole and had clinical and microbiological improvement after three weeks of treatment. Unfortunately, the patient acquired nosocomial methicillin-resistant Staphylococcus aureus infection and died due to overwhelming sepsis.
    Matched MeSH terms: Fluconazole/therapeutic use
  18. Fulltext Design, synthesis and therapeutic potential of 3-(2-(1H-benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamide analogues
    Tahlan S, Ramasamy K, Lim SM, Shah SAA, Mani V, Narasimhan B
    Chem Cent J, 2018 Dec 19;12(1):139.
    PMID: 30569392 DOI: 10.1186/s13065-018-0513-3
    BACKGROUND: The emergence of bacterial resistance is a major public health problem. It is essential to develop and synthesize new therapeutic agents with better activity. The mode of actions of certain newly developed antimicrobial agents, however, exhibited very limited effect in treating life threatening systemic infections. Therefore, the advancement of multi-potent and efficient antimicrobial agents is crucial to overcome the increased multi-drug resistance of bacteria and fungi. Cancer, which remains as one of the primary causes of deaths and is commonly treated by chemotherapeutic agents, is also in need of novel and efficacious agents to treat resistant cases. As such, a sequence of novel substituted benzamides was designed, synthesized and evaluated for their antimicrobial and anticancer activities.

    METHODOLOGY: All synthesized compounds were characterized by IR, NMR, Mass and elemental analysis followed by in vitro antimicrobial studies against Gram-positive (Staphylococcus aureus), Gram-negative (Salmonella typhi and Klebsiella pneumoniae) bacterial and fungal (Candida albicans and Aspergillus niger) strains by the tube dilution method. The in vitro anticancer evaluation was carried out against the human colorectal carcinoma cell line (HCT116), using the Sulforhodamine B assay.

    RESULTS, DISCUSSION AND CONCLUSION: Compound W6 (MICsa, st, kp = 5.19 µM) emerged as a significant antibacterial agent against all tested bacterial strains i.e. Gram-positive (S. aureus), Gram-negative (S. typhi, K. pneumoniae) while compound W1 (MICca, an = 5.08 µM) was most potent against fungal strains (A. niger and C. albicans) and comparable to fluconazole (MIC = 8.16 µM). The anticancer screening demonstrated that compound W17 (IC50 = 4.12 µM) was most potent amongst the synthesized  compounds and also more potent than the standard drug 5-FU (IC50 = 7.69 µM).

    Matched MeSH terms: Fluconazole
  19. Fulltext Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives
    Kumar S, Lim SM, Ramasamy K, Mani V, Shah SAA, Narasimhan B
    Chem Cent J, 2018 Jun 25;12(1):73.
    PMID: 29938365 DOI: 10.1186/s13065-018-0440-3
    BACKGROUND: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies.

    RESULTS: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay.

    CONCLUSIONS: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line.

    Matched MeSH terms: Fluconazole
  20. Fulltext Disseminated histoplasmosis in a non-immunocompromised child
    Hasliza M, Nur Atiqah NA, Lim CB, Hussain IH
    Med J Malaysia, 1999 Mar;54(1):120-4.
    PMID: 10972016
    We describe a 2 year-old non-immunocompromised girl with disseminated histoplasmosis who presented with a 2-month history of fever and bloody diarrhoea. On presentation, she was severely wasted and anaemic. There were gross hepatosplenomegaly and multiple lymphadenopathy. A septic screen was negative. A subsequent stool culture isolated Salmonella enteriditis. Serial Widal-Weil Felix (WWF) titres showed serological response after 2 weeks of Ceftriaxone. However, she continued to have spiking fever, bloody diarrhoea and weight loss. She developed pancytopaenia and disseminated intravascular coagulation. A bone marrow aspirate and trephine, and lymph node biopsy showed the presence of Histoplasma capsulatum, confirmed by Gomori-Methenamine Silver staining. She responded to intravenous amphotericin B followed by fluconazole (intravenous then oral) for 6 months after discharge. Human Immunodeficiency Virus screening tests were negative. Complement and immunoglobulin levels were normal. T and B enumeration tests showed gross leucopaenia with very low T cell function with defective phagocytic function. A repeat T and B cell enumeration test and phagocytic function tests done 3 months later were normal.
    Matched MeSH terms: Fluconazole/therapeutic use
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