Chemistry Techniques, Synthetic
Combinatorial Chemistry Techniques
Microbial desulfurization of organic sulfur compounds in petroleum. (1/1894)Sulfur removal from petroleum is important from the standpoint of the global environment because the combustion of sulfur compounds leads to the production of sulfur oxides, which are the source of acid rain. As the regulations for sulfur in fuels become more stringent, the existing chemical desulfurizations are coming inadequate for the "deeper desulfurization" to produce lower-sulfur fuels without new and innovative processes. Biodesulfurization is rising as one of the candidates. Several microorganisms were found to desulfurize dibenzothiophene (DBT), a representative of the organic sulfur compounds in petroleum, forming a sulfur-free compound, 2-hydroxybiphenyl. They are promising as biocatalysts in the microbial desulfurization of petroleum because without assimilation of the carbon content, they remove only sulfur from the heterocyclic compounds which is refractory to conventional chemical desulfurization. Both enzymological and molecular genetic studies are now in progress for the purpose of obtaining improved desulfurization activity of organisms. The genes involved in the sulfur-specific DBT desulfurization were identified and the corresponding enzymes have been investigated. From the practical point of view, it has been proved that the microbial desulfurization proceeds in the presence of high concentrations of hydrocarbons, and more complicated DBT analogs are also desulfurized by the microorganisms. This review outlines the progress in the studies of the microbial desulfurization from the basic and practical point of view. (+info)
5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats. (2/1894)We previously demonstrated a change in the receptors mediating 5-hydroxytryptamine (5-HT)-induced contraction in arteries of deoxycorticosterone acetate (DOCA)-salt-hypertensive rats. Specifically, contraction to 5-HT is mediated primarily by 5-HT2A receptors in arteries from normotensive sham rats and by both 5-HT2A and 5-HT2B receptors in arteries from hypertensive rats. We hypothesized that the 5-HT2B receptor may play a role in maintaining the high blood pressure of DOCA-salt-hypertensive rats, and herein we provide data connecting in vitro and in vivo findings. The endothelium-denuded isolated superior mesenteric artery of DOCA-salt rats displayed a marked increase in maximum contraction to the newly available 5-HT2B-receptor agonist BW-723C86 compared with that of arteries from sham rats, confirming that the 5-HT2B receptor plays a greater role in 5-HT-induced contraction in arteries from DOCA-salt rats. In chronically instrumented rats, the 5-HT2B-receptor antagonist LY-272015 (0.3, 1.0, and 3.0 mg/kg iv at 30-min intervals) was given cumulatively 1 time/wk during 4 wk of continued DOCA-salt treatment. LY-272015 did not reduce blood pressure of the sham-treated rats at any time or dose. However, LY-272015 (1.0 and 3. 0 mg/kg) significantly reduced mean blood pressure in a subgroup of week 3 (-20 mmHg) and week 4 DOCA-salt (-40 mmHg) rats that had extremely high blood pressure (mean arterial blood pressure approximately 200 mmHg). Blockade of 5-HT2B receptors by in vivo administration of LY-272015 (3.0 mg/kg) was verified by observing reduced 5-HT-induced contraction in rat stomach fundus, the tissue from which the 5-HT2B receptor was originally cloned. These data support the novel hypothesis that 5-HT2B-receptor expression is induced during the development of DOCA-salt hypertension and contributes to the maintenance of severe blood pressure elevations. (+info)
Cleavage of the HER2 ectodomain is a pervanadate-activable process that is inhibited by the tissue inhibitor of metalloproteases-1 in breast cancer cells. (3/1894)HER2/neu, a Mr 185,000 tyrosine kinase receptor that is overexpressed in breast cancer, undergoes proteolytic cleavage of its extracellular domain (ECD). In contrast with other membrane-bound proteins, including growth factor receptors, that are cleaved by a common machinery system, we show that HER2 cleavage is a slow process and is not activated by protein kinase C. Pervanadate, a general inhibitor of protein-tyrosine phosphatases, induces a rapid and potent shedding of HER2 ECD. The shedding of HER2 ECD is inhibited by the broad-spectrum metalloprotease inhibitors EDTA, TAPI-2, and batimastat. The tissue inhibitor of metalloproteases-1; an inhibitor of matrix metalloproteases that does not inhibit cleavage by the general protein kinase C-dependent shedding machinery, also inhibited HER2 ECD shedding, whereas tissue inhibitor of metalloproteases-2 did not. These data suggest that HER2 cleavage is a process regulated by an as-yet-unidentified distinct protease. (+info)
