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Synthesis and evaluation of 2-(4-[4-acetylpiperazine-1-carbonyl] phenyl)-1H-benzo[d]imidazole-4-carboxamide derivatives as potential PARP-1 inhibitors and preliminary study on structure-activity relationship
Although 1H-benzo[d]imidazole-4-carboxamide derivatives have been explored for a long time, the structure–activity relationship of the substituents in the hydrophobic pocket (AD binding sites) has not thoroughly discovered. Here in, a series of 2-(4-[4-acetylpiperazine-1-carbonyl]phenyl)-1H-benzo[d]imidazole-4-carboxamide derivatives have been designed, synthesized, and successful characterization as novel and effective poly ADP-ribose polymerases (PARP)-1 inhibitors to improve the structure–activity relationships about the substituents in the hydrophobic pocket. These derivatives were evaluated for their PARP-1 inhibitory activity and cellular inhibitory against BRCA-1 deficient cells (MDA-MB-436) and wild cells (MCF-7) using PARP kit assay and MTT method. The results indicated that compared with other heterocyclic compounds, furan ring-substituted derivatives 14n-14q showed better PARP-1 inhibitory activity. Among this derivatives, compound 14p displayed the strongest inhibitory effects on PARP-1 enzyme (IC50?=?0.023 μM), which was close to that of Olaparib. 14p (IC50?=?43.56 ± 0.69 μM) and 14q (IC50?=?36.69 ± 0.83 μM) displayed good antiproliferation activity on MDA-MB-436 cells and inactivity on MCF-7 cells, indicating that 14p and 14q have high selectivity and targeting. The molecular docking method was used to explore the binding mode of compound 14p and PARP-1, and implied that the formation of hydrogen bond was essential for PARP-1 inhibition activities. This study also showed that in the hydrophobic pocket (AD binding sites), the introduction of strong electronegative groups (furan ring, e.g.) or halogen atoms in the side chain of benzimidazole might improve its inhibitory activity and this strategy could be applied in further research.
Cao, Xuan,Chen, Miaojia,Huang, Honglin,Jiang, Lizhi,Li, Yang,Liu, Yunfan,Peng, Junmei,Tang, Guotao,Wu, Kaiyue
(2021/06/25)

Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists
N-Benzyl substitution of phenethylamine 5-HT2A receptor agonists has dramatic effects on binding affinity, receptor selectivity and agonist activity. In this paper we examine how affinity for the 5-HT2A/2C receptors are influenced by N-benzyl substitution of 4-bromo-2,5-dimethoxyphenethylamine derivatives. Special attention is given to the 2′ and 3′-position of the N-benzyl as such compounds are known to be very potent. We found that substitutions in these positions are generally well tolerated. The 2′-position was further examined using a range of substituents to probe the hydrogen bonding requirements for optimal affinity and selectivity, and it was found that small changes in the ligands in this area had a profound effect on their affinities. Furthermore, two ligands that lack a 2′-benzyl substituent were also found to have high affinity contradicting previous held notions. Several high-affinity ligands were identified and assayed for functional activity at the 5-HT2A and 5-HT2C receptor, and they were generally found to be less efficacious agonists than previously reported N-benzyl phenethylamines.
Hansen, Martin,Jacobsen, Stine Engesgaard,Plunkett, Shane,Liebscher, Gudrun Eckhard,McCorvy, John D.,Br?uner-Osborne, Hans,Kristensen, Jesper Langgaard
supporting information
p. 3933 - 3937
(2015/01/30)

