cas 13720-94-0, ETHYL 4-CHLORO-3-QUINOLINECARBOXYLATE

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A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease
2-(piperazin-1-yl)–N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides are described as a new class of selective and potent acetylcholinesterase (AChE) inhibitors and amyloid β aggregation inhibitors. Formation of synthesized compounds (P1–P9) was justified via H1 NMR, C13 NMR, mass spectra and single crystal X-Ray diffraction study. All compounds were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity, inhibition of self-mediated Aβ aggregation and Cu(II)-mediated Aβ aggregation. Also, docking study carried out was in concordance with in vitro results. The most potent molecule amongst the derivatives exhibited excellent anti-AChE activity (IC50 = 4.8 nM). Kinetic study of P3 suggested it to be a mixed type inhibitor. In vitro study revealed that all the compounds are capable of inhibiting self-induced β-amyloid (Aβ) aggregation with the highest inhibition percentage to be 81.65%. Potency of P1 and P3 to inhibit self-induced Aβ1-42 aggregation was ascertained by TEM analysis. Compounds were also evaluated for their Aβ disaggregation, antioxidation, metal-chelation activity.
Umar, Tarana,Shalini, Shruti,Raza, Md Kausar,Gusain, Siddharth,Kumar, Jitendra,Seth, Prerna,Tiwari, Manisha,Hoda, Nasimul
p. 2 - 19
(2019)
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PANICINOTAM DERIVATIVE, PREPARATION METHOD AND USE THEREOF
Provided are penicinotam derivatives, a tautomer, a stereoisomer, a racemate, a nonequal mixture of enantiomers, a geometric isomer, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, and a pharmaceutical composition comprising the deriva
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Paragraph 0184; 0186

(2021/01/25)

Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights
Aurora kinases (AURKs) were identified as promising druggable targets for targeted cancer therapy. Aiming at the development of novel chemotype of dual AURKA/B inhibitors, herein we report the design and synthesis of three series of 4-anilinoquinoline derivatives bearing a sulfonamide moiety (5a-d, 9a-d and 11a-d). The percent inhibition of AURKA/B was determined for all target quinolines, then compounds showed more than 50percent inhibition on either of the enzymes, were evaluated further for their IC50 on the corresponding enzyme. In particular, compound 9d displayed potent AURKA/B inhibitory activities with IC50 of 0.93 and 0.09 μM, respectively. Also, 9d emerged as the most efficient anti-proliferative analogue in the US-NCI anticancer assay toward the NCI 60 cell lines panel, with broad spectrum activity against different cell lines from diverse cancer subpanels. Docking studies, confirmed that, the sulfonamide SO2 oxygen was involved in a hydrogen bond with Lys162 and Lys122 in AURKA and AURKB, respectively, whereas, the sulfonamide NH could catch hydrogen bond interaction with the surrounding amino acid residues Lys141, Glu260, and Asn261 in AURKA and Lys101, Glu177, and Asp234 in AURKB. Furthermore, N1 nitrogen of the quinoline scaffold formed an essential hydrogen bond with the hinge region key amino acids Ala213 and Ala173 in AURKA and AURKB, respectively.
Abdelgawad, Mohamed A.,Al-Sanea, Mohammad M.,Alharbi, Khalid S.,Ali Farahat, Ibrahim,Alzarea, Abdulaziz I.,Alzarea, Sami I.,Bakr, Rania B,El Kerdawy, Ahmed M.,Eldehna, Wagdy M.,Elkamhawy, Ahmed,Elshemy, Heba A. H.,Joo Roh, Eun,Lee, Kyeong,Paik, Sora,Syed Nasir Abbas, Bukhari
(2020/05/08)

Cyclopropanation–ring expansion of 3-chloroindoles with α-halodiazoacetates: Novel synthesis of 4-quinolone-3-carboxylic acid and norfloxacin
We present a short and efficient way of synthesizing two synthetically versatile 4-quinolone-3-carboxylate building blocks by cyclopropanation-ring expansion of 3-chloroindoles with α-halodiazoacetates as the key step. This novel transformation was applied towards the synthesis of the antibiotic drug norfloxacin.
Peeters, Sara,Berntsen, Linn Neerbye,Rongved, P?l,Bonge-Hansen, Tore
supporting information
p. 2156 - 2160
(2019/09/30)