Phase I study of intrapleural batimastat (BB-94), a matrix metalloproteinase inhibitor, in the treatment of malignant pleural effusions. (4/1894)Tumor cells and associated stromal cells secrete matrix metalloproteinases (MMPs), contributing to invasion, angiogenesis, and metastasis. Batimastat (BB-94) is a broad-spectrum MMP inhibitor that causes resolution of ascites and/or tumor growth delay in animal models of breast, ovarian, and colorectal cancer. We recruited 18 patients with cytologically positive malignant pleural effusions into a Phase I study of intrapleural BB-94. Three patients received single doses of BB-94 at each dose level: 15, 30, 60, 105, 135, and 300 mg/m2. Two patients were retreated with a second course at 60 and 105 mg/m2. BB-94 was detectable in plasma 1 h after intrapleural administration, and peak levels of 20-200 ng/ml occurred after 4 h to 1 week. BB-94 persisted in the plasma for up to 12 weeks, at levels exceeding the IC50s for target MMPs. Peak values were higher, and persistence in the plasma was longer after higher doses of BB-94. The treatment was well tolerated. Toxic effects included low-grade fever for 24-48 h (6 of 18 patients, 33%) and reversible asymptomatic elevation of liver enzymes (8 patients, 44%). Toxicity seemed unrelated to BB-94 dose or plasma levels. Sixteen patients evaluable for response required significantly fewer pleural aspirations in the 3 months after BB-94 compared with the 3 months before. Seven patients (44%) required no further pleural aspiration until death/last follow-up. After 1 month, patients treated with 60-300 mg/m2 BB-94 had significantly better dyspnea scores, indicating improved exercise tolerance, compared with baseline scores the day after BB-94. The maximum tolerated intrapleural dose remains to be defined, but it is clear that intrapleural BB-94 is well tolerated, with evidence of local activity. (+info)
Limited anti-inflammatory efficacy of cyclo-oxygenase-2 inhibition in carrageenan-airpouch inflammation. (5/1894)1. Cyclo-oxygenase-2 (COX-2) is expressed at sites of inflammation and is believed to be the major source of inflammation-associated prostaglandin synthesis. Selective inhibition of COX-2 has been suggested to produce anti-inflammatory effects with reduced toxicity in the gastrointestinal tract. We examined the extent to which suppression of COX-2 led to inhibition of various components of inflammation in the carrageenan-airpouch model in the rat. 2. Indomethacin (> or =0.3 mg kg(-1)), nimesulide (> or =3 mg kg(-1)) and the selective COX-2 inhibitor, SC-58125 (> or =0.3 mg kg(-1)), significantly suppressed the production of prostaglandin E2 at the site of inflammation. At higher doses, indomethacin (> or =1 mg kg(-1)) and nimesulide (30 mg kg(-1)), but not SC-58125 (up to 10 mg kg(-1)), significantly inhibited COX-1 activity (as measured by whole blood thromboxane synthesis). 3. All three test drugs significantly reduced the volume of exudate in the airpouch, but only at doses greater than those required for substantial (>90%) suppression of COX-2 activity. Similarly, reduction of leukocyte infiltration was only observed with the doses of indomethacin and nimesulide that caused significant suppression of COX-1 activity. 4. SC-58125 did not significantly affect leukocyte infiltration into the airpouch at any dose tested (up to 10 mg kg(-1)). A second selective COX-2 inhibitor, Dup-697, was also found to suppress exudate PGE2 levels without significant effects on leukocyte infiltration. 5. These results indicate that selective inhibition of COX-2 results in profound suppression of PGE2 synthesis in the carrageenan-airpouch, but does not affect leukocyte infiltration. Exudate volume was only reduced with the highly selective COX-2 inhibitor when a dose far above that necessary for suppression of COX-2 activity was used. Inhibition of leukocyte infiltration was observed with indomethacin and nimesulide, but only at doses that inhibited both COX-1 and COX-2. (+info)
