Recent advancement of triazole derivatives and their biological
... Pharmaceutical chemistry is devoted to the discovery and development of new agents for treating diseases. Inorganic compound continue to be important in therapy, for example as antacids, mineral supplements and radiopharmaceuticals, but organic molecules with increasingly specific pharmacological ac ...
... Pharmaceutical chemistry is devoted to the discovery and development of new agents for treating diseases. Inorganic compound continue to be important in therapy, for example as antacids, mineral supplements and radiopharmaceuticals, but organic molecules with increasingly specific pharmacological ac ...
E. Diuretics
... Reabsorption of Na in the kidney results in the reabsorption of water. It follows that inhibition of Na reabsorption will result in diuresis. Because of this, the term diuretic has come to mean any agent that will inhibit the tubular absorption of sodium. Primary mechanism of most diuretics: direct ...
... Reabsorption of Na in the kidney results in the reabsorption of water. It follows that inhibition of Na reabsorption will result in diuresis. Because of this, the term diuretic has come to mean any agent that will inhibit the tubular absorption of sodium. Primary mechanism of most diuretics: direct ...
Poster
... promote vasodilation and angiogenesis, and act to inhibit systemic antiinflammatory response (1). The enzyme soluble epoxide hydrolase (sEH) breaks down EETs into dihydroxyeicosatrienoic acids (DHETs). A drug-like inhibitor of sEH could maximize the concentration of EETs in the blood and thus have u ...
... promote vasodilation and angiogenesis, and act to inhibit systemic antiinflammatory response (1). The enzyme soluble epoxide hydrolase (sEH) breaks down EETs into dihydroxyeicosatrienoic acids (DHETs). A drug-like inhibitor of sEH could maximize the concentration of EETs in the blood and thus have u ...
The anti-inflammatory and antioxidant activity of
... Full list of author information is available at the end of the article ...
... Full list of author information is available at the end of the article ...
Sebastiania chamaelea Research Article N.YASODAMMA*, K.S.SHANTHI SREE, C.ALEKHYA
... Objective: There is an immense need in the herbal remedies still in the treatment of diarrhea. The juice of the Sebastiania chamealea is used as astringent and used as a remedy for diarrhea by the herbalists. Hence antidiarrhoel activity of leaf extracts was carried out. Methods: Acute toxicity stud ...
... Objective: There is an immense need in the herbal remedies still in the treatment of diarrhea. The juice of the Sebastiania chamealea is used as astringent and used as a remedy for diarrhea by the herbalists. Hence antidiarrhoel activity of leaf extracts was carried out. Methods: Acute toxicity stud ...
Pharmacological Effects of Rutaecarpine, an Alkaloid Isolated from
... can lead to relaxation of vascular smooth muscle. The other candidates are prostaglandin I2 (PGI2) and endothelium-derived hyperpolarizing factor (EDHF). Systematic examination with appropriate antagonists revealed that a cyclooxygenase inhibitor, indomethacin (30 M), or a nonselective K+ channel b ...
... can lead to relaxation of vascular smooth muscle. The other candidates are prostaglandin I2 (PGI2) and endothelium-derived hyperpolarizing factor (EDHF). Systematic examination with appropriate antagonists revealed that a cyclooxygenase inhibitor, indomethacin (30 M), or a nonselective K+ channel b ...
Inhibition by D-Glutamate of Growth and Glutamate
... a potent growth inhibitor for the two Neurospora crassa strains studied, and its inhibition was easily annulled by L-glu or glutamine at 2-5times smaller molar concentrations. Although cell-free preparations showed no glutaminase activity, it is not certain that the glutamine itself, and not some en ...
... a potent growth inhibitor for the two Neurospora crassa strains studied, and its inhibition was easily annulled by L-glu or glutamine at 2-5times smaller molar concentrations. Although cell-free preparations showed no glutaminase activity, it is not certain that the glutamine itself, and not some en ...
Inhibition by D-Glutamate of Growth and Glutamate
... a potent growth inhibitor for the two Neurospora crassa strains studied, and its inhibition was easily annulled by L-glu or glutamine at 2-5times smaller molar concentrations. Although cell-free preparations showed no glutaminase activity, it is not certain that the glutamine itself, and not some en ...
... a potent growth inhibitor for the two Neurospora crassa strains studied, and its inhibition was easily annulled by L-glu or glutamine at 2-5times smaller molar concentrations. Although cell-free preparations showed no glutaminase activity, it is not certain that the glutamine itself, and not some en ...
Peptidomimetic building blocks for drug discovery: An overview
... sequence. It has been shown that a tilted amide exists in the ground state of the structure by X-ray diffraction and 13C-NMR investigation. Recently, several groups reported that aziridine-containing peptides were effective cysteine protease inhibitors.* The following compounds (Scheme 5) have been ...
