sulfonamides-part-1
... The distinction is variable, with some drugs being cidal for some microorganisms and static for others: Macrolides: static against atypicals and GNR, cidal against S. pyogenes and S. pneumoniae. ...
... The distinction is variable, with some drugs being cidal for some microorganisms and static for others: Macrolides: static against atypicals and GNR, cidal against S. pyogenes and S. pneumoniae. ...
Department of Pharmacology
... aspirin, acetaminophen and other NSAIDs. Drugs used in acute attack of gouty arthritis (colchicine, NSAIDs, glucocorticoids). Drugs used in chronic therapy of hyperuricemia: uricosurics (probenecid, sulphinpyrazone) and inhibitors of uric acid synthesis (allopurinol, febuxostat) - mechanism of actio ...
... aspirin, acetaminophen and other NSAIDs. Drugs used in acute attack of gouty arthritis (colchicine, NSAIDs, glucocorticoids). Drugs used in chronic therapy of hyperuricemia: uricosurics (probenecid, sulphinpyrazone) and inhibitors of uric acid synthesis (allopurinol, febuxostat) - mechanism of actio ...
Project 1 Pradimicine Derivates as new Antiviral Drug Leads
... our existing collaboration (isolation of marine natural products) with the CAS in Marine Biology (Annamalai University, south east India). Samples from this region have only been sparsely studied so far. We envision to collect samples (e.g. soil, wood, mud; collection will be performed during a visi ...
... our existing collaboration (isolation of marine natural products) with the CAS in Marine Biology (Annamalai University, south east India). Samples from this region have only been sparsely studied so far. We envision to collect samples (e.g. soil, wood, mud; collection will be performed during a visi ...
Pharmacotherapy of drug poisoning and emergency states Common
... • Facilitated diffusion – with the help of proteins-transporters: glucose, aminoacids, vitamins (specific gastromucoprotein synthesized in stomach is necessary for absorption of vitamin В12 in small intestine) • Filtration – through pores in membrane, the size of which is around 0,35-0,8 nm. Substan ...
... • Facilitated diffusion – with the help of proteins-transporters: glucose, aminoacids, vitamins (specific gastromucoprotein synthesized in stomach is necessary for absorption of vitamin В12 in small intestine) • Filtration – through pores in membrane, the size of which is around 0,35-0,8 nm. Substan ...
Transformation of Peptides into Non-Peptides
... novel inhibitor structure in that the core portion of the inhibitor lacks nitrogen. At the time we began this work, no nonnitrogen-containing tight-binding inhibitors of pepsin were known, and we simplified 8 to produce a series of compounds designed to determine whether GrowMol had produced a reali ...
... novel inhibitor structure in that the core portion of the inhibitor lacks nitrogen. At the time we began this work, no nonnitrogen-containing tight-binding inhibitors of pepsin were known, and we simplified 8 to produce a series of compounds designed to determine whether GrowMol had produced a reali ...
Fragment library screening against the Hepatitis C drug target
... dilutions from 1 mM, were performed in 96-well plates. Eight concentration series were prepared per plate. In addition to three sample plates (holding in total 24 fragment concentration series), a fourth plate with solvent correction and control solutions was included in each run, thereby utilizing ...
... dilutions from 1 mM, were performed in 96-well plates. Eight concentration series were prepared per plate. In addition to three sample plates (holding in total 24 fragment concentration series), a fourth plate with solvent correction and control solutions was included in each run, thereby utilizing ...
Antitubercular Agents
... PZA is thought to enter M. tub. by passive diffusion and converted to pyrazinoic acid (its active metabolite) by bact. pyrazinamidase enz. .This metabolite inhibits mycobact. fatty acid synthase -I enz. and disrupts mycolic acid synthesis needed for cell wall synthesis -Mutation in the gene (pcn A) ...
... PZA is thought to enter M. tub. by passive diffusion and converted to pyrazinoic acid (its active metabolite) by bact. pyrazinamidase enz. .This metabolite inhibits mycobact. fatty acid synthase -I enz. and disrupts mycolic acid synthesis needed for cell wall synthesis -Mutation in the gene (pcn A) ...
DENS 521 8th S - Home - KSU Faculty Member websites
... Nystatin is too toxic for parenteral administration and is only used topically. It is currently available in creams, ointments, suppositories and other forms for application to skin and mucous membranes Nystatin is not absorbed to a significant degree from skin, mucous membranes, or the gastro ...
... Nystatin is too toxic for parenteral administration and is only used topically. It is currently available in creams, ointments, suppositories and other forms for application to skin and mucous membranes Nystatin is not absorbed to a significant degree from skin, mucous membranes, or the gastro ...