Effects of angiogenesis inhibitors on multistage carcinogenesis in mice. (6/1894)Solid tumors depend on angiogenesis for their growth. In a transgenic mouse model of pancreatic islet cell carcinogenesis (RIP1-Tag2), an angiogenic switch occurs in premalignant lesions, and angiogenesis persists during progression to expansive solid tumors and invasive carcinomas. RIP1-Tag2 mice were treated so as to compare the effects of four angiogenesis inhibitors at three distinct stages of disease progression. AGM-1470, angiostatin, BB-94, and endostatin each produced distinct efficacy profiles in trials aimed at preventing the angiogenic switch in premalignant lesions, intervening in the rapid expansion of small tumors, or inducing the regression of large end-stage cancers. Thus, anti-angiogenic drugs may prove most efficacious when they are targeted to specific stages of cancer. (+info)
Marked suppression of T cells by a benzothiophene derivative in patients with human T-lymphotropic virus type I-associated myelopathy/tropical spastic paraparesis. (7/1894)In a search for new anti-autoimmune agents that selectively suppress activation of autoreactive T cells, one such agent, 5-methyl-3-(1-methylethoxy)benzo[b]thiophene-2-carboxamide (CI-959-A), was found to be effective. This compound, which is known to suppress tumor necrosis factor alpha (TNF-alpha)-induced CD54 expression, inhibited the primary proliferative response of the T cell to antigen (Ag)-presenting cells (APCs) including allogenic dendritic cells (DCs), autologous Epstein-Barr virus-infected B cells, and human T lymphotropic virus type I (HTLV-I)-infected T cells. Autoreactive T cells from patients with HTLV-I-associated myelopathy/tropical spastic paraparesis (HAM/TSP) spontaneously proliferate in vitro, and their activation is reported to be associated with CD54 expression. The spontaneous proliferation of T cells from patients with HAM/TSP was entirely blocked by CI-959-A. However, in this study, the T-cell proliferation in 15 patients with HAM/TSP was found to depend more extensively on major histocompatibility complex (MHC) class II and CD86 than on CD54 Ags. Since most important APCs for the development of HAM/TSP are DCs and HTLV-I-infected T cells, the effect of CI-959-A on DC generation and on the expression of surface molecules on activated T cells is examined. CI-959-A suppressed recombinant granulocyte-macrophage colony stimulating factor (GM-CSF)- and recombinant interleukin-4-dependent differentiation of DCs from monocytes and inhibited the expression of CD54 and, more extensively, MHC class II and CD86 Ags. CI-959-A showed little toxicity toward lymphoma or HTLV-I-infected T-cell lines or toward monocytes and cultured DCs. These results suggest that CI-959-A might be a potent anti-HAM/TSP agent. (+info)
Dorzolamide effect on ocular blood flow. (8/1894)PURPOSE: To evaluate the effect of dorzolamide on ocular blood flow in normal and glaucomatous eyes. METHODS: Twenty-six eyes with documented open-angle glaucoma of 26 patients and 13 normal control eyes of 8 age-matched subjects were included in this study. All eyes underwent color Doppler imaging for measuring peak-systolic velocity, end-diastolic velocity, and resistance index in the ophthalmic and central retinal arteries and the maximal and minimal velocities in the central retinal vein. Eyes were grouped in control and initial and advanced glaucoma categories. Measurements were made in all groups before and after application of topical dorzolamide. Intragroup comparisons between baseline and dorzolamide conditions were made using paired Student's t-test. Intergroup comparisons under baseline conditions between normal and glaucomatous eyes were made by using the one-way ANOVA test. Statistical significance was set at P < 0.05. RESULTS: The peak-systolic velocity of the central retinal artery in glaucomatous eyes and the end-diastolic velocity of the ophthalmic and central retinal arteries in all groups were significantly higher after application of dorzolamide. The minimal velocity of the central retinal vein showed significantly higher values after dorzolamide, whereas the maximal velocity remained unchanged. The peak-systolic velocity of the ophthalmic artery in all groups and the peak-systolic velocity of the central retinal artery in normal eyes also remained unchanged. The resistance index was significantly lower in the ophthalmic and central retinal arteries in all groups after dorzolamide. The intraocular pressure was significantly reduced in all groups after dorzolamide. Under baseline conditions normal control eyes and glaucomatous eyes showed differences in various measurements. Peak-systolic velocity was significantly lower in glaucomatous eyes than in normal control eyes with the exception of the ophthalmic artery in the initial glaucoma group. End-diastolic velocity was lower in glaucomatous eyes than in control eyes in both arteries. Maximal and minimal velocities of the central retinal vein were lower in glaucomatous eyes than in normal control eyes. Resistance index was higher in glaucomatous eyes than in normal control eyes in the ophthalmic artery but not in the central retinal artery. CONCLUSIONS: Most hemodynamic parameters of intraocular and periocular vessels improve after application of topical dorzolamide in both normal control and glaucomatous eyes. Dorzolamide should be regarded as a useful drug for treatment of glaucoma not only because it reduces intraocular pressure but also because it improves the ocular blood supply. (+info)