4 - Amino quinoline -3 - a ester derivative and its preparation method and application
The invention provides a 4 - substituted amino quinoline - 3 - carboxylic acid ester derivative and its preparation method and application, 4 - amino quinoline - 3 - carboxylic acid ester derivative of the general formula: . The compounds in vitro demonstrates very good anti-tumor activity, can be applied to the preparation of anti-tumor drug.
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(2019/05/15)

Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino)benzenesulfonamidesAQ3 as carbonic anhydrase isoforms I and II inhibitors
Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes that are involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel series of benzenesulfonamides incorporating un/substituted ethyl quinoline-3-carboxylate moieties. The newly synthesised compounds were in vitro evaluated as inhibitors of the cytosolic human (h) isoforms hCA I and II. Both isoforms hCA I and II were inhibited by the quinolines reported here in variable degrees: hCA I was inhibited with KIs in the range of 0.966–9.091 μM, whereas hCA II in the range of 0.083–3.594 μM. The primary 7-chloro-6-flouro substituted sulphfonamide derivative 6e (KI = 0.083 μM) proved to be the most active quinoline in inhibiting hCA II, whereas, its secondary sulfonamide analog failed to inhibit the hCA II up to 10 μM, confirming the crucial role of the primary sulphfonamide group, as a zinc-binding group for CA inhibitory activity.
Al-Sanea, Mohammad M.,Elkamhawy, Ahmed,Paik, Sora,Bua, Silvia,Ha Lee, So,Abdelgawad, Mohamed A.,Roh, Eun Joo,Eldehna, Wagdy M.,Supuran, Claudiu T.
p. 1457 - 1464
(2019/08/26)

Tetracyclic lactam compound, preparation method and application thereof
The invention relates to a tetracyclic lactam compound, or a tautomer, a stereisomer, racemate, a non-equivalent mixture of an enantiomer, a geometrical isomer, a solvate, medically acceptable salt orprodrug thereof, and a drug combination containing the same. The invention further discloses application of the tetracyclic lactam compound or the drug combination serving as drugs, particularly as antibacterial, antiviral and antiparasitic drugs.
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Paragraph 0142; 0149

(2018/10/19)

Method for preparing penicinotam compound
The invention belongs to the field of organic synthesis and in particular relates to a method for preparing a penicinotam compound. The method comprises the following steps: by taking phenylamine andethoxy methylene propane dioic acid dio-ethylest as initial raw materials, carrying out a condensation reaction, carrying out a Gould-Jacob reaction so as to form a quinoline mother ring, further carrying out a bromo- and Suzuki reaction so as to obtain a 2-(1-(t-butyloxycarboryl)-1H-pyrrole-2-yl)-4-chloroquinoline-3-ethyl formate intermediate, and finally carrying out a ring closing reaction, thereby obtaining a target product, namely the penicinotam.
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Page/Page column 7

(2018/10/27)

Method for preparing penicinoline compound
The invention discloses a method for preparing a penicinoline compound and belongs to the field of organic synthesis. The method comprises the following steps: by taking phenylamine and ethoxy methylene propane dioic acid dio-ethylest as initial raw materials, carrying out a condensation reaction, carrying out a Gould-Jacob reaction so as to form a quinoline mother ring, further carrying out a bromo- and Suzuki reaction so as to obtain a 2-(1-(t-butyloxycarboryl)-1H-pyrrole-2-yl)-4-chloroquinoline-3-ethyl formate intermediate, and finally carrying out hydrolysism obtaining penicinoline.
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Paragraph 0015

(2018/10/19)

Panicinotam analog and preparation method and use thereof
The present invention relates to a panicinotam analog, or a tautomer, a stereoisomer, a raceme, a non-equivalent mixture of enantiomers, a geometrical isomer, a solvate, a pharmaceutically-acceptablesalt or a prodrug thereof, and a pharmaceutical composition comprising the panicinotam analog. The present invention also provides use of the panicinotam analog or the pharmaceutical composition serving as drugs, and especially as antivirus, antibacterial and antiparasitic drugs.
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Paragraph 0144; 0145

