Abstract:
:Microbial resistance to the available drugs poses a serious threat in modern medicine. We report the design, synthesis and in vitro antimicrobial evaluation of new functionalized 2,3-dihydrothiazoles and 4-thiazolidinones tagged with sulfisoxazole moiety. Compound 8d was most active against Bacillis subtilis (MIC, 0.007 µg/mL). Moreover, compounds 7c-d and 8c displayed significant activities against B. subtilis and Streptococcus pneumoniae (MIC, 0.03-0.06 µg/mL and 0.06-0.12 µg/mL versus ampicillin 0.24 µg/mL and 0.12 µg/mL; respectively). Compounds 7a and 7c-d were highly potent against Escherichia coli (MIC, 0.49-0.98 µg/mL versus gentamycin 1.95 µg/mL). On the other hand, compounds 7e and 9c were fourfolds more active than amphotericin B against Syncephalastrum racemosum. Molecular docking studies showed that the synthesized compounds could act as inhibitors for the dihydropteroate synthase enzyme (DHPS). This study is a platform for the future design of more potent antimicrobial agents.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Nasr T,Bondock S,Eid Sdoi
10.3109/14756366.2015.1016514subject
Has Abstractpub_date
2016-01-01 00:00:00pages
236-46issue
2eissn
1475-6366issn
1475-6374journal_volume
31pub_type
杂志文章abstract::Two carbonic anhydrase IX (CA IX) inhibitors were radiolabeled with (18)F, and evaluated for imaging CA IX expression. Despite good affinity for CA IX and excellent plasma stability, uptake of both tracers in CA IX-expressing HT-29 tumor xenografts in mice was low. (18)F-FEC accumulated predominately in the liver and ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2013.773994
更新日期:2014-04-01 00:00:00
abstract::Poly(ADP-ribose) polymerase (PARP)-1 inhibitor has been suggested to attenuate the ischemia-reperfusion injury. We investigated the protective effect of the cardioplegia with a PARP-1 inhibitor, 4-hydoxyquinazoline (4-HQ), against myocardial ischemia-reperfusion injury. Isolated rat hearts were perfused on a Langendor...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2011.642373
更新日期:2013-02-01 00:00:00
abstract::In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360701654894
更新日期:2008-08-01 00:00:00
abstract::Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360701626223
更新日期:2008-12-01 00:00:00
abstract::The inhibitory effect of four structurally related flavonoids, apigenin, baicalein, luteolin and quercetin on the matrix metalloproteinase (MMP)-9 and -13 expressions in osteoblasts was investigated. Treatment with IL-1β induced both MMP-9 and -13 mRNA expressions as measured by quantitative real-time PCR. Luteolin an...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2011.587415
更新日期:2012-04-01 00:00:00
abstract::A set of novel quinolone-triazole conjugates (12-31) were synthesized in three steps in good yields starting from 2-phenylquinoline-4-carboxylic acid. All the intermediates, as well as the final 1,2,4-triazolyl quinolines were fully characterized by their detailed spectral analysis utilizing different techniques such ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2016.1190714
更新日期:2016-01-01 00:00:00
abstract::A new series of N-heteroarylsubstituted triazolosulfonamide compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. Compounds (3 a-k) were prepared by propargylation of N-heteroaryl compounds. Compound 5 was obtained from sulfanilamide...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2014.940933
更新日期:2015-06-01 00:00:00
abstract::A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2018.1518957
更新日期:2019-12-01 00:00:00
abstract::Phthalates, used in medical devices (MDs), have been identified as reproductive and developmental toxicants. Their toxicity varies somewhat depending on the specific phthalate and is in part linked to the activation of Peroxisome Proliferating-Activated Receptors (PPARs). So, the use of MDs containing targeted phthala...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2015.1037748
更新日期:2016-01-01 00:00:00
abstract::Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2018.1474211
更新日期:2018-12-01 00:00:00
abstract::Selective PDE3 inhibitors improve cardiac contractility and may be used in congestive heart failure. However, their proarrhythmic potential is the most important side effect. In this research we designed, synthesized and evaluated the potential cardiotonic activity of thirteen PDE3 inhibitors (4-[(4-methyl-2-oxo-1,2-d...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360802448063
更新日期:2009-08-01 00:00:00
abstract::Analogs of pralidoxime, which is a commercial antidote for intoxication from neurotoxic organophosphorus compounds, were designed, synthesized, characterized, and tested as potential inhibitors or reactivators of acetylcholinesterase (AChE) using the Ellman's test, nuclear magnetic resonance, and molecular modeling. T...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2015.1094468
更新日期:2016-12-01 00:00:00
abstract::Cytosine deaminase (CD) from Aspergillus parasiticus, which has half-life of 1.10 h at 37°C, was stabilized by immobilization on calcium alginate beads. The immobilized CD had pH and temperature optimum of 5 and 50°C respectively. The immobilized enzyme also stoichiometrically deaminated Cytosine and 5-fluorocytosine ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2012.724406
更新日期:2013-12-01 00:00:00
abstract::Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous enzymes that catalyze the hydration of CO(2) to bicarbonate and protons. Inhibition of CAs has been clinically exploited for the treatment of various classes of diseases for decades, but investigating new classes of inhibitors continues to be important. We have synt...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2011.639016
