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Topic: Benzimidazole

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	Benzimidazole derivatives - Patent 6166219
		Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts.
		The benzimidazole derivative or its pharmaceutically acceptable salt of claim 1, wherein said derivative is selected from the group consisting of 6-benzenesulfonylcarbamoyl-1-(2-chlorobenzyl)-2-methylbenzimidazole, 1-(biphenyl-4-ylmethyl)-6-(1-butanesulfonylcarbamoyl)-2-methylbenzimidazol e, 1-(biphenyl-4-ylmethyl)-6-(1-butanesulfonylcarbamoyl)-2-ethylbenzimidazole, 6-benzenesulfonylcarbamoyl-2-cyclopropyl-1-(2-fluorobenzyl)benzimidazole, 6-benzenesulfonylcarbamoyl-1-(2,4-dichlorobenzyl)-2-methylbenzimidazole, 6-benzenesulfonylcarbamoyl-1-(2,4-difluorobenzyl-2-methylbenzimidazole, 6-(1-butanesulfonylcarbamoyl)-1-[(3-fluorobiphenyl-4-yl)methyl]-2-methylbe nzimidazole, 1-(2,4-dichlorobenzyl)-2-methyl-6-(1-pentanesulfonylcarbamoyl)benzimidazol e, and 1-(4-biphenylmethyl)-2-ethyl-6-(1-pentanesulfonylcarbamoyl)benzimidazole.
		The compound of formula (24) may be converted into a benzimidazole compound of formula (25) in the same manner as in the step (e) of converting the compound of formula (20) into the compound of formula (21).
	www.freepatentsonline.com /6166219.html (7390 words)

	Patent 6,077,528
		It is therefore an object of the present invention to provide a percutaneous preparation superior in percutaneous absorption of benzimidazole compound and duration of efficacy, that exhibits an improved stability of the benzimidazole compound (which is as an active ingredient) in the preparation.
		When a pharmacologically acceptable acid addition salt of the benzimidazole compound is used, an organic base (e.g., ethanolamine and the like) or an inorganic base (e.g., sodium hydroxide and sodium carbonate and the like) may be concurrently added to the adhesive layer, whereby said acid addition salt becomes a free base in the adhesive layer.
		The 2-mercaptobenzimidazole inhibits reactions between the benzimidazole compound and the components contained in the adhesive in trace amounts, thereby affording an improved stability of the benzimidazole compound in the preparation.
	www.pharmcast.com /Patents/062000OG/6077528_Percutaneous062000.htm (2896 words)

	Frac
		Benzimidazoles are low use-rate, broad-spectrum fungicides that have been used commercially for the control of plant diseases since the late 1960’s.
		Benzimidazoles are potent inhibitors of ß-tubulin polymerization in many species of fungi and have been used for plant disease control since the late 1960’s.
		Due to the widespread incidence of benzimidazole resistance in many fungal populations, good resistance management practices must be implemented as soon as possible in order to delay or prevent further changes in sensitivity in the target pathogens.
	www.frac.info /frac/work/work_benz.htm (1381 words)

	Benzimidazole compounds and their use - Patent 5141950
		Certain benzimidazole compounds and their pharmaceutically acceptable salts, are dual inhibitors of lipoxygenase and cycylooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
		A pharmaceutical composition suitable for inhibition of cyclooxygenase and lipoxygenase enzymes in a mammalian subject, which comprises a cyclooxygenase or lipoxygenase inhibiting amount of a compound according to claim 11 and a pharmaceutically acceptable carrier or diluent.
		The new compounds of the present invention are inhibitors of both the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are of use in the treatment or alleviation of allergic or inflammatory conditions in mammals including humans.
	www.freepatentsonline.com /5141950.html (2987 words)

	CARBENDAZIM (2-BENZIMIDAZOLECARBAMIC ACID METHYL ESTER)
		Benzimidazole is a dicyclic compound having midazole ring fused to benzene.
		Benzimidazole structure is a part of the nucleotide portion of vitamin B
		Benzimidazole structure is the nucleus in some drugs such as proton pump inhibitors and anthelmintic agents.
	www.chemicalland21.com /lifescience/agro/CARBENDAZIM.htm (416 words)

	Birth Defects (Site not responding. Last check: 2007-11-06)
		Benzimidazole worm products should not be given in the first month of pregnancy to avoid abortions and birth defects.
		We have long known that we should avoid the use of benzimidazole in early pregnancy, and we have recommended against their use in any pregnant ewe.
		Benzimidazole wormers should not be given in early pregnancy to avoid abortions and birth defects.
	www.pipevet.com /articles/Birth_Defects.htm (282 words)