(2018/11/04)

Quinolinone alkaloid compounds as well as preparation method and application thereof
The invention relates to quinolinone alkaloid compounds, or a heterogeneous mixture of a tautomer, a stereisomer, a raceme and an enantiomer, a geometrical isomer, a solvate, pharmaceutically acceptable salt or prodrug as well as a medicinal composition containing the compounds. The invention also discloses application of the compounds and the medicinal composition serving as medicines, particularly serving as agricultural insecticide, bactericidal and herbicide medicines.
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Paragraph 0067

(2018/10/19)

Quinolinone acid derivatives as well as preparation method and application thereof
The invention relates to quinolinone acid derivatives, or a heterogeneous mixture of a tautomer, a stereisomer, a raceme and an enantiomer, a geometrical isomer, a solvate, pharmaceutically acceptablesalt or prodrug as well as a medicinal composition containing the compounds. The invention also discloses application of the compounds and the medicinal composition serving as medicines, particularlyserving as antituberculous and antiparasitic medicines.
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Page/Page column 36-37

(2018/10/27)

A four-ring quinolinone alkaloid derivative and its preparation method and application (by machine translation)
The invention relates to a four-ring quinolinone alkaloid derivative, or a tautomer thereof, stereo isomer, racemate, enantiomer of non-isometric mixture, geometric isomer, solvate, pharmaceutically acceptable salt or prodrug, and pharmaceutical composition containing the compound. The invention also discloses such compounds and pharmaceutical compositions thereof as a medicament, in particular as anti-virus, antibacterial and the anti-parasitic drug use. (by machine translation)
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Paragraph 0193; 0200; 0207

(2018/10/27)

Lactam-containing tetracyclic derivative as well as preparation method and application thereof
The invention relates to a lactam-containing tetracyclic derivative, or a heterogeneous mixture of a tautomer, a stereoisomer, a raceme and an enantiomer of the lactam-containing tetracyclic derivative, a geometrical isomer, a solvate, medically acceptable salt or a prodrug, and a drug composition containing the compound. The invention further discloses use of the compound and the drug compositionthereof as an insecticide, a bactericide and a herbicide in the agricultural field.
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Paragraph 0065; 0066; 0072-0073; 0079; 0080; 0086-0087; 0093

(2018/10/27)

Potent Antimalarial 2-Pyrazolyl Quinolone bc1 (Qi) Inhibitors with Improved Drug-like Properties
A series of 2-pyrazolyl quinolones has been designed and synthesized in 5-7 steps to optimize for both in vitro antimalarial potency and various in vitro drug metabolism and pharmacokinetics (DMPK) features. The most potent compounds display no cross-resistance with multidrug resistant parasite strains (W2) compared to drug sensitive strains (3D7), with IC50 (concentration of drug required to achieve half maximal growth suppression) values in the range of 15-33 nM. Furthermore, members of the series retain moderate activity against the atovaquone-resistant parasite isolate (TM90C2B). The described 2-pyrazoyl series displays improved DMPK properties, including improved aqueous solubility compared to previously reported quinolone series and acceptable safety margin through in vitro cytotoxicity assessment. The 2-pyrazolyl quinolones are believed to bind to the ubiquinone-reducing Qi site of the parasite bc1 complex, which is supported by crystallographic studies of bovine cytochrome bc1 complex.
David Hong,Leung, Suet C.,Amporndanai, Kangsa,Davies, Jill,Priestley, Richard S.,Nixon, Gemma L.,Berry, Neil G.,Samar Hasnain,Antonyuk, Svetlana,Ward, Stephen A.,Biagini, Giancarlo A.,O'Neill, Paul M.
p. 1205 - 1210
(2018/11/23)

