Diverse models for anti-HIV activity of purine nucleoside analogs
... neoplastic and autoimmune diseases. In the present study, classification models have been developed for the prediction of the anti-HIV activity of purine nucleoside analogs. Results: The topochemical version of superaugmented pendentic index-4 has been proposed and successfully utilized for the deve ...
... neoplastic and autoimmune diseases. In the present study, classification models have been developed for the prediction of the anti-HIV activity of purine nucleoside analogs. Results: The topochemical version of superaugmented pendentic index-4 has been proposed and successfully utilized for the deve ...
In vitro and in vivo structure and activity relationship analysis of
... polymethoxylated flavones and flavanones have been reported to have promising anticancer and anticarcinogenesis activity, which are frequently associated with excessive angiogenesis, the effect of this subclass of flavonoids on angiogenesis remains unclear. Only two recent studies touched on the ant ...
... polymethoxylated flavones and flavanones have been reported to have promising anticancer and anticarcinogenesis activity, which are frequently associated with excessive angiogenesis, the effect of this subclass of flavonoids on angiogenesis remains unclear. Only two recent studies touched on the ant ...
patrick_ch22_p3
... Substituents which increase the basicity of the pyridine ring are good for activity Promotes the mechanism of activation Methyl substituents at the meta position have an inductive effect Methoxy substituent are more effective at para position than meta position Resonance effect increases electron de ...
... Substituents which increase the basicity of the pyridine ring are good for activity Promotes the mechanism of activation Methyl substituents at the meta position have an inductive effect Methoxy substituent are more effective at para position than meta position Resonance effect increases electron de ...
Inhibition of Serine Amidohydrolases by Complexes of Vanadate
... transfer transition state. Structural analogs of such a transition state might well therefore be effective and novel -lactamase inhibitors. Complexes of vanadate with hydroxamic acids may be able to achieve such a structure. Indeed, mixtures of these two components, but neither one alone, were foun ...
... transfer transition state. Structural analogs of such a transition state might well therefore be effective and novel -lactamase inhibitors. Complexes of vanadate with hydroxamic acids may be able to achieve such a structure. Indeed, mixtures of these two components, but neither one alone, were foun ...
The Role of Intracellular Signaling Pathways in the Pathogenesis of
... including MM, and has received great attention as a molecular target for treatment. In myeloma cells, many genes that are targets of NF-κB are highly expressed, suggesting that myeloma cells are dependent on bone marrow stromal cells, and that extrinsic signaling is important in MM. 24,25 Bone marro ...
... including MM, and has received great attention as a molecular target for treatment. In myeloma cells, many genes that are targets of NF-κB are highly expressed, suggesting that myeloma cells are dependent on bone marrow stromal cells, and that extrinsic signaling is important in MM. 24,25 Bone marro ...
A modular approach to sphingolipid analogs mediated by aziridines: Synthesis
... In the plasma membrane the distribution of lipids is not uniform, particularly, sphingolipids and cholesterol form platforms or rafts that float in the liquid phase.3 Furthermore, these lipid rafts are important in signal transduction processes and some key components of si ...
... In the plasma membrane the distribution of lipids is not uniform, particularly, sphingolipids and cholesterol form platforms or rafts that float in the liquid phase.3 Furthermore, these lipid rafts are important in signal transduction processes and some key components of si ...
Enzyme -3. Factors affecting enzyme activity Lecture NO: 1st MBBS
... the catalytic action of the enzyme in a normal way • Enzyme inhibition interferes with catalysis and slows down or stops the enzymatic reaction ...
... the catalytic action of the enzyme in a normal way • Enzyme inhibition interferes with catalysis and slows down or stops the enzymatic reaction ...
Pharmacologyonline 3: 201-216 (2006) Kumarappan et al. CT
... market. Despite the successes that have been achieved over the years with natural products as a platform for drug discovery has waxed and waned in popularity with various pharmaceutical companies. Natural products today are most likely going to continue to exist and grow to become even more valuable ...
... market. Despite the successes that have been achieved over the years with natural products as a platform for drug discovery has waxed and waned in popularity with various pharmaceutical companies. Natural products today are most likely going to continue to exist and grow to become even more valuable ...
Phytochemistry 24:
... those for GS from other sources [26] except for hydroxylamine. To obtain the K, for ammonia, a method reported by Orr and Haselkorn [27], relying on the form of the time course as ammonia is consumed, was used, giving a K, value of 12.5pM. This was confirmed by the K, value of 13.7pM obtained using ...
... those for GS from other sources [26] except for hydroxylamine. To obtain the K, for ammonia, a method reported by Orr and Haselkorn [27], relying on the form of the time course as ammonia is consumed, was used, giving a K, value of 12.5pM. This was confirmed by the K, value of 13.7pM obtained using ...