IN SILICO QUINAZOLINONES AS NMDA RECEPTOR INHIBITORS FOR ANTICONVULSANT ACTIVITY Research Article
... with test compound or the standard (e.g. Memantine 15mg/kg s.c.) by oral or subcutaneous administration. Controls received the vehicle only. 30 minutes after s.c. or 60 minutes after p.o treatment the animals are injected with subcutaneous dose of 200mg/kg NMDA (Nmethyl-D-aspartate). During the next ...
... with test compound or the standard (e.g. Memantine 15mg/kg s.c.) by oral or subcutaneous administration. Controls received the vehicle only. 30 minutes after s.c. or 60 minutes after p.o treatment the animals are injected with subcutaneous dose of 200mg/kg NMDA (Nmethyl-D-aspartate). During the next ...
Print this article - Research in Pharmaceutical Sciences
... Investigation of the structure-activity relationship around this compound was reported to identify a more potent dual TNF-α/IL-23 inhibitor (19). In July 2010, An3365 now GSK052 (Fig. 12) was developed for treatment of infections caused by Gram-negative bacteria (20). The presence of a boron atom in ...
... Investigation of the structure-activity relationship around this compound was reported to identify a more potent dual TNF-α/IL-23 inhibitor (19). In July 2010, An3365 now GSK052 (Fig. 12) was developed for treatment of infections caused by Gram-negative bacteria (20). The presence of a boron atom in ...
FinMedChem2011
... endogenous cathecolamines epinephrine and norepinephrine. In the central nervous system they modulate a wide variety of physiological functions such as arousal, attention, learning and memory. Historically, the adrenergic receptor family has been divided to α1-adrenoceptors, α2adrenoceptors and β1-a ...
... endogenous cathecolamines epinephrine and norepinephrine. In the central nervous system they modulate a wide variety of physiological functions such as arousal, attention, learning and memory. Historically, the adrenergic receptor family has been divided to α1-adrenoceptors, α2adrenoceptors and β1-a ...
PDF
... It is clear, then, that in the total absence ofcell division, blastoderm expansion can continue, at least for a time. The epiblast cells adopt an alternative strategy, that of increasing the area occupied by each cell. Such areas can be calculated from the number of nuclei within a fixed counting ar ...
... It is clear, then, that in the total absence ofcell division, blastoderm expansion can continue, at least for a time. The epiblast cells adopt an alternative strategy, that of increasing the area occupied by each cell. Such areas can be calculated from the number of nuclei within a fixed counting ar ...
Novel Antimicrobial Agents
... The natural products distamycin and netropsin, which are oligoamides of pyrrole amino acids that bind to the minor groove of DNA, have been known for 50 years to have antibacterial and antiviral activity. Only in the last 10 years, however, have derivatives been obtained with sufficient selectivity ...
... The natural products distamycin and netropsin, which are oligoamides of pyrrole amino acids that bind to the minor groove of DNA, have been known for 50 years to have antibacterial and antiviral activity. Only in the last 10 years, however, have derivatives been obtained with sufficient selectivity ...
Beta-lactams_E
... The oral second-generation cephalosporins are active against beta-lactamase-producing H. influenzae or Moraxella catarrhalis and have been primarily used to treat sinusitis, otitis, or lower respiratory tract infections, in which these organisms have an important role. Because of their activity aga ...
... The oral second-generation cephalosporins are active against beta-lactamase-producing H. influenzae or Moraxella catarrhalis and have been primarily used to treat sinusitis, otitis, or lower respiratory tract infections, in which these organisms have an important role. Because of their activity aga ...
5.2 Mitosis and Cytokinesis
... • Interphase prepares the cell to divide. • During interphase, the DNA is duplicated. Interesting things happen! ...
... • Interphase prepares the cell to divide. • During interphase, the DNA is duplicated. Interesting things happen! ...
Role of Transition metal complexes as potential therapeutic agents
... compound like iron (III)-salophene with selective cytotoxic and ant-proliferative properties have been used in platinum resistant ovarian cancer cells (8).Different strategies have been used to improve efficacy of cis-platin like use of nanotechnology to specify the effect of the drug in the target ...
... compound like iron (III)-salophene with selective cytotoxic and ant-proliferative properties have been used in platinum resistant ovarian cancer cells (8).Different strategies have been used to improve efficacy of cis-platin like use of nanotechnology to specify the effect of the drug in the target ...
alkaloid discovery as natural acetylcholinesterase
... knowledge (Elgorashi and Van Staden, 2004). Alkaloids are important molecules derived from secondary metabolism that can act as rich sources of research in biomedicine and drug discovery area (Lu et al., 2012). Thus, several alkaloids isolated from natural herbs exhibit potential activity against ca ...
