Discovery of novel oxindole derivatives as potent α-glucosidase inhibitors

Khan, Momin; Yousaf, Muhammad Junaid; Wadood, Abdul; Junaid, Muhammad; Ashraf, Muhammad; Alam, Umber; Ali, Muhammad; Arshad, Muhammad; Hussain, Zahid; Khan, Khalid Mohammed

doi:10.1016/j.bmc.2014.04.033

Cited by 61 publications

(32 citation statements)

References 19 publications

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“…The longer duration of surgery also seemed to cause more SSIs incidence. The ASA score of 3 or greater than was considered to be a significant risk for SSIs in our study group and this is also shown in other studies like that of Cheng K et al [14], Khan M et al [15] and Wloch C et al [16]. There was no readmission for SSIs in our study however the percentage of readmission for SSIs was 0.6% for women who underwent Caesarian sections in Wloch et al [16].…”

Section: Discussionsupporting

confidence: 86%

Surgical Site Infections Incidence, their Predictors and Causative Organisms in a Teaching Hospital

Rawabdeh¹,

Mulhim²,

Khan³

2016

Int J Community Fam Med

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Purposes: Nosocomial infections (NCIs) are infections that generally occur 48 hours after hospitalization. Surgical site infections (SSIs) are the major contributor to patient morbidity, health care costs and death. The rational for this study was to assess the frequency of NCIs in surgical wards and investigate possible predictors for SSIs. Methods: It was an observational and prospective study for the purpose of providing structured opportunities for Hospital administration and health professionals in countering SSIs. The total number of patients were 1611 including Saudis and non-Saudi nationals. Each patient was followed up from the time of admission until discharge (with a maximum period of 30 days postoperatively). Surgical wounds were inspected at the time of the first dressing and weekly thereafter for 30 days. Also, swabs from a deeper part of the wound were taken from the infected surgical sites, and routinely from the surface of non-infected sites. The specimens were gram stained and examined for the presence of organisms (cultured aerobically and anaerobically). Findings: The main findings were: SSIs causative organisms were Staphylococcus aureus (25% incidence) followed by Echeriashia coli (23% incidence). The incidence rate of surgical site infections was 11.4%. The presences of co-morbidities were a risk factor for SSIs in this study and a higher level of education was related to decreases in SSIs. Recommendations: This article recommended proper nursing care, sterilization and disinfection of instruments and equipment with careful handling of intensive procedures to control infection which will improve the efficiency and quality of surgical care.

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Section: Discussionsupporting

confidence: 86%

Surgical Site Infections Incidence, their Predictors and Causative Organisms in a Teaching Hospital

Rawabdeh¹,

Mulhim²,

Khan³

2016

Int J Community Fam Med

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“…The basic skeletons of known compounds are either luteolin (1,2,4,7,13,14,16,17) or apigenin (3,5,10,11,12). They were elucidated as isoorientin (1), 16 orientin (2), 16 luteolin-7-O-β-glucoside (4), 17,18 5 7-O-β-glucosyl-6''-(E)-p-cinnamate (13), 19 and 4'-O-β-glucoside (16), 18 isoorientin 2''-(E)-p-coumarate (7), 20 3'-O-methylluteolin (14), 21 luteolin (17), 22 isovitexin (3), 23 apigenin 7-O-β-glucoside (cosmosiin) (5), 24 cosmosiin-6''-(E)-p-coumarate (10) 24 and 6''-(Z)-p-coumarate (11), 25 and apigenin (12), 26 respectively, by comparison of their 1 H NMR spectroscopic data (Supplementary data) and MS with those reported in the literatures.…”

Section: Chemistrymentioning

confidence: 99%

“…Other therapeutic potential of such inhibitors includes the diseases related to the cell glycoprotein process such as human immunodeficiency virus (HIV) infection, hepatitis virus infection, and metastatic cancer. 11 Recently, several potent α-glucosidase inhibitors, including derivatives of oxadiazole and thiadiazole, 12 oxindole, 13 biscoumarin, 14 and 2-methoxybenzoylhydrazone, 15 4 have been developed. This study was aimed to disclose new natural α-glucosidase inhibitors from the leaf part of T. crispa.…”

Section: Introductionmentioning

confidence: 99%

“…13 C, and 2D NMR spectra were obtained on Bruker AV-400 or AVIII-600 (dual cryoprobe) NMR spectrometers (Bermen, Germany) (methanol-d4 , δ H 3.30 and δ C 49.0 ppm; CD 3 CN, δ H 1.93 and δ C 118.2 ppm) using standard pulse programs. Mass spectra were recorded on an Esquire 2000 (ESI-MS) and a micrOTOF orthogonal ESI-TOF mass spectrometer (Bruker Daltonics) (HR-ESI-MS).…”

mentioning

confidence: 99%

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Acylated glucosylflavones as α-glucosidase inhibitors from Tinospora crispa leaf

Chang

Lee

2015

Bioorganic & Medicinal Chemistry

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“…α-Glucosidase inhibitors (viz. [11][12][13][14][15][16][17][18][19] Figure 1. 9 They inhibit the membrane bound αglucosidase at the brush border of the small intestine that reduces digestion of starch and other dietary sugars which in turn prevents hyperglycemia and maintains normal blood sugar level.…”

Section: Introductionmentioning

confidence: 99%

Substituted furopyridinediones as novel inhibitors of α-glucosidase

et al. 2015

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The global preponderance of diabetes mellitus has prompted the medical community to opt for various therapeutic solutions to curb the menace. One of the means involved controlling the post prandial hyperglycemia. α-glucosidase inhibitors are known to be excellent agents of controlling postprandial hyperglycemia. Different classes of α-glucosidase inhibitors has been discovered.In this context, a diverse library of substituted furopyridinediones (12a-v) was designed as potential inhibitors of α-glucosidase, using an intuitive scaffold hopping approach (which was further rationalized by molecular docking). They were synthesized in one step via an aldol condensation reaction of furopyridinedione scaffold and appropriate aldehydes. The compounds were screened against α-glucosidase using acarbose as the reference inhibitor. Among the screened compounds, 12p transpired to be the lead candidate with an IC 50 of 0.24 µM.Lineweaver Burke analysis of 12p indicated it to be a mixed inhibitor. X-ray crystallography of 12p further confirmed its structure. Molecular modelling studies and molecular dynamic simulation experiments were performed against a homology model of α-glucosidase to observe the binding interaction of 12p with the enzymes.

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Discovery of novel oxindole derivatives as potent α-glucosidase inhibitors

Cited by 61 publications

References 19 publications

Surgical Site Infections Incidence, their Predictors and Causative Organisms in a Teaching Hospital

Surgical Site Infections Incidence, their Predictors and Causative Organisms in a Teaching Hospital

Acylated glucosylflavones as α-glucosidase inhibitors from Tinospora crispa leaf

Substituted furopyridinediones as novel inhibitors of α-glucosidase

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