PRELIMINARY STUDIES ON GASTRO-PROTECTIVE CHIMERIC DERIVATIVE OF BIPHENYL
... origin followed by renal damage, skin reactions, blood dyscrasias, headaches and nausea2. COX-2 inhibitors decrease incidence of GIT adverse effects, but have significant renal and cardiovascular toxicities. The difficulties limiting use of SAARDs in the long-term treatment are those of side-effects ...
... origin followed by renal damage, skin reactions, blood dyscrasias, headaches and nausea2. COX-2 inhibitors decrease incidence of GIT adverse effects, but have significant renal and cardiovascular toxicities. The difficulties limiting use of SAARDs in the long-term treatment are those of side-effects ...
INVITRO ANTI-INFLAMMATORY ACTIVITY OF METHANOL
... cellular activity of these enzymes are said to be Table 3: Effect of EAME on heat induced haemolysis of erythrocyte Treatment(s ) Concentration (µg/ml) Absorbance at 660nm % inhibition of haemolysis ...
... cellular activity of these enzymes are said to be Table 3: Effect of EAME on heat induced haemolysis of erythrocyte Treatment(s ) Concentration (µg/ml) Absorbance at 660nm % inhibition of haemolysis ...
ANALGESIC AND ANTHELMINTIC ACTIVITY OF VARIOUS EXTRACTS OF ANDROGRAPHIS Research Article
... The extracts of Andrographispaniculata(N)were tested for anthelmintic activity according to method described in detail by Kuppast and Nayak[27]. Pheretimaposthuma (earthworms obtained from Shibpur Botanical Garden, Kolkata) of nearly equal size (6±1 cm) were selected randomly for present study. The ...
... The extracts of Andrographispaniculata(N)were tested for anthelmintic activity according to method described in detail by Kuppast and Nayak[27]. Pheretimaposthuma (earthworms obtained from Shibpur Botanical Garden, Kolkata) of nearly equal size (6±1 cm) were selected randomly for present study. The ...
... form found in older cultures. If the U . urealyticum PPase was similar, activators would have had little effect and thiol inhibitors a large effect on the enzyme activity, since the extract was prepared from cells in the exponential phase of growth. This is consistent with our observations that oxid ...
Invited Review - International Journal of Pharmaceutical Science
... 1.2.1. Antitumor activity Ramla et al [13] synthesized a variety of 1-substituted-2methyl-5-nitrobenzimidazoles and evaluated them for antitumor activity. The anti-tumor effect of compound [1] was found to be significant. Popsavin et al [14] reported a set of 2-(2, 3-anhydrofuranosyl) thiazole-4-car ...
... 1.2.1. Antitumor activity Ramla et al [13] synthesized a variety of 1-substituted-2methyl-5-nitrobenzimidazoles and evaluated them for antitumor activity. The anti-tumor effect of compound [1] was found to be significant. Popsavin et al [14] reported a set of 2-(2, 3-anhydrofuranosyl) thiazole-4-car ...
- International Journal of Advanced Biological and
... to liquorice with concentrations lower than 7.5%, however all tested bacterial strains exhibited susceptibility to high concentration of liquorice (Shirazi et al, 2007). The antibacterial activities of the alcohol, ethyl acetate, acetone and chloroform extracts of 5 plant species were studied by Ate ...
... to liquorice with concentrations lower than 7.5%, however all tested bacterial strains exhibited susceptibility to high concentration of liquorice (Shirazi et al, 2007). The antibacterial activities of the alcohol, ethyl acetate, acetone and chloroform extracts of 5 plant species were studied by Ate ...
Human Immunodeficiency Virus-Reverse Transcriptase and
... HIV-RT inhibition activity of fullerene derivatives is listed in Table 1. All examined fullerene derivatives were effective than non-nucleoside analog of HIV-RT inhibitor, nevirapine (IC50 23 µM).6 Especially, the amino acid type fullerene derivative, 5, strongly inhibited HIVRT. Recently, Bosi et a ...
... HIV-RT inhibition activity of fullerene derivatives is listed in Table 1. All examined fullerene derivatives were effective than non-nucleoside analog of HIV-RT inhibitor, nevirapine (IC50 23 µM).6 Especially, the amino acid type fullerene derivative, 5, strongly inhibited HIVRT. Recently, Bosi et a ...
Drug exposure and EEG/qEEG findings
... MAO Inhibitors: These medications have a wider variation of response than the other antidepressants. Isocarboxazide increases 30-20 Hz and decreases slower and higher frequencies, similar to a stimulant profile. Nialamide and Tranylcypromine produce a more typical profile, though with more variabili ...
