What's the difference between thienyl and thiophene?
Thienyl
Definition:
(n.) The hypothetical radical C4H3S, regarded as the essential residue of thiophene and certain of its derivatives.
Example Sentences:
(1) In addition, we have found that the dissociative anesthetic N-(1-[2-thienyl]cyclohexyl)3,4-piperidine ([3H]TCP) binds to a site whose regional distribution is highly correlated with that of NMDA receptor sites.
(2) MnO2 reduction with glucose by induced whole cells and cell extracts, was inhibited by 1 mM atebrine, 0.1 mM dicumarol, and 10 mM cyanide but not by antimycin A, 2n-nonyl-4-hydroxyguinoline-N-oxide) (NOQNO), 4,4,4-trifluoro-1-(2-thienyl),1,3-butanedione, or carbon monoxide.
(3) Thienyl-PCP (TCP), a drug that is behaviorally more potent than PCP, partially blocked IK at low doses (31% at 1 microM), but even at high doses (25 microM) the degree of block was never as great as that produced by PCP.
(4) One of the analogs, cis-2-hydroxymethyl-r-1-(N-piperidyl)-1-(2-thienyl) cyclohexane (5) was found to show a high affinity (IC50 = 16 nM) for the phencyclidine (PCP) binding sites, very close to that of TCP, and to be 38-fold more potent in binding than its trans isomer.
(5) [3H]N-1-(2-Thienyl)cyclohexyl-3,4-piperidine binding to the phencyclidine site associated with the N-methyl-D-aspartate receptor was reduced by 60-80% in all brain regions examined (P less than 0.001).
(6) The binding of [3H]TCP (N-[1-(2-thienyl)cyclo-hexyl]-3,4-piperidine) to the NMDA receptor remained unchanged in all the experimental groups tested.
(7) Thirty-seven arylcyclohexylamines including phencyclidine (PCP) and derivatives, N[1-(2-thienyl)cyclohexyl]piperidine (TCP) and derivatives and N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine (BTCP) were assessed for their ability to inhibit [3H]PCP binding and [3H]dopamine ([3H]DA) synaptosomal uptake.
(8) Two potential degradation products, i.e., cis-isomer of morantel tartrate and N-(3-methylaminopropyl)-trans-3-(3-methyl-2-thienyl)acrylamide, and a related anthelmintic, i.e., pyrantel tartrate, do not interfere.
(9) [3H]N-(1-[thienyl] cyclohexyl)piperidine (TCP) binding to brain membranes is stimulated by NMDA and glycine receptor agonists.
(10) Compounds (+)-1, (-)-1, (-)-2, and (+)-2 were compared for their binding affinities at kappa opioid, sigma, D2-dopamine, and phencyclidine (PCP) receptors in competitive binding assays using [3H]bremazocine ([3H]BREM) or [3H]U69,593, [3H]-(+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine [[3H]-(+)-3-PPP], or [3H]-1,3-di(o-tolyl)guanidine ([3H]DTG), [3H]-(-)-sulpiride [[3H]-(-)SULP], and [3H]-1- [1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP), respectively.
(11) Opposed to this course, the reaction of 1b with 1,1,1,2,2,3,3-heptafluoro-6-(2-thienyl)-4,6-hexanedione (4) fails to lead to ring closure but rather yields 4,4,5,5,6,6,6-heptafluoro-3-(2-methyl-1-thioureido)-1-(2-thienyl)-1-hexen-1,3-diol (5).
(12) Derivatives with fluoromethyl and hydroxymethyl groups on the cyclohexyl ring of 1-[1-(2-thienyl)cyclohexyl]piperidine (TCP), a noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptor, were tested in a radioligand binding assay to evaluate their ability to inhibit [3H]TCP binding by rat brain homogenates.
(13) The phenyl ring of tetramisole and 2,3-dehydrotetramisole was also replaced by a naphthyl ring, and the phenyl ring of 2,3-dehydrotetramisole was substituted by a thienyl ring system.
(14) Analgesic effect and tolerability of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) drops were tested in an open study including 51 informed outpatients with moderate to severe postoperative and posttraumatic pain.
(15) (R)-N-[4,4-Bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid (NO 328) has previously been shown to be a potent anticonvulsant in both mice and rats.
(16) The distribution of sigma and phencyclindine binding sites in the gastrointestinal tract of the guinea pig was studied by autoradiography after in vitro incubation of tissue slices with (+)3H-SKF 10,047 and 3H-1-1-[(2-thienyl)cyclohexyl] piperidine to locate sigma and phencyclidine receptors, respectively.
(17) The compounds 4- and 6-fluoro-tryptophan, 5-methyltryptophan, selenocystine and beta-(2-thienyl)alanine gave strong growth inhibition in minimal medium, which disappeared after addition of structurally related natural amino acids or in an enriched broth.
(18) In enzymatically-dispersed single ventricular cardiomyocytes of adult rats and guinea pigs the inhibition of the cardiac sodium current by a novel sodium channel blocking agent (LG 83-6-05, 1-[3-(2-Hydroxy-3-(2-methylpropylamino)-propoxy)-4-methyl-2- thienyl++ ]-3-phenyl-1-propanon hydrochloride) was studied.