... knowledge (Elgorashi and Van Staden, 2004). Alkaloids are important molecules derived from secondary metabolism that can act as rich sources of research in biomedicine and drug discovery area (Lu et al., 2012). Thus, several alkaloids isolated from natural herbs exhibit potential activity against ca ...
HIV treatment
... transcriptase complexed with an inhibitor. Science 256, 1783–1790 (1992). Sarafianos, S. G., Hughes, S. H. & Arnold, E. Designing anti-AIDS drugs targeting the major mechanism of HIV-1 RT resistance to nucleoside analog drugs. Int. J. Biochem. Cell Biol. 36, 1706–1715 (2004). Brik, A. & Wong, C.-H. ...
... transcriptase complexed with an inhibitor. Science 256, 1783–1790 (1992). Sarafianos, S. G., Hughes, S. H. & Arnold, E. Designing anti-AIDS drugs targeting the major mechanism of HIV-1 RT resistance to nucleoside analog drugs. Int. J. Biochem. Cell Biol. 36, 1706–1715 (2004). Brik, A. & Wong, C.-H. ...
Anticancer efficacy and toxicokinetics of a novel paclitaxel-clofazimine nanoparticulate co- formulation
... improved systemic therapies for cancer [4]. Categorically, MDR is classically associated with the overexpression of ATP binding cassette (ABC) transmembrane proteins, particularly ABCB1/MDR1/Pglycoprotein (Pgp). These energy dependent efflux pumps extrude various structurally and mechanistically unr ...
... improved systemic therapies for cancer [4]. Categorically, MDR is classically associated with the overexpression of ATP binding cassette (ABC) transmembrane proteins, particularly ABCB1/MDR1/Pglycoprotein (Pgp). These energy dependent efflux pumps extrude various structurally and mechanistically unr ...
Molecular Basis of Multidrug Transport by ATP
... multidrug transporters is crucial for the development of new drugs which are not transported, and for the development of modulators which may inhibit these proteins through high-affinity binding. Unlike other transporters in the ABC family, each of which is relatively specific for its substrate (e.g ...
... multidrug transporters is crucial for the development of new drugs which are not transported, and for the development of modulators which may inhibit these proteins through high-affinity binding. Unlike other transporters in the ABC family, each of which is relatively specific for its substrate (e.g ...
Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5
... confirmed by its clinical activity.9 Some evidence also exists that the client protein bound to the Hsp90 cochaperone complex is more susceptible to ubiquitination and targeting to the proteasome for degradation.10,11 These data when taken together indicate the potential utility of Hsp90 inhibitors; ...
... confirmed by its clinical activity.9 Some evidence also exists that the client protein bound to the Hsp90 cochaperone complex is more susceptible to ubiquitination and targeting to the proteasome for degradation.10,11 These data when taken together indicate the potential utility of Hsp90 inhibitors; ...
Lecture6_RW
... The dissociation constant is the concentration of ligand [L] at which the binding site on a particular protein is half occupied, i.e. KD is the concentration of ligand, at which the concentration of protein with ligand bound [PL], equals the concentration of protein with no ligand bound [P]. ...
... The dissociation constant is the concentration of ligand [L] at which the binding site on a particular protein is half occupied, i.e. KD is the concentration of ligand, at which the concentration of protein with ligand bound [PL], equals the concentration of protein with no ligand bound [P]. ...
Drugs from nature" past achievements, future prospects
... folklore and traditional medicine. 2~ Of the plant-derived anticancer drugs in clinical use, the best known are the so-called vinca alkaloids, vinblastine and vincristine, which are isolated from the Madagascar periwinkle, Catharanthus roseus. C. roseus was used by various cultures for the treatment ...
... folklore and traditional medicine. 2~ Of the plant-derived anticancer drugs in clinical use, the best known are the so-called vinca alkaloids, vinblastine and vincristine, which are isolated from the Madagascar periwinkle, Catharanthus roseus. C. roseus was used by various cultures for the treatment ...
Drug chirality: Stereoselectivity in the action and disposition
... Equipotency ratio of 1.5:1 of ropivacaine and other two drugs produces similar clinical profile and better motor preservation. Ropivacaine thus produces similar sensory block and less motor blockade as compared to bupivacaine. In obstetric population, ropivacaine produces a better patient sati ...
... Equipotency ratio of 1.5:1 of ropivacaine and other two drugs produces similar clinical profile and better motor preservation. Ropivacaine thus produces similar sensory block and less motor blockade as compared to bupivacaine. In obstetric population, ropivacaine produces a better patient sati ...