Thiophenes are a class of organic compounds that contain a five-membered ring with one sulfur atom and two carbon atoms. They are commonly found in a variety of natural and synthetic compounds, including some pharmaceuticals and pesticides. In the medical field, thiophenes are sometimes used as ingredients in drugs to treat a variety of conditions. For example, some thiophene-containing drugs are used to treat high blood pressure, while others are used to treat depression and anxiety. Some thiophenes have also been studied for their potential use in treating cancer. It is important to note that thiophenes can have potential side effects, and their use in medicine is carefully regulated by regulatory agencies such as the U.S. Food and Drug Administration (FDA).
In the medical field, furans are a class of organic compounds that are characterized by a five-membered ring containing two oxygen atoms. They are often found as byproducts of various industrial processes, including the production of dyes, pesticides, and pharmaceuticals. Some furans have been identified as potential carcinogens, meaning they can cause cancer in humans. For example, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), which is a furan, is a highly toxic and persistent environmental pollutant that has been linked to a range of health problems, including cancer, reproductive disorders, and immune system dysfunction. In addition to their potential health risks, furans can also be found in certain foods, such as coffee and beer, and have been associated with certain types of cancer in humans. As a result, the levels of furans in food and the environment are closely monitored by regulatory agencies to ensure that they do not pose a risk to human health.
In the medical field, "Chemistry Techniques, Synthetic" refers to the use of chemical reactions and processes to create or modify molecules for therapeutic or diagnostic purposes. This can include the synthesis of small molecules, such as drugs, or the modification of larger molecules, such as proteins or nucleic acids. Synthetic chemistry techniques are often used in drug discovery and development, as well as in the production of medical imaging agents and other diagnostic tools. These techniques may involve the use of specialized equipment and procedures, such as chromatography, spectroscopy, and mass spectrometry, to purify and characterize the synthesized molecules.
Anisoles are a class of organic compounds that contain a benzene ring with an oxygen atom bonded to one of the carbon atoms. They are also known as phenols or phenolic ethers. In the medical field, anisoles are used as antiseptics, disinfectants, and antifungal agents. They are also used as flavoring agents in food and beverages. Some common examples of anisoles include anisole, estragole, and thymol.
In the medical field, cyclization refers to a chemical reaction in which a molecule undergoes a rearrangement to form a ring structure. This process can occur naturally in the body as part of metabolic pathways, or it can be induced artificially in the laboratory to synthesize new compounds with specific properties. Cyclization reactions are important in the synthesis of many drugs and other bioactive molecules, as they can be used to create molecules with specific shapes and chemical properties that are necessary for their biological activity. For example, the synthesis of many antibiotics involves cyclization reactions to create the ring structures that are essential for their activity against bacteria. In addition to their use in drug synthesis, cyclization reactions are also important in the study of biological molecules such as proteins and nucleic acids. Cyclization can occur naturally in these molecules as part of their structure, and understanding the mechanisms of cyclization can provide insights into the function and regulation of these molecules.