	SUGARBEET DISEASE CONTROL
		Benzimidazole (Benlate or Topsin M) resistant strains, grow normally in the laboratory in the presence of 5 ppm of benzimidazole fungicide.
		The benzimidazole fungicides Benlate and Topsin M should be applied at 3/8 lb/A in a tank mix with mancozeb at 2 lb/A. The higher rate (1/2 lb) of Benlate or Topsin M should not be needed and will only increase costs.
		Tank mixes of the benzimidazole fungicides (Benlate or Topsin M) with mancozeb should be followed by an application of mancozeb or Super Tin 10 days after the tank mix has been applied in southern Minnesota, 10-12 days in the southern Red River Valley and 10-14 days in the northern Red river Valley.
	www.sbreb.org /productguide/diseasechem.htm (2208 words)

	4.30 Thiabendazole (R)**
		The hydroxylation of the benzimidazole ring at the 5-position to form 5-hydroxythiabendazole and subsequent conjugation to form the glucuronide and sulfate are the major metabolic steps.
		Benzimidazole was detected only in shoot tissues (<0.05 mg/kg in forage and 7.49 mg/kg in straw), either free or as the sugar conjugate(s).
		Thiabendazole, free and conjugated 5-hydroxythiabendazole, and benzimidazole were found to be stable during frozen storage in crops for periods of 12 to 28 months, and in animal commodities for at least 2 months.
	www.fao.org /docrep/w8141e/w8141e17.htm (4751 words)

	Identification and Characterization of Benzimidazole Resistance in Monilinia fructicola from Stone Fruit Orchards in ...
		Identification and Characterization of Benzimidazole Resistance in Monilinia fructicola from Stone Fruit Orchards in California -- Ma et al.
		Mutations of the ß-tubulin gene associated with different phenotypes of benzimidazole resistance in the cereal eyespot fungi Tapesia yallundae and Tapesia acuformis.
		Benzimidazole fungicides: mechanism of action and biological impact.
	aem.asm.org /cgi/content/full/69/12/7145 (4469 words)

	BENZIMIDAZOLE (N,N'-METHYLENYL-O-PHENYLENEDIAMINE)
		Benzimidazole is a white to slightly beige solid; melting at 172 C, boils at 360 C, slightly soluble in water, soluble in ethanol.
		Benzimidazole and its derivatives are used in organic synthesis and vermicides or fungicides as they inhibit the action of certain microorganisms.
		Benzimidazole structure is the nucleus in some drugs such as p
	www.chemicalland21.com /specialtychem/finechem/BENZIMIDAZOLE.htm (434 words)

	Comparison of benzimidazole nucleosides and ganciclovir on the in vitro proliferation and colony formation of human ...
		Comparison of benzimidazole nucleosides and ganciclovir on the in vitro proliferation and colony formation of human bone marrow progenitor cells.
		Recently we have shown that certain benzimidazole ribonucleosides are potent and selective inhibitors of human cytomegalovirus (HCMV) replication.
		In contrast to the benzimidazoles, ganciclovir decreased colony formation by 84% for BFU-E and 86% for CFU-GM at 100 microM.
	www.aegis.com /aidsline/1996/sep/M9690707.html (583 words)

	NZPPS Benzimidazole Management Strategy (Site not responding. Last check: 2007-11-06)
		Using dicarboximides and benzimidazoles in the same spray programme may lead to development of pathogen strains with dual resistance.
		They all generate MBC (methyl benzimidazol carbamate), either as the principal active ingredient, or as a breakdown compound formed on mixing with water.
		Benzimidazole fungicides were introduced into New Zealand in the late 1960's and they offered systemic, curative fungicidal activity on a number of problem diseases (e.g.
	www.hortnet.co.nz /publications/nzpps/resistance/benzimidazole.htm (685 words)

	Fitness of benzimidazole-resistant and susceptible worms of Teladorsagia circumcincta, a nematode parasite of small ...
		The fact that there were no differences in fitness suggests that the installation of benzimidazole resistance in a worm population is irreversible.
		Benzimidazoles (BZ) derivatives have become the most widely used of these drugs but resistance to them is now common throughout the world (Bjorn, 1994, Conder and Campbell, 1995).
		As the benzimidazole resistance is linked to the replacement of a phenylalanine at residue 200 by a tyrosine, a decrease in fitness was also suspected in resistant genotype.
	www.tours.inra.fr /urbase/internet/theses/elard/article5.htm (4012 words)

	Benzimidazole - Wikipedia, the free encyclopedia
		This bicyclic compound consists of the fusion of benzene and imidazole.
		The most prominent benzimidazole in nature is N-ribosyl-dimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12.
		(NH Benzimidazole, as well as the analog imidazole have been used as carbon skeletons for N-heterocyclic carbenes.
	en.wikipedia.org /wiki/Benzimidazole (148 words)