Catalytic formation of ketones from unactivated esters through rhodium chelation-assisted C-O bond activation
A new method for building aryl aryl ketones containing heterocyclic rings through chelation-assisted C-O bond activation catalyzed by a rhodium complex has been developed. In this reaction, methyl quinoline-8-carboxylate, methyl quinoxaline-5-carboxylate, and their derivatives were reacted with an excess amount of a substituted phenyl boronic acid in the presence of a rhodium(I) complex to give substituted phenyl(quinolin-8-yl)methanone, phenylquinoxalin-5- ylmethanone, and their derivatives in medium to high yields. The current method offers a highly favorable synthetic pathway to efficiently build related drugs with an 8-benzoylquinoline core structure. This method may prove especially valuable for medicinal chemists for the late-stage introduction of versatile ketone moieties into complex scaffolds for diversity-oriented synthetic strategies.
Wang, Jingjing,Zuo, Sujing,Chen, Weiqiang,Zhang, Xinrui,Tan, Kaixin,Tian, Yun,Wang, Jianhui
p. 8217 - 8231
(2013/09/24)

1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF
Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
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Paragraph 0624

(2013/11/19)

Benzimidazole-4-Carboxamide Derivatives, Their Preparation Methods, Pharmaceutical Compositions And Their Uses
The present invention relates to the benzimidazole-4-carboxamide derivatives, their preparation methods, pharmaceutical compositions and their uses; wherein X represents monosubstituted or bissubstituted or polysubstitued C1-C14 alkoxy, monosubstituted or bisubstituted or polysubstitued C1-C14 alkyl, monosubstituted or bisubstituted or polysubstitued C2-C14 alkenyl, monosubstituted or bisubstituted or polysubstitued C6-C14 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom; Y represents hydrogen, monosubstituted or bisubstituted or polysubstitued C1-C16 alkyl, monosubstituted or bisubstituted or polysubstitued C6-C12 aryl, or monosubstituted or bisubstituted or polysubstitued 5 to 6 membered heterocyclic group, or monosubstituted or bisubstituted or polysubstitued fused ring group containing nitrogen heteroatom. The derivatives of the present invention have the functions of antiviral medicine.
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(2011/11/12)

Inhibitory properties of 2-substituent-1H-benzimidazole-4-carboxamide derivatives against enteroviruses
A series of novel benzimidazole derivatives were designed, synthesized, and evaluated for their activities against four kinds of enteroviruses, that is, Coxsackie virus A16, B3, B6 and Enterovirus 71 in VERO cells. Strong activities against enterovirus replication and low cytotoxicities were observed in these benzimidazoles generally. The most promising compound was (l)-2-(pyridin-2-yl)- N-(2-(4-nitrophenyl)pentan-3-yl)-1H-benzimidazole-4-carboxamide (16), with a high antiviral potency (IC50 = 1.76 μg/mL) and a remarkable selectivity index (328). These compounds were selected for further evaluation as novel enterovirus inhibitors.
Xue, Fei,Luo, Xianjin,Ye, Chenghao,Ye, Weidong,Wang, Yue
body text
p. 2641 - 2649
(2011/06/11)

LIPOIC ACID AND NITROXIDE DERIVATIVES AND USES THEREOF
The present invention provides bifunctional compounds comprising a poly(ADP-ribose) polymerase (PARP) inhibitor moiety and a reactive oxygen species (ROS) scavenger moiety, more particularly, a lipoic acid or cyclic nitroxide derivative, covalently attached either directly or via a linker, as well as pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions of the invention are useful for prevention, treatment, or management of diseases, disorders and conditions associated with elevated PARP activity or expression.
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Page/Page column 32-34

(2011/12/02)

DIHYDROOROTATE DEHYDROGENASE INHIBITORS
The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
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Page/Page column 62

(2010/11/03)

Copper-catalyzed direct amination of ortho-functionalized haloarenes with sodium azide as the amino source
A simple copper-catalyzed direct amination of ortho-functionalized haloarenes (2-halobenzoic acid, 2-halobenzamide, and N-(2-bromophenyl)acetamide derivatives) has been developed with use of NaN3 as the amino source in ethanol, and the corresponding ortho-functionalized aromatic amines were synthesized in good to excellent yields. The protocol undergoes one-pot Ullmann-type coupling of ortho-functionalized haloarenes with NaN3 to lead to ortho-functionalized azidoarenes, followed by reduction with ethanol.
Zhao, Haibo,Fu, Hua,Qiao, Renzhong
experimental part
p. 3311 - 3316
(2010/08/05)