Heterocyclic compounds are organic compounds that contain at least one ring composed of atoms other than carbon. In the medical field, heterocyclic compounds are often used as pharmaceuticals due to their ability to interact with biological targets and produce therapeutic effects. Examples of heterocyclic compounds used in medicine include: 1. Pyrimidines: These are a class of heterocyclic compounds that include thymine, cytosine, and uracil. They are important components of DNA and RNA and are used in the development of antiviral and anticancer drugs. 2. Purines: These are another class of heterocyclic compounds that include adenine and guanine. They are also important components of DNA and RNA and are used in the development of antiviral and anticancer drugs. 3. Imidazoles: These are heterocyclic compounds that contain a nitrogen atom and a carbon atom in a six-membered ring. They are used in the development of antifungal and anti-inflammatory drugs. 4. Quinolines: These are heterocyclic compounds that contain a nitrogen atom and two carbon atoms in a six-membered ring. They are used in the development of antimalarial and antituberculosis drugs. Overall, heterocyclic compounds play an important role in the development of new drugs and therapies in the medical field.
Palladium is a chemical element with the symbol Pd and atomic number 46. It is a soft, silvery-white metal that is highly resistant to corrosion and is often used in jewelry and dental work. In the medical field, palladium is used in the treatment of certain types of cancer, such as ovarian cancer and lung cancer. It is also used in the production of medical equipment and in the manufacture of certain drugs. Palladium is not typically used as a medication on its own, but rather as a component in other treatments.
In the medical field, sulfur compounds refer to chemical compounds that contain sulfur as a central element. Sulfur is a naturally occurring element that is essential for the proper functioning of the human body, and sulfur compounds are found in many biological molecules, including proteins, lipids, and carbohydrates. There are many different types of sulfur compounds, including organic sulfur compounds and inorganic sulfur compounds. Organic sulfur compounds are those that contain sulfur covalently bonded to carbon atoms, and they are found in many important biological molecules, such as cysteine and methionine, which are essential amino acids. Inorganic sulfur compounds, on the other hand, do not contain sulfur covalently bonded to carbon atoms, and they include compounds such as hydrogen sulfide and sulfuric acid. Sulfur compounds play important roles in many biological processes, including the formation of connective tissue, the metabolism of carbohydrates and lipids, and the detoxification of harmful substances. In the medical field, sulfur compounds are used in a variety of therapeutic applications, including the treatment of skin conditions such as acne and psoriasis, and the management of certain types of cancer.
Combinatorial chemistry techniques are a set of methods used to generate and screen large libraries of chemical compounds in order to identify potential drug candidates. These techniques are commonly used in the pharmaceutical industry to accelerate the drug discovery process and increase the chances of finding effective and selective drugs. In the medical field, combinatorial chemistry techniques are used to generate libraries of small molecules that can interact with biological targets such as enzymes, receptors, and nucleic acids. These libraries are then screened using high-throughput screening methods to identify compounds that have the desired biological activity. Once a promising compound is identified, it can be further optimized through medicinal chemistry techniques to improve its potency, selectivity, and pharmacokinetic properties. This process can ultimately lead to the development of new drugs for the treatment of various diseases and conditions. Overall, combinatorial chemistry techniques play a crucial role in the drug discovery process by enabling the rapid generation and screening of large libraries of chemical compounds, which can help to identify potential drug candidates with high efficiency and accuracy.
In the medical field, catalysis refers to the acceleration of a chemical reaction by a catalyst. A catalyst is a substance that increases the rate of a chemical reaction without being consumed or altered in the process. Catalysts are commonly used in medical research and drug development to speed up the synthesis of compounds or to optimize the efficiency of chemical reactions. For example, enzymes are biological catalysts that play a crucial role in many metabolic processes in the body. In medical research, enzymes are often used as catalysts to speed up the synthesis of drugs or to optimize the efficiency of chemical reactions involved in drug metabolism. Catalysis is also used in medical imaging techniques, such as magnetic resonance imaging (MRI), where contrast agents are used to enhance the visibility of certain tissues or organs. These contrast agents are often synthesized using catalytic reactions to increase their efficiency and effectiveness. Overall, catalysis plays a critical role in many areas of medical research and drug development, helping to accelerate the synthesis of compounds and optimize the efficiency of chemical reactions.