... sequence. It has been shown that a tilted amide exists in the ground state of the structure by X-ray diffraction and 13C-NMR investigation. Recently, several groups reported that aziridine-containing peptides were effective cysteine protease inhibitors.* The following compounds (Scheme 5) have been ...
L-ASPG86 - Journal of Microbiology and Biotechnology
... enzymatic activity at 40ºC, and similar activity was detected at 37ºC (Fig. 5A). Its activity decreased gradually from 50ºC. In the optimum pH assay, the highest activity was observed at pH 9, and more than 60% of the relative activity was retained within the pH range of 7-10, as shown in Fig. 5B. T ...
... enzymatic activity at 40ºC, and similar activity was detected at 37ºC (Fig. 5A). Its activity decreased gradually from 50ºC. In the optimum pH assay, the highest activity was observed at pH 9, and more than 60% of the relative activity was retained within the pH range of 7-10, as shown in Fig. 5B. T ...
Characteristics of Sophorolipid as an Antimicrobial Agent
... Toxicity or irritation of skin is an important property when looking at cosmetic ingredients. If the sophorolipid is to be used in a body cleanser, such as a shampoo, toxicity and skin compatibility should be evaluated. We have tested sophorolipid toxicity on 40 rats and 6 rabbits as test animals. W ...
... Toxicity or irritation of skin is an important property when looking at cosmetic ingredients. If the sophorolipid is to be used in a body cleanser, such as a shampoo, toxicity and skin compatibility should be evaluated. We have tested sophorolipid toxicity on 40 rats and 6 rabbits as test animals. W ...
The Influence of Conformational Isomerism on Drug
... Consider the following hypothetical example. Assume a drug contains two functional groups, X and Y, which are located on adjacent carbon atoms and which are essential for biological activity. Further assume that the drug is capable of binding to three different receptor types or subtypes. Given this ...
... Consider the following hypothetical example. Assume a drug contains two functional groups, X and Y, which are located on adjacent carbon atoms and which are essential for biological activity. Further assume that the drug is capable of binding to three different receptor types or subtypes. Given this ...
The Use of Botanical Extracts as Topical Skin
... Skin-Lightening Agents for the Improvement of Skin Pigmentation Disorders Wenyuan Zhu1 and Jie Gao1 Both physicians and dermatology patients are searching for long-term topical skin care solutions (both cosmetic and cosmeceutical) to address problems presented by skin hyperpigmentation. Specifically ...
... Skin-Lightening Agents for the Improvement of Skin Pigmentation Disorders Wenyuan Zhu1 and Jie Gao1 Both physicians and dermatology patients are searching for long-term topical skin care solutions (both cosmetic and cosmeceutical) to address problems presented by skin hyperpigmentation. Specifically ...
Inhibition of acetylcholinesterase and NADH oxidase
... galanthamine are the only drugs currently approved for the treatment of Alzheimer's disease however, these drugs are known to have limitations for clinical use due to their short half lives and/or unfavorable side-effects.4 NADH oxidase catalyzes the twoelectron reduction of oxygen to peroxide or th ...
... galanthamine are the only drugs currently approved for the treatment of Alzheimer's disease however, these drugs are known to have limitations for clinical use due to their short half lives and/or unfavorable side-effects.4 NADH oxidase catalyzes the twoelectron reduction of oxygen to peroxide or th ...
anti-inflammatory screening of jatropha curcas root, stem and leaf in
... promise for the discovery of therapeutic agents with beneficial effects not only in the suppressing relevant aspects of the anti-inflammatory cascade but also on the diverse disease conditions where the inflammatory response is amplifying the disease process. This present study was carried out to as ...
... promise for the discovery of therapeutic agents with beneficial effects not only in the suppressing relevant aspects of the anti-inflammatory cascade but also on the diverse disease conditions where the inflammatory response is amplifying the disease process. This present study was carried out to as ...
H INHIBITORS OF HIV-1 REVERSE TRANSCRIPTASE Research Article
... conformations of the ligands in pdb format[17]. Energy minimized conformation of ligands were subjected to calculation of GasteigerHuckel charges and saved in default format of Autodock. Autodock generated 50 possible binding conformations i.e., 50 runs for each docking by using LGA search. Default ...
... conformations of the ligands in pdb format[17]. Energy minimized conformation of ligands were subjected to calculation of GasteigerHuckel charges and saved in default format of Autodock. Autodock generated 50 possible binding conformations i.e., 50 runs for each docking by using LGA search. Default ...