... MAO Inhibitors: These medications have a wider variation of response than the other antidepressants. Isocarboxazide increases 30-20 Hz and decreases slower and higher frequencies, similar to a stimulant profile. Nialamide and Tranylcypromine produce a more typical profile, though with more variabili ...
enzymes-inhibition-text
... Reversible enzyme inhibition: enzyme activity can be recovered by removing the inhibitor (e.g. dialysis, gel filtration); ...
... Reversible enzyme inhibition: enzyme activity can be recovered by removing the inhibitor (e.g. dialysis, gel filtration); ...
Modulation of the immune system by Boswellia serrata extracts and
... been shown by Syrovets et al. (2005) that acetyl-␣-BA and AKBA inhibited the generation of TNF-␣ in concentrations between 1 and 10 M in lipopolysaccharide-stimulated human monocytes. AKBA was found to be the most active compound. The effect was mediated by a direct inhibitory action on IK B␣ kinas ...
... been shown by Syrovets et al. (2005) that acetyl-␣-BA and AKBA inhibited the generation of TNF-␣ in concentrations between 1 and 10 M in lipopolysaccharide-stimulated human monocytes. AKBA was found to be the most active compound. The effect was mediated by a direct inhibitory action on IK B␣ kinas ...
NOVEL FAK-SELECTIVE INHIBITORS
... FAK is a non-receptor tyrosine kinase which is overexpressed (through either gene amplification or increased levels of protein expression), or over-activated in many human cancers (including solid tumours and acute myelogenous leukaemia (AML)). Increased levels of FAK and/or phosphorylated FAK are o ...
... FAK is a non-receptor tyrosine kinase which is overexpressed (through either gene amplification or increased levels of protein expression), or over-activated in many human cancers (including solid tumours and acute myelogenous leukaemia (AML)). Increased levels of FAK and/or phosphorylated FAK are o ...
analgesic and anti-inflammatory activity of different fractions of
... evaluate the anti-inflammatory activity. Carrageenan-induced rat paw edema model has been commonly used as an experimental animal model for acute inflammation and is believed to be biphasic. The early phase (1-2 h) of the carrageenan model is mainly mediated by histamine, serotonin and increased syn ...
... evaluate the anti-inflammatory activity. Carrageenan-induced rat paw edema model has been commonly used as an experimental animal model for acute inflammation and is believed to be biphasic. The early phase (1-2 h) of the carrageenan model is mainly mediated by histamine, serotonin and increased syn ...
International Journal of Pharmaceutical Sciences and Drug Research 2014; 6(4): 329-333
... for Clinical Laboratory Standards (NCCLS) by gradually adding normal saline to compare their turbidity to McFarland standard of 0.5 which is approximately 1.0 × 106 CFU/ml. Antimicrobial assay – Well diffusion method The modified agar well diffusion method was employed to determine the antibacterial ...
... for Clinical Laboratory Standards (NCCLS) by gradually adding normal saline to compare their turbidity to McFarland standard of 0.5 which is approximately 1.0 × 106 CFU/ml. Antimicrobial assay – Well diffusion method The modified agar well diffusion method was employed to determine the antibacterial ...
Fengyan Jin1*, Wei Li1, Joel G. Turner
... prescribed as a sleeping pill (or tranquilizer) and particularly used as an antiemetic and sedative to ease morning sickness in pregnant women. In 1960, thalidomide was found to cause a severe birth defect known as phocomelia, a name for the flipper-like limbs, and almost immediately withdrawn from ...
... prescribed as a sleeping pill (or tranquilizer) and particularly used as an antiemetic and sedative to ease morning sickness in pregnant women. In 1960, thalidomide was found to cause a severe birth defect known as phocomelia, a name for the flipper-like limbs, and almost immediately withdrawn from ...
B-lactam antibiotics
... this group of antibiotics is derived from its complex structure, which includes in the molecules • Macrocycle lacton ring, • one or more deoxysugars. The lactone rings are usually 14, 15 or 16-membered. ...
... this group of antibiotics is derived from its complex structure, which includes in the molecules • Macrocycle lacton ring, • one or more deoxysugars. The lactone rings are usually 14, 15 or 16-membered. ...
Development of analogs of thalidomide
The development of analogs of thalidomide was precipitated by the discovery of the anti-angiogenic and anti-inflammatory properties of the drug yielding a new way of fighting cancer as well as some inflammatory diseases after it had been banned in 1961. The problems with thalidomide included; teratogenic side effects, high incidence of other adverse reactions, poor solubility in water and poor absorption from the intestines.In 1998 thalidomide was approved by the US Food and Drug Administration (FDA) for use in newly diagnosed multiple myeloma (MM) under strict regulations. This has led to the development of a number of analogs with fewer side effects and increased potency which include; lenalidomide, (currently marketed), pomalidomide and apremilast (currently marketed), all of which are manufactured by Celgene.