	Resistance of Human Cytomegalovirus to Benzimidazole Ribonucleosides Maps to Two Open Reading Frames: UL89 and UL56 -- ...
		we have proposed that the benzimidazole ribonucleosides inhibit
		Susceptibilities of HCMV strains and recombinants to benzimidazole ribonucleosides and GCV
		Benzimidazole ribonucleosides inhibit the cleavage of concatemeric, viral DNA to monomeric, genomic-length units at concentrations
	jvi.asm.org /cgi/content/full/72/6/4721 (6979 words)

	Polymorphism of the isotype 1 b-tubulin gene in benzimidazole-resistant
		In this work, we demonstrated that the acquisition of the benzimidazole (BZ) resistance in the small ruminant parasite Teladorsagia circumcincta is linked to the selection of individuals that are characterized by a tyrosine (Tyr) at the amino acid 200 of their isotype 1 ß-tubulin gene.
		(1994) have observed that the Phe-200 is a strong predictor of benzimidazole susceptibility for protozoan parasites.
		Kwa MS, Veenstra JG, Roos MH (1994) Benzimidazole resistance in Haemonchus contortus is correlated with a conserved mutation at amino acid 200 in b-tubulin isotype 1.
	www.tours.inra.fr /urbase/internet/theses/elard/article4.htm (3841 words)

	Benzimidazole
		Structural and mechanistic aspects of transcriptional induction of cytochrome P450 1A1 by benzimidazole derivatives...
		benÂ·zimÂ·idÂ·azÂ·ole (b n z -m -d z l, -m d -z l) n.
		Synthesis and antimicrobial activities of 5-fluoro-1,2,6-trisubstituted benzimidazole carboxamide and acetamide...
	www.igetridoffleas.com /pets/fleas84.htm (925 words)

	ARS \| Publication request: Analysis of Benzimidazole-Tolerance in Cercospora Beticola. (Site not responding. Last check: 2007-11-06)
		Benzimidazole fungicides target beta-tubulin and are used in some production regions for disease control.
		However, benzimidazole use is increasingly limited as benzimidazole-resistance becomes more widespread in the pathogen population.
		C. beticola isolates collected in the central High Plains region of the United States in 2004 are being tested for their response to benzimidazoles and NPC, and a PCR-based method for detection of benzimidazole sensitivity is being investigated.
	ars.usda.gov /research/publications/publications.htm?SEQ_NO_115=171560 (267 words)

	Inhibition of Human Cytomegalovirus Replication by Benzimidazole Nucleosides Involves Three Distinct Mechanisms -- ...
		Benzimidazole nucleosides 853, 1311, maribavir, and BDCRB and a GCV control were added to cells infected with HCMV at time zero and at the indicated time points.
		To emphasize the differences between late-acting inhibitors, virus-infected cells were incubated with a lower amount of FBS at 34°C instead of 37°C, which is ordinarily used as in the experiment shown in Fig.
		HCMV time-of-addition study for benzimidazole nucleosides 1311 and BDCRB with GCV and pyrrolo[2,3-d]pyrimidine 1028 control compounds.
	aac.asm.org /cgi/content/full/48/10/3918 (5315 words)

	Inhibition of Epstein-Barr Virus Replication by a Benzimidazole L-Riboside: Novel Antiviral Mechanism of ...
		Neither compound is phosphorylated in vitro or in vivo (5, 6).
		Antiviral activity and mechanism of action of 1263W94, a benzimidazole riboside inhibitor of human cytomegalovirus, abstr.
		Benzimidazole ribonucleosides: a new class of antivirals with potent and selective activity against human cytomegalovirus.
	jvi.asm.org /cgi/content/full/73/9/7271 (5891 words)

	256. Benomyl (WHO Pesticide Residues Series 3)
		Similar to other benzimidazole fungicides it is active against a broad spectrum of fungi, among which are Ascomycetes, Basidiomycetes and some Deuteromycetes, while it is found completely inactive against the Phycomycetes fungi (Edgington et al., 1971; Bollen, 1972).
		Among the well-controlled fungal diseases are powdery mildew, apple scab (Venturia inaequalis) and the grey mould fungus Botrytis cinerea (Evans, 1971).
		Cow feeding trials show that hydroxylated methyl benzimidazole carbamates are formed from benomyl with MBC as the probable intermediate metabolite.
	www.inchem.org /documents/jmpr/jmpmono/v073pr04.htm (3333 words)