SUBSTITUTED BENZIMIDAZOLES, BENZOTHIAZOLES AND BENZOXAZOLES
The present invention relates to substituted benzimidazoles, benzothiazoles and benzoxazoles, processes for their preparation, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
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Page/Page column 109-110

(2010/12/29)

2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as endometriosis, prostate cancer and others. Traditional therapy has been limited to peptide agonists and
Pelletier, Jeffrey C.,Chengalvala, Murty,Cottom, Josh,Feingold, Irene,Garrick, Lloyd,Green, Daniel,Hauze, Diane,Huselton, Christine,Jetter, James,Kao, Wenling,Kopf, Gregory S.,Lundquist IV, Joseph T.,Mann, Charles,Mehlmann, John,Rogers, John,Shanno, Linda,Wrobel, Jay
p. 6617 - 6640
(2008/12/22)

PYRIDAZINE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS
Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula (I) indicates a single bond or a double bond; X is O, S or N-R5; R1, R2 are independently selected from the group consisting of H, NH2, NH-C1-C6-alkyl, OH, =O, (i.e. a carbonyl group), C1-C6-alkoxy, halogen, methyl, C2-C4-alkyl, C3- C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, formyl, C1-C3-alkylcarbonyl, and an aromatic radical Ar, R1 and R2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and O, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1 , 2 or 3 substituents selected, independently of each other, from the group of radicals R4 as defined below; R3 is hydrogen OH, halogen, CN, nitro, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6- hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, fluorinated C3-C7-cycloalkyl, C1-C6-alkoxy, C1-C6- hydroxyalkoxy, C1C6-alkoxy-C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6- alkylthio, fluorinated-C1-C6 alkylthio, C1C6-alkylsulfinyl, fluorinated C1-C6- alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6 alkylsulfonyl, C1C6- alkylcarbonyl, fluorinated C1C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, fluorinated C1-C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, NRaRb, C(O)-NReRf, NH-C(O)-N ReRf, NRaRb-C1-C6-alkylene, O-NRaRb, etc. and wherein R4 and R5 are as defined in the specification and the claims.
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Page/Page column 28; 33

(2010/11/25)

SUBSTITUTED DIHYDROPYRIDINES AND METHODS OF USE
Compounds are provided that are modulators of the C5a receptor. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of C5a receptors.
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Page/Page column 132

(2010/11/27)

NOVEL DUAL ACTION RECEPTORS ANTAGONISTS (DARA) AT THE AT1 AND ETA RECEPTORS
The present invention relates to new compounds of the formula [Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, R3, and R31 are as specified herein. The invention also relates to a method for preparation thereof, as well as combinations of the new compounds with previously known agents. The invention also relates to the use of the above-mentioned compounds and combinations for the preparation of a medicament for treating hypertension of different kinds, alleviating organ damage of different kinds, treating or preventing diabetic nephropathy, treating endothelin and angiotensin mediated disorders, and treating prostate cancer.
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Page/Page column 252-253

(2010/11/28)

Process development for ABT-472, a benzimidazole PARP inhibitor
A nine-step convergent process was developed for the synthesis of ABT-472, a benzimidazole PARP inhibitor. The identity and origin of several impurities were determined, and the process was modified to reduce or eliminate these impurities. A number of safety and control issues were investigated. The original synthesis was shortened to 9 steps and streamlined while maintaining a convergent strategy. A stable salt was selected, and control of the API solid form was established. The process was successfully scaled up to provide 8.5 kg of final product of >99% purity in 33% yield over 9 steps.
Barkalow, Jufang H.,Breting, Jeffrey,Gaede, Bruce J.,Haight, Anthony R.,Henry, Rodger,Kotecki, Brian,Mei, Jianzhang,Pearl, Kurt B.,Tedrow, Jason S.,Viswanath, Shekhar K.
p. 693 - 698
(2012/12/29)

Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles
Four classes of UK-1 analogues were synthesized and their cytotoxicity testing against human A-549, BFTC-905, RD, MES-SA, and HeLa carcinoma cell lines was determined. The results revealed that UK-1 and four of these analogues (15-18) are potent against the cancer cell lines. In particular, compound 16 is more potent than UK-1 against A-549 and HeLa cell lines, and compounds 15, 17, and 18 selectively exhibit potent cytotoxic activity against the BFTV-905 cells (IC50 9.6 μM), A-549 cells (IC50 6.6 μM), and MES-SA cells (IC50 9.2 μM), respectively.
Huang, Shu-Ting,Hsei, I-Jen,Chen, Chinpiao
p. 6106 - 6119
(2007/10/03)

Synthesis and antiviral activity against Coxsackie virus B3 of some novel benzimidazole derivatives
Some benzimidazole derivatives were synthesized and the antiviral evaluation against Coxsackie virus B3 is reported. These compounds are proved to be excellent inhibitors of CVB3. Some benzimidazole derivatives were synthesized and evaluated for their antiviral properties. Compounds 20 and 21 showed potent selective activity against Coxsackie virus B3 in VERO cells. Some structure-activity relationships were discussed.
Cheng, Jun,Xie, Jiangtao,Luo, Xianjin
p. 267 - 269
(2007/10/03)

Nicotinamide derivatives useful as PDE4 inhibitors
This invention relates to nicotinamide derivatives of general formula (I): in which R1, R2 and R3 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
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Page 17

(2010/02/10)

PIPERIDINE DERIVATIVES HAVING CCR3 ANTAGONISM
The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.
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Page 434-435

(2008/06/13)

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: Discovery and preliminary SAR of benzimidazole derivatives
Benzimidazole 5-carboxamide derivatives from a combinatorial screening library were discovered as specific inhibitors of the NS5B polymerase of the hepatitis C virus (HCV). Initial hit-to-lead activities taking advantage of high-throughput parallel synthetic techniques, identified a 1,2-disubstituted benzimidazole 5-carboxylic acid scaffold as the minimum core for biological activity. Potent analogues in this series inhibit the polymerase at low micromolar concentrations and provide an attractive 'drug-like' lead structure for further optimization and the development of potential HCV therapeutics.
Beaulieu, Pierre L.,Boes, Michael,Bousquet, Yves,Fazal, Gulrez,Gauthier, Jean,Gillard, James,Goulet, Sylvie,LaPlante, Steven,Poupart, Marc-Andre,Lefebvre, Sylvain,McKercher, Ginette,Pellerin, Charles,Austel, Volkhard,Kukolj, George
p. 119 - 124
(2007/10/03)

Cyclo-alkyl substituted benzimidazoles and their use as PARP inhibitors
Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.
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Page column 10

(2008/06/13)

XANTHINE OXIDASE INHIBITORS
The invention relates to compounds of the following formula (I) or their salts: in which R1 represents OR4 or others, in which R4 is an alkyl group having 1-8 carbon atoms which may have a substituent or the like; R2 is halogen, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur, in which R11 is hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CR12 or nitrogen, in which R12 has the same meaning as R3 above, and a xanthine oxidase inhibitor containing the compound as an active ingredient.
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(2010/02/08)

IMIDAZO(1,2-a)PYRIDINE DERIVATIVE
A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
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Page 106; 107

(2010/02/09)

Substituted benzimidazoles
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
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(2008/06/13)

Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase
The nuclear enzyme poly(ADP-ribose) polymerase (PARP) facilitates the repair of DNA strand breaks and is implicated in the resistance of cancer cells to certain DNA-damaging agents. Inhibitors of PARP have clinical potential as resistance-modifying agents capable of potentiating radiotherapy and the cytotoxicity of some forms of cancer chemotherapy. The preclinical development of 2-aryl-1H-benzimidazole-4-carboxamides as resistance-modifying agents in cancer chemotherapy is described. 1H-Benzimidazole-4-carboxamides, particularly 2-aryl derivatives, are identified as a class of potent PARP inhibitors. Derivatives of 2-phenyl-1H-benzimidazole-4-carboxamide (23, K(i) = 15 nM), in which the phenyl ring contains substituents, have been synthesized. Many of these derivatives exhibit K(i) values for PARP inhibition 10 nM, with 2-(4-hydroxymethylphenyl)-1H-benzimidazole-4-carboxamide (78, K(i) = 1.6 nM) being one of the most potent. Insight into structure-activity relationships (SAR) for 2-aryl-1H-benzimidazole-4-carboxamides has been enhanced by studying the complex formed between 2-(3-methoxyphenyl)-1H-benzimidazole-4-carboxamide (44, K(i) = 6 nM) and the catalytic domain of chicken PARP. Important hydrogen-bonding and hydrophobic interactions with the protein have been identified for this inhibitor. 2-(4-Hydroxyphenyl)-1H-benzimidazole-4-carboxamide (45, K(i) = 6 nM) potentiates the cytotoxicity of both temozolomide and topotecan against A2780 cells in vitro (by 2.8- and 2.9-fold, respectively).
White,Almassy,Calvert,Curtin,Griffin,Hostomsky,Maegley,Newell,Srinivasan,Golding
p. 4084 - 4097
(2007/10/03)

Benzimidazole compounds
Benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.
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(2008/06/13)

A convenient copper-catalyzed direct animation of nitroarenes with 9-alkylhydroxylamines
O-Alkylhydroxylamines, particularly O-methylhydroxylamine, aminate nitroarenes in the presence of a strong base and a copper catalyst to give aminonitroarenes in good yields, ortho- or para-Animation with respect to the nitro group takes place, and in some cases the ortho-aminated product is preferentially obtained. With 3-substituted nitrobenzenes where the substituent has a lone pair of electrons, preferential amination occurs at the 2-position to give the sterically most congested 3c-f, 14 and 22g.
Seko, Shinzo,Miyake, Kunihito,Kavvamura, Norio
p. 1437 - 1444
(2007/10/03)

Stereoselective synthesis of tilivalline
Tilivalline 1, a metabolite from Klebsiella pneumoniae var. ocytoca, was easily synthesized in five steps from (S)-proline and 3-(benzyloxy)isatoic anhydride 4g. This synthesis is based on modified Curtius reactions of 3- substituted phthalic anhydrides 11 to 3-substituted isatoic anhydrides 4, conversion of lactams 6 to the acyliminium precursors 7 and stereoselective introduction of indole from the less hindered side of 7.
Nagasaka, Tatsuo,Koseki, Yuji
p. 6797 - 6801
(2007/10/03)