更新日期:2013-04-01 00:00:00
abstract::Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor-2 (VEGFR-2), two protein tyrosine kinases, are involved in pathological disorders and the progression of different types of carcinomas. Concomitant inhibition of both tyrosine kinase activities appears to be an attractive target fo...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756360903169485
更新日期:2010-04-01 00:00:00
abstract::A series of N-(5-methyl-isoxazol-3-yl/1,3,4-thiadiazol-2-yl)-4-(3-substitutedphenylureido) benzenesulfonamide derivatives has been designed, synthesized and screened for their in vitro human carbonic anhydrase (hCA; EC 4.2.1.1) inhibition potential. These newly synthesized sulfonamide compounds were assessed against i...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2016.1197221
更新日期:2016-01-01 00:00:00
abstract::Protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase are important targets to treat obesity and diabetes, due to their deep correlation with insulin and leptin signalling, and glucose regulation. The methanol extract of Paulownia tomentosa fruits showed potent inhibition against both enzymes. Purification of this...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2017.1368502
更新日期:2017-12-01 00:00:00
abstract::Continuous efforts to identify sEH inhibitors using activity-guided fractionation have revealed 12 known compounds, 2-13, from Rheum undulatum. Compounds 2-13 and 1, which was obtained from the in-house library, were tested for inhibitory activity against sEH. Compounds 1-9, 11, and 12 were shown to have inhibitory ac...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2016.1189421
更新日期:2016-01-01 00:00:00
abstract::Abstract Twenty-three phenolic compounds were isolated from Dioscorea opposita by bioactivity-guided method and their inhibitory effect against pancreatic lipase was evaluated. A total of 15 isolates reduced lipase activity at IC50 values of less than 50 µM and 3,3',5-trihydroxy-2'-methoxybibenzyl showed the highest i...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2012.742517
更新日期:2014-02-01 00:00:00
abstract::An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2012.737787
更新日期:2013-12-01 00:00:00
abstract::Carbonic anhydrases (CAs) are widespread metalloenzymes in higher vertebrates including humans. A series of phenolic compounds, including guaiacol, 4-methylguaiacol, 4-propylguaiacol, eugenol, isoeugenol, vanillin, syringaldehyde, catechol, 3-methyl catechol, 4-methyl catechol and 3-methoxy catechol were investigated ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2014.956310
更新日期:2015-01-01 00:00:00
abstract::This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibitors. A 69-fold selectivity against MAGL over FAAH was achieved ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2015.1010530
更新日期:2016-01-01 00:00:00
abstract::Nitrofurazone (NF) and its derivative, hydroxymethylnitrofurazone (NFOH), have presented antichagasic activity. NFOH has higher activity and lower mutagenicity. The aim of this work was to assess whether NF and its derivative NFOH would also be inhibitors of cruzain, besides their trypanothione reductase inhibitory ac...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756360902941058
更新日期:2010-02-01 00:00:00
abstract::A novel set of 16 hybrids of bromopyrrole alkaloids with aroyl hydrazone were designed, synthesized and evaluated for antibacterial and antibiofilm activities against methicillin-resistant Staphylococcus aureus (MRSA; ATCC 43866), methicillin-susceptible Staphylococcus aureus (MSSA; ATCC 35556) and Staphylococcus epid...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.3109/14756366.2013.793183
更新日期:2014-06-01 00:00:00
abstract::The current study was designed to assess the inhibitory activity of Broussonetia papyrifera-derived polyphenols against 3-chymotrypsin-like and papain-like coronavirus cysteine proteases. The isolated compounds were broussochalcone B (1), broussochalcone A (2), 4-hydroxyisolonchocarpin (3), papyriflavonol A (4), 3'-(3...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2016.1265519
更新日期:2017-12-01 00:00:00
abstract::The galangal (the rhizome of Alpinia officinarum, Hance) is popular in Asia as a traditional herbal medicine. The present study reports that the galangal extract (GE) can potently inhibit fatty-acid synthase (FAS, E.C.2.3.1.85). The inhibition consists of both reversible inhibition with an IC50 value of 1.73 microg dr...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000118419
更新日期:2003-08-01 00:00:00
abstract::The limited arsenal of synthetic antifungal agents and the emergence of resistant Candida strains have prompted the researchers towards the investigation of naturally occurring compounds or their semisynthetic derivatives in order to propose new innovative hit compounds or new antifungal combinations endowed with redu...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2016.1180596
更新日期:2016-01-01 00:00:00
abstract::The results of extensive quantitative structure-activity relationship (QSAR) analyses on 15 series of cytochrome P450 inhibitors, covering a total of 7 enzymes and 199 compounds, are reported. In general, it is found that lipophilicity represents the most important single factor in describing differences in inhibitory...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360600952183
更新日期:2007-02-01 00:00:00
abstract::In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumar...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2020.1713114
更新日期:2020-12-01 00:00:00
abstract::The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756366.2019.1608198
更新日期:2019-12-01 00:00:00