Thesis - Archive ouverte UNIGE
... Tumour necrosis factor (TNF) is a proinflammatory cytokine that plays a key role in most of the inflammatory processes, as well as in immune responses to infections and tumour antigens [1]. Human TNF-alpha, which is located on chromosome 6, is translated as a 233 amino acid, 26-kDa proprotein that l ...
... Tumour necrosis factor (TNF) is a proinflammatory cytokine that plays a key role in most of the inflammatory processes, as well as in immune responses to infections and tumour antigens [1]. Human TNF-alpha, which is located on chromosome 6, is translated as a 233 amino acid, 26-kDa proprotein that l ...
D. Tetracyclines
... Tetracyclines are still used in rickettsia, Chlamydia, mycoplasma and acne infections. Some of them have antiparasitic properties such as the use of Doxycycline in the treatment and prophylaxis of malaria. They have bacteriostatic action, not recommended in life threatening infections such as septic ...
... Tetracyclines are still used in rickettsia, Chlamydia, mycoplasma and acne infections. Some of them have antiparasitic properties such as the use of Doxycycline in the treatment and prophylaxis of malaria. They have bacteriostatic action, not recommended in life threatening infections such as septic ...
PowerPoint Show Title 32pt bold For internal and external
... duration of action compared to native GIP, but had poor physical stability > G2 analogs showed both improved efficacy and physical stability – Experimental results correlated well with their higher net charge and more negative GRAVY scores predicted in silico. – At 1 mg/mL concentrations were physic ...
... duration of action compared to native GIP, but had poor physical stability > G2 analogs showed both improved efficacy and physical stability – Experimental results correlated well with their higher net charge and more negative GRAVY scores predicted in silico. – At 1 mg/mL concentrations were physic ...
of Conformationally constrained chemotactic peptide analogs R.J.
... 3 kcal .mol-' [ 111. This is small enough to be offset by other interactions. While several examples of @-turn structures are documented in the solid state [lo-131, the p-turn has been observed crystallographically in the cyclic peptide dihydrochlamydocin [ 171. C7 conformations have also been propo ...
... 3 kcal .mol-' [ 111. This is small enough to be offset by other interactions. While several examples of @-turn structures are documented in the solid state [lo-131, the p-turn has been observed crystallographically in the cyclic peptide dihydrochlamydocin [ 171. C7 conformations have also been propo ...
13. chapter - vi
... diffuse out from antibiotic-containing disk and inhibit growth of S. aurous resulting in a zone of inhibition. The successful outcome of antimicrobial therapy with antibacterial compounds depends on several factors. These include host defense mechanisms, the location of infection, and the pharmacoki ...
... diffuse out from antibiotic-containing disk and inhibit growth of S. aurous resulting in a zone of inhibition. The successful outcome of antimicrobial therapy with antibacterial compounds depends on several factors. These include host defense mechanisms, the location of infection, and the pharmacoki ...
Inhibition of Trypanosoma c ruzi Hexokinase by Bisphosphonates
... respectively1-3). In each case, one or more life-cycle stages are dependent on glycolysis for energy production, and consequently, there is interest in the development of specific inhibitors of parasite enzymes involved in glycolysis,4 including glucose transporters,5 as novel routes for chemotherap ...
... respectively1-3). In each case, one or more life-cycle stages are dependent on glycolysis for energy production, and consequently, there is interest in the development of specific inhibitors of parasite enzymes involved in glycolysis,4 including glucose transporters,5 as novel routes for chemotherap ...
MOMORDICA CHARANTIA LIPOXYGENASE ENZYME Research Article
... extracted from soybean seed. The inhibitory effect of Momordica charantia on the activity of the enzyme was studied as the enzyme has a same mechanisms of inflammation involve a series of events in which the metabolism of arachidonic acid. The enzyme in the presence of the plant extract showed a goo ...
... extracted from soybean seed. The inhibitory effect of Momordica charantia on the activity of the enzyme was studied as the enzyme has a same mechanisms of inflammation involve a series of events in which the metabolism of arachidonic acid. The enzyme in the presence of the plant extract showed a goo ...
Selective phosphodiesterase inhibitors for the treatment
... High concentrations of theophylline suppress reactive oxygen metabolite production by neutrophils and eosinophils but lower concentrations enhance this response [74,75]. At high concentrations, the survival time of eosinophils in culture is reduced [76], apparently through the induction of apoptosis ...
... High concentrations of theophylline suppress reactive oxygen metabolite production by neutrophils and eosinophils but lower concentrations enhance this response [74,75]. At high concentrations, the survival time of eosinophils in culture is reduced [76], apparently through the induction of apoptosis ...
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.