(19) 96, 4962) gave new derivatives of adenosine cyclic 3',5'-phosphate with the following 2-substituents: n-propyl, n-hexl, n-octyl, n-decyl, styryl, o-methoxyphenyl, and 2-thienyl.
(20) All four compounds completely inhibited the use-dependent binding of [3H]N-[1-(2-thienyl) cyclohexyl]-piperidine and were noncompetitive, glycine-reversible inhibitors of both NMDA-induced biochemical and electrophysiological responses in brain slice preparations.
Thiophene
Definition:
(n.) A sulphur hydrocarbon, C4H4S, analogous to furfuran and benzene, and acting as the base of a large number of substances which closely resemble the corresponding aromatic derivatives.
Example Sentences:
(1) Quantitative structure activity relationships of 2-amino-3-carboxylic acid ethyl ester thiophene derivatives are described.
(2) Some of the thiophenes and their acetylenic derivatives possess extremely potent phototoxic activities toward membrane-containing viruses.
(3) The compounds were obtained by condensation of appropriate hydrazines with thiophene 2-carboxaldehyde (series 1), thiophene 3-carboxaldehyde (series 2), and 5-nitrothiophene-2-carboxaldehyde (series 3).
(4) The prototype kappa-selective agonist, PD117302 (trans-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzo[b]thiophene-4- acetamide, 2) has been regio- and stereoselectively substituted in the C-4 and C-5 positions of the cyclohexyl ring with the methyl ether and spiro tetrahydrofuran groups.
(5) Since no previously identified genes involved in thiophene metabolism are located in this region, we designated the gene for the 48-kDa protein as thdF.
(6) Among the compounds described are 6-hydroxybenzo[b]thiophene-2-sulfonamide (16) and its acetate ester (23), which are among the most potent ocular hypotensive agents in this class, as assessed in the alpha-chymotrypsinized rabbit.
(7) The normalizing effects of the thiophene compounds on serum phosphorus levels were not significant at the dosages used.
(8) Maximum photo-basophil-histamine-release was 4% with acetylsalicylic acid, 10% with benoxaprofen, 20% with thiophene, 28% with diclofenac, 39% with tiaprofenic acid, 40% with carprofen, 55% with ketoprofen, and not demonstrable with indoprofen.
(9) The more hydrophobic cephalosporins, with a thiophene moiety at the C7 position, were more active than C7-methoxyiminoaminothiazole derivatives against S. aureus H (beta-lactam-susceptible), and compounds with a thioether function at C3 were more active than those with a sulphonyl function at this position.
(10) Several guanidine compounds were synthesized by the reaction of acid chlorides of thiophene and furan with guanidines.
(11) Alpha-terthienyl (alpha-T), a phototoxic thiophene compound isolated from marigolds (Tagetes species), affects cell membranes and does not appear to induce cytogenetic damage.
(12) In a directed search for the best compounds for clinical evaluation, some 150 selected nitroaromatic compounds, representing 6 distinct types, namely, furans, thiophenes, imidazoles, pyrazoles, pyrroles, and triazoles, have been synthesized and tested as hypoxic cell radiosensitisers and bioreductive drugs.
(13) Replacement of ring A by heterocyclic rings (thiophene or pyridine) leads to analogues with only moderate activity.
(14) These results clearly show that all three thiophene systems have potent activity as antihypertensive agents and that 3 and 4 are more potent than 1 or 2 as alpha 1-antagonists in vivo.
(15) A comparative study of the intestinal transport of DL-tryptophan and its 1-methylindole (tryptophan-l-Me) and benzo[b]thiophene (tryptophan-S) analogs has been carried out in vitro, using the everted intestinal sac of the rat and hamster.
(16) Except for cardioselectivity at low doses, the thiophenic analogue of metoprolol behaves in a very similar way as this compound in all the aspects considered in a preliminary pharmacological study.
(17) Six-month chronic oral toxicity studies of 7-chloro-3-[1-(2, 4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethoxy-methyl] benzo[b]thiophene (sertaconazole, FI-7045, CAS 99592-32-2) were carried out in rats and ferrets.
(18) N-(3-dimethylaminopropyl)naphtho[2,1-b]thiophene-4-carboxamide and the 6-substituted methoxy, methyl, fluoro, chloro, bromo, trifluoromethyl, and cyano derivatives have been shown to bind to DNA via intercalation with binding constants in the 35-900 X 10(3) range at 25 degrees C, pH 7, and [Na+] = 0.019M.
(19) Tienilic acid (TA) is metabolized by human liver microsomes in the presence of NADPH with the major formation of 5-hydroxytienilic acid (5-OHTA) which is derived from the hydroxylation of the thiophene ring of TA.
(20) The synthesis of 1-substituted benzothieno[2,3-d]imidazoles and their most suitable synthesis precursor 2-nitro-3-substituted-amino benzo[b]thiophenes is reported.