Fiesselmann thiophene synthesis
Dialkylbiaryl phosphine ligands
Thiophenes, Benzothiophenes, and Thiophenols
N-(3-aminophenyl)thiophene-2-carboxamide | C11H10N2OS | CID 675398 - PubChem
IUCr) A thio-phene-based aza-cryptand Mannich base: 18,24-bis--(p-tolyl-sulfonamido)-2,5,8,11,21-penta-oxa-15,27-di-thia-18,24...
Electrical Characteristics of the Junction between PEDOT:PSS and Thiophene-Functionalized Silicon Microwires
Synthesis of 2-Alkoxy-Substituted Thiophenes, 1,3-Thiazoles, and Related S-Heterocycles via Lawesson's Reagent-Mediated...
Small molecules containing rigidified thiophenes and a cyanopyridone acceptor unit for solution-processable bulk-heterojunction...
Non-covalent close contacts in fluorinated thiophene-phenylene-thiophene conjugated units: understanding the nature and...
1309677-06-2 5-(6-Methyl-4,8-dioxo-1,3,6,2-dioxazaborocan-2-yl)thiophene-2-carbaldehyde AKSci AMTB848
methyl 3-(aminomethyl)thiophene-2-carboxylate MDL MFCD14155898 - Labseeker
Thiophene chromium tricarbonyl
Thiophene | Amadis Chemical Company Limited
2-(4-Fluorophenyl)thiophene - Georganics
3-hydroxy thiophene - Proactive Molecular Research
Changzhou WaterWeed New Material Co., Ltd. --Aniline|Pyridine|Benzonitrile|Thiophene
Thiophene-pyrrole containing S,N-heteroheptacenes: synthesis, and optical and electrochemical characterisation
91041-18-8 | Methyl 3-(2-nitrophenoxy)-2-thiophene carboxylate | MFCD00202719 | C12H9NO5S
Synthesis of Benzo[b]furan and Benzo[b]thiophene-3-acetic Acids | Abstract
Vibronic coupling in organic semiconductors: The case of fused polycyclic benzene-thiophene structures
The fragmentation behaviour of alkylated thiophene-1,1-dioxides<...
Low band gap thienothiophene-thiophene copolymer: synthesis, characterization and application in polymer solar cells
Ternary blend polymer solar cells with enhanced power conversion efficiency | Nature Photonics
1,3,6-triphenyl-9H-carbazole CS850 - Carbazole, Anthracene, Aromatic Amine, Pyrene, Thiophene OLED Material
Fentanyl Analog Screening Kit and Emergent Panels (FAS, FAS V1-V4 Kits) | CDC
Utata » Tribal Photography » Projects
Alkylated Dinaphtho[2,3-b:2',3'-f]thieno[3,2-b]thiophenes (Cn-DNTTs): Organic Semiconductors for High-Performance Thin-Film...
Publications - Universität Ulm
Palladium catalysis with sulfurated substrates under aerobic conditions: A direct oxidative carbonylation approach to thiophene...