	In Vitro Activities of Benzimidazole D- and L-Ribonucleosides against Herpesviruses -- Williams et al. 47 (7): 2186 -- ...
		In Vitro Activities of Benzimidazole D- and L-Ribonucleosides against Herpesviruses -- Williams et al.
		Development of novel benzimidazole riboside compounds for treatment of cytomegalovirus disease.
		Benzimidazoles for the treatment of human cytomegalovirus infections.
	aac.asm.org /cgi/content/full/47/7/2186 (4475 words)

	Percutaneous needle aspiration, injection, and reaspiration with or without benzimidazole coverage for uncomplicated ...
		Two randomised clinical trials on the puncture, aspiration, injection, and re-aspiration method for patients with uncomplicated hepatic hydatid cyst were identified.
		To assess the benefits and harms of PAIR with or without benzimidazole coverage for patients with uncomplicated hepatic hydatid cyst in comparison with sham/no intervention, surgery, or medical treatment.
		PAIR seems promising, but there is insufficient evidence to support or refute PAIR with or without benzimidazole coverage for treating patients with uncomplicated hepatic hydatid cyst.
	www.cochrane.org /reviews/en/ab003623.html (527 words)

	Benzimidazole derivatives (Site not responding. Last check: 2007-11-06)
		Benzimidazole derivatives represented by formula I-1 or their pharmaceutically acceptable salts: ##STR64##
		Compounds which are described in claim 1, in which the benzimidazole derivatives represented by the formula I are
		A pharmaceutical composition comprising a nociceptin receptor-antagonistically effective amount of a compound of formula I as set forth in claim 1 or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable adjuvant.
	www.well.com /~ulee/purge_gas_sensor/benzimidazole_derivatives.html (1832 words)

	263. Carbendazim (WHO Pesticide Residues Series 3)
		A minor metabolite from benomyl is believed to be 2-amino benzimidazole.
		Carbendazim is generally recognized as the chemical entity, which is mainly responsible for the fungitoxic activity of some other systemic benzimidazole fungicides, including benomyl and thiophanate-methyl.
		By analogy to other benzimidazole compounds, carbendazim may be anticipated to metabolize in the animal into hydroxylated analogues which may appear in meat and milk products.
	www.inchem.org /documents/jmpr/jmpmono/v073pr11.htm (4218 words)

	IngentaConnect Analysis of -tubulin Gene Fragments from Benzimidazole-sensitive ... (Site not responding. Last check: 2007-11-06)
		Cercospora leaf spot of sugar beet, caused by the fungus Cercospora beticola, is a major foliar pathogen on sugar beet.
		The precise genetics of this resistance is not known in this fungus.
		We tested benzimidazole-tolerant and -sensitive isolates and found a single mutation in the β-tubulin gene of benzimidazole-tolerant isolates that corresponds to a mutation known to confer benzimidazole tolerance in other ascomycetes.
	www.ingentaconnect.com /content/bsc/jph/2006/00000154/00000006/art00001 (289 words)

	Inhibition of Ganciclovir-Susceptible and -Resistant Human Cytomegalovirus Clinical Isolates by the Benzimidazole ...
		Inhibition of Ganciclovir-Susceptible and -Resistant Human Cytomegalovirus Clinical Isolates by the Benzimidazole L-Riboside 1263W94 -- McSharry et al.
		The benzimidazole ribonucleosides represent a new class of antiviral compounds that inhibit HCMV replication by blocking the
		Inhibition of human cytomegalovirus DNA methylation by a benzimidazole ribonucleoside is mediated through the UL89 gene product.
	cdli.asm.org /cgi/content/full/8/6/1279 (1984 words)

	DETECTION OF BENZIMIDAZOLE RESISTANCE-ASSOCIATED MUTATIONS IN THE FILARIAL NEMATODE WUCHERERIA BANCROFTI AND EVIDENCE ...
		Interaction of anthelmintic benzimidazoles and benzimidazole derivatives with bovine brain tubulin.
		Benzimidazole resistance in Haemonchus contortus is correlated with a conserved mutation at amino acid 200 in beta-tubulin isotype 1.
		Importance of the mutation of amino acid 200 of the isotype 1 ß-tubulin gene in the benzimidazole resistance of the small-ruminant parasite Teladorsagia circumcincta.
	www.ajtmh.org /cgi/content/full/73/2/234 (3353 words)

	(WO/1997/021437) NAPHTHYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS ANTICOAGULANTS (Site not responding. Last check: 2007-11-06)
		(EN) Novel naphthyl-substituted benzimidazole compounds and their pharmaceutically acceptable salts are described herein.
		This invention is also directed to an anticoagulant composition comprising a naphthyl-substituted benzimidazole compound described herein.
		The novel compound or its composition has inhibitory activity against human factor Xa or IIa, thereby useful in treating a disease state mediated by factor Xa or IIa.
	www.wipo.int /pctdb/en/wo.jsp?WO=1997/21437 (180 words)

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