High-affinity α-aminobutyric acid A/benzodiazepine ligands: Synthesis and structure - Activity relationship studies of a new series of tetracyclic imidazoquinoxalines
A series of tetracyclic imidazoquinoxaline analogs was developed which constrain the carbonyl group of the partial agonist 3-(5-cyclopropyl-1,2,4- oxadiazol-3-yl)-5-[(dimethylamino)carbonyl]4,5-dihydroimidazo[1,5- a]quinoxaline (2, U-91571) away from the benzene ring. These analogs orient the carbonyl group in the opposite direction of the previously reported full agonist 1-(5-cyclopropyl- 1,2,4-oxadiazol-3-yl)- 12,12a-dihydroimidazo[1,5- a]pyrrolo[2,1-c]quinoxalin- 10(11H)one (3, U-89267). A number of approaches were utilized to form the 'bottom' ring of this tetracyclic ring system including intramolecular cyclizations promoted by Lewis acids or base, as well as metal-carbenoid conditions. The size and substitution pattern of the additional ring was widely varied. Analogs within this series had high affinity for the benzodiazepine receptor on the α-aminobutyric acid A chloride ion channel complex. From TBPS shift and Cl- current assays, the in vitro efficacy of compounds within this class ranged from antagonists to partial agonists with only 18a identified as a full agonist. Additionally, several analogs were quite potent at antagonizing metrazole-induced seizures indicating possible anticonvulsant or anxiolytic activity. Unlike 3, analogs in this series did not have high affinity for the diazepam insensitive α6β2δ2 subtype. These results suggest that either constraining the carbonyl group away from the benzene ring or the greater planarity that results from the additional cyclic structure provides analogs with partial agonist properties and prevents effective interaction with the α6β2δ2 subtype.
Mickelson, John W.,Jacobsen, E. Jon,Carter, Donald B.,Im, Haesook K.,Im, Wha Bin,Schreur, Peggy J. K. D.,Sethy, Vimala H.,Tang, Andy H.,McGee, James E.,Petke, James D.
p. 4654 - 4666
(2007/10/03)

Imidazo[1,5-A]quinoxalines
An invention relating to Imidazo[1,5-a]quinoxalines (I) STR1 which do not contain an endocyclic carbonyl group and which are useful as anxiolytic and sedative/hypnotic agents.
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(2008/06/13)

Imidazopyridine derivatives as angiotensin II receptor antagonists, pharmaceuticals, and treatment of hypertension therewith
Imidazo-fused iso- and heterocycles, process for their preparation, compositions containing them and their useA compound of the formula STR1 in which the symbols have the following meaning: X is a monocyclic radical having 3,4 or 5 ring atoms,R 1,R 2,R 3,
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(2008/06/13)

Structure-activity relationships of imidazo[4,5-f]quinoline partial structures and analogs. Discovery of pyrazolo[3,4-f]quinoline derivatives as potent immunostimulants
Structure-activity studies have been carried out on a series of imidazo[4,5-f]quinoline derivatives reported to have potent in vivo immunostimulatory activity. This activity has been confirmed, and subtle structure-activity relationships have been uncovered which resulted in the identification of novel analogs (pyrazolo[3,4-f]quinoline derivatives, 7a,b) with potent in vivo effects in a mouse protection model. Regioisomeric pyrazolo[4,3-f]quinoline derivatives (6a,b) were shown to be inactive. Data are presented which support the notion that the in vivo activity is mediated by an immunostimulatory mechanism.
Moyer,Weber,Gross
p. 4595 - 4601
(2007/10/02)

Potential Antitumor Agents. 59. Structure-Activity Relationships for 2-Phenylbenzimidazole-4-carboxamides, a New Class of "Minimal" DNA-Intercalating Agents Which May Not Act via Topoisomerase II
A series of substituted 2-phenylbenzimidazole-4-carboxamides has been synthesized and evaluated for in vitro and in vivo antitumor activity.These compounds represent the logical conclusion to our search for "minimal" DNA-intercalating agents with the lowest possible DNA-binding constants.Such "2-1" tricyclic chromophores, of lower aromaticity than the structurally similar 2-phenylquinolines, have the lowest DNA binding affinity yet seen in the broad series of tricyclic carboxamide intercalating agents.Despite very low in vitro cytotoxicities, several of the compoundshad moderate levels of in vivo antileukemic effects.However, the most interesting aspect of their biological activity was the lack of cross-resistance shown to an amsacrine-resistant P388 cell line, suggesting that these compounds may not express their cytotoxicity via interaction with topoisomerase II.
Denny, William A.,Rewcastle, Gordon W.,Baguley, Bruce C.
p. 814 - 819
(2007/10/02)