- In this work the synthesis, the spectroscopic and photovoltaic characterization of a thienothiophene-thiophene copolymer are reported. (unimore.it)
- Electrical measurements using a standard probe station indicated that the junction between individual thiophene-functionalized Si MWs and the conducting polymer poly(3,4-ethylenedioxythiophene)/poly(styrenesulfonate) (PEDOT:PSS) became more ohmic as more thiophene was added to the MW surface. (caltech.edu)
- the longest intramolecular distance between the two thiophene rings is 13.479 (4) Å for C4⋯C14 and the longest between the two tosyl rings is 9.983 (3) Å for C25⋯C29. (iucr.org)
- Under a light-limited current of 20 nA, representative of operation of Si MWs under 1 Sun illumination conditions, the iR loss of thiophene-n-Si MW/PEDOT-PSS contacts was 20 mV, representing an order of magnitude reduction compared with PEDOT-PSS junctions formed with methyl terminated n-Si MWs. (caltech.edu)
- Such iR losses are much less than typical catalytic overpotentials for fuel formation, and hence the thiophene-functionalized Si MW contacts will not limit the performance of a Si MW array-based solar fuels device under 1 Sun illumination. (caltech.edu)
- In vitro anti-mycobacterial activity of novel benzo(c)thiophene-1,3-dione: A novel scaffold against Mycobacterium tuberculosis. (physiciansweekly.com)
- The present study evaluated anti-tuberculosis activity of benzo(c)thiophene-1,3-dione against Mycobacterial tuberculosis H37RV in vitro and in vivo in tuberculosis mice model. (physiciansweekly.com)
- The MIC of benzo(c)thiophene-1,3-dione, rifampicin and isoniazid were found to be 4.0, 2.0 and 1.0 μg/ml, respectively. (physiciansweekly.com)
- Benzo(c)thiophene-1,3-dione showed MIC in the range of 8-14 μg/ml against four drug-resistant isolates of M. tuberculosis and MBC 14 μg/ml against M. tuberculosis H37RV. (physiciansweekly.com)
- Interaction of benzo(c)thiophene-1,3-dione with rifampicin led to 2-fold increase in anti-TB activity whereas with isoniazid improvement showed 4-fold enhancement. (physiciansweekly.com)
- Treatment with benzo(c)thiophene-1,3-dione at 1X MIC indicated bacteriostatic activity whereas at 2X, 4X and 4X MIC doses significant reduction in M. tuberculosis load was observed. (physiciansweekly.com)
- The benzo(c)thiophene-1,3-dione administration to mice at doses of 5000 and 1000 mg/kg caused no changes in behaviour nor any death. (physiciansweekly.com)
- Benzo(c)thiophene-1,3-dione treatment of tuberculosis mice model effectively inhibited pulmonary CFU compared to model group. (physiciansweekly.com)
- Data obtained from MTT assay showed negligible cytotoxicity of benzo(c)thiophene-1,3-dione against CMMT, MB 157, CL-S1, normal breast cells in 5-320 μg/ml concentration range. (physiciansweekly.com)
- Thus, benzo(c)thiophene-1,3-dione exhibits promising anti-mycobacterial activity against Mycobacterium tuberculosis H37RV and other drug resistant strains. (physiciansweekly.com)
- In Mycobacterium tuberculosis mice model benzo(c)thiophene-1,3-dione significantly suppressed bacterial load and showed synergism with isoniazid. (physiciansweekly.com)
- Therefore, benzo(c)thiophene-1,3-dione has potential to be evaluated further for development of anti-tuberculosis treatment. (physiciansweekly.com)
- 2-Ethylbutyryl chloride was used in syntheses of bicyclic thiophene derivatives. (sigmaaldrich.com)
- In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. (nih.gov)
- Ventilation measurements and informal discussions were conducted to evaluate worker exposures to nitrobenzene (98953), pyridine (110861), thiophene (110021), and n-amyl-acetate (628637) at the Center for Molecular Nutrition and Sensory Disorders (SIC-8010) in Washington, D.C. on October 14, 1982. (cdc.gov)
- The goal of this study was to report on the pharmacological properties of the novel thiophene sulfonamide gamma secretase inhibitor (GSI), GSI-953,also known as begacestat.In summary, the preclinical data for GSI-953 demonstrate a potent Abeta lowering activity, with nano molar potency, and in vitro selectivity against Notch processing. (nih.gov)
- Poly(2,5-bis(3-alkylthiophen-2-yl)thieno[3,2-b]thiophene), PBTTT, is one such electron donating conjugated polymer typically used in transistors and solar cells because of its high charge carrier mobility. (confex.com)
- An overview of Genetic Toxicology Bacterial Mutagenicity study conclusions related to Thiophene (110-02-1). (nih.gov)