OXIDATIVE DEGRADATION OF 8-NITROQUINOLINE WITH HYDROGEN PEROXIDE IN ACETIC ACID --- A POSSIBLE MECHANISM THROUGH 3,4-EPOXIDE OF QUINOLINE RING
The treatment of 8-nitroquinoline with hydrogen peroxide and acetic acid at 60 grad C afforded 7-nitroindole, 7-nitro-2-oxindole, 2-amino-3-nitrobenzoic acid, 2-amino-3-nitrobenzaldehyde, 3,4-dihydro-3,4-trans-dihydroxy-8-nitrocarbostyril, 3,4-trans-dihyd
Kaiya, Toyo,Kawazoe, Yutaka
p. 511 - 518
(2007/10/02)

Chemical Properties

Appearance/Colour :WHITE TO BROWN SOLID, POWDER, CRYSTALS, CRYSTALLINE POWDER, AND/OR CHUNKS
Melting Point: 207-211 °C
Boiling Point: 390.4 °C at 760 mmHg
Flash Point:189.9 °C
Density: 1.568 g/cm³
Solubility:DMSO, Methanol
Storage Temp.:Refrigerator
Vapor Pressure: 8.55E-07mmHg at 25°C
Refractive Index: 1.5880 (estimate)
PKA: 4.20±0.20(Predicted)
PSA: 109.14000
LogP: 1.97960

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Henan Sinotech Import&Export Corporation
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Henan Wentao Chemical Product Co., Ltd.
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Shanghai Upbio Tech Co.,Ltd
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Wuhan Wonda Pharm Limited
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Wuhan Han Sheng New Material Technology Co.，Ltd
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Xiamen Hisunny Chemical Co.,Ltd
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Hangzhou Keyingchem Co.,Ltd
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Ality Chemical Corporation
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Hangzhou J&H Chemical Co., Ltd.
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SHANGHAI SYSTEAM BIOCHEM CO., LTD
Business Type:Lab/Research institutions
Min Order:100 Gram
FOB Price:USD $ 100.0-2000.0 / Gram
Main Products:24
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HANGZHOU YUNUO CHEMICAL CO.,LTD
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Siwei Development Group Ltd.
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Article Database

606-18-8

Articles about 606-18-8Total 34 be found

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Chemical Properties

Appearance/Colour :WHITE TO BROWN SOLID, POWDER, CRYSTALS, CRYSTALLINE POWDER, AND/OR CHUNKS

Melting Point: 207-211 °C

Boiling Point: 390.4 °C at 760 mmHg

Flash Point:189.9 °C

Density: 1.568 g/cm³

Solubility:DMSO, Methanol

Storage Temp.:Refrigerator

Vapor Pressure: 8.55E-07mmHg at 25°C

Refractive Index: 1.5880 (estimate)

PKA: 4.20±0.20(Predicted)

PSA: 109.14000

LogP: 1.97960

Global suppliers and manufacturers of 606-18-8total 116 suppliers on LookChem

Article Database

606-18-8

Articles about 606-18-8Total 34 be found

More Articles about upstream products of 606-18-8

More Articles about downstream products of 606-18-8

Chemical Properties

Appearance/Colour :WHITE TO BROWN SOLID, POWDER, CRYSTALS, CRYSTALLINE POWDER, AND/OR CHUNKS

Melting Point: 207-211 °C

Boiling Point: 390.4 °C at 760 mmHg

Flash Point:189.9 °C

Density: 1.568 g/cm3

Solubility:DMSO, Methanol

Storage Temp.:Refrigerator

Vapor Pressure: 8.55E-07mmHg at 25°C

Refractive Index: 1.5880 (estimate)

PKA: 4.20±0.20(Predicted)

PSA: 109.14000

LogP: 1.97960

Global suppliers and manufacturers of 606-18-8total 116 suppliers on LookChem

Density: 1.568 g/cm³