Synthesis and preliminary structure-activity relationship study of 2-aryl-2H-pyrazolo[4,3-c]quinolin-3-ones as potential checkpoint kinase 1 (Chk1) inhibitors
The serine-threonine checkpoint kinase 1 (Chk1) plays a critical role in the cell cycle arrest in response to DNA damage. In the last decade, Chk1 inhibitors have emerged as a novel therapeutic strategy to potentiate the anti-tumour efficacy of cytotoxic chemotherapeutic agents. In the search for new Chk1 inhibitors, a congeneric series of 2-aryl-2 H-pyrazolo[4,3-c]quinolin-3-one (PQ) was evaluated by in-vitro and in-silico approaches for the first time. A total of 30 PQ structures were synthesised in good to excellent yields using conventional or microwave heating, highlighting that 14 of them are new chemical entities. Noteworthy, in this preliminary study two compounds 4e2 and 4h2 have shown a modest but significant reduction in the basal activity of the Chk1 kinase. Starting from these preliminary results, we have designed the second generation of analogous in this class and further studies are in progress in our laboratories.
Malvacio, Ivana,Cuzzolin, Alberto,Sturlese, Mattia,Vera, D. Mariano A.,Moyano, E. Laura,Moro, Stefano
p. 171 - 183
(2017/12/26)

4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation
Mycobacterial DNA gyrase B subunit has been identified to be one of the potentially underexploited drug targets in the field of antitubercular drug discovery. In the present study, we employed structural optimization of the reported GyrB inhibitor resulting in synthesis of a series of 46 novel quinoline derivatives. The compounds were evaluated for their in vitro Mycobacterium smegmatis GyrB inhibitory ability and Mycobacterium tuberculosis DNA supercoiling inhibitory activity. The antitubercular activity of these compounds was tested over Mtb H37Rv strain and their safety profile was checked against mouse macrophage RAW 264.7 cell line. Among all, three compounds (23, 28, and 53) emerged to be active displaying IC50 values below 1 μM against Msm GyrB and were found to be non-cytotoxic at 50 μM concentration. Compound 53 was identified to be potent GyrB inhibitor with 0.86 ± 0.16 μM and an MIC (minimum inhibitory concentration) of 3.3 μM. The binding affinity of this compound towards GyrB protein was analysed by differential scanning fluorimetry which resulted in a positive shift of 3.3 °C in melting temperature (Tm) when compared to the native protein thereby reacertaining the stabilization effect of the compound over protein.
Medapi, Brahmam,Suryadevara, Priyanka,Renuka, Janupally,Sridevi, Jonnalagadda Padma,Yogeeswari, Perumal,Sriram, Dharmarajan
p. 1 - 16
(2015/09/02)

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-Dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators
Results from a 2012 high-throughput screen of the NIH Molecular Libraries Small Molecule Repository (MLSMR) against the human muscarinic receptor subtype 1 (M1) for positive allosteric modulators is reported. A content-rich screen utilizing an intracellular calcium mobilization triple-addition protocol allowed for assessment of all three modes of pharmacology at M1, including agonist, positive allosteric modulator, and antagonist activities in a single screening platform. We disclose a dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-one hit (DBPQ, CID 915409) and examine N-benzyl pharmacophore/SAR relationships versus previously reported quinolin-3(5H)-ones and isatins, including ML137. SAR and consideration of recently reported crystal structures, homology modeling, and structure-function relationships using point mutations suggests a shared binding mode orientation at the putative common allosteric binding site directed by the pendant N-benzyl substructure.
Han, Changho,Chatterjee, Arindam,Noetzel, Meredith J.,Panarese, Joseph D.,Smith, Emery,Chase, Peter,Hodder, Peter,Niswender, Colleen,Jeffrey Conn,Lindsley, Craig W.,Stauffer, Shaun R.
p. 384 - 388
(2015/04/13)

Two-face, two-turn α-helix mimetics based on a cross-acridine scaffold: Analogues of the bim BH3 domain
The design of a cross-acridine scaffold mimicking the i, i+3, i+5, and i+7 residues distributed over a two-face, two-turn α-helix is described. Docking studies and 2D 1H,15N HSQC NMR spectroscopy provide compelling evidence that compound 3-d accurately reproduces the arrangement of four hotspots in the Bim BH3 peptide to permit binding to the Mcl-1 and Bcl-2 proteins (Ki 0.079 and 0.056 μM, respectively). Furthermore, the hotspot mutation could also be mimicked by individual or multiple deletions of side chains on the scaffold. Building site: A cross-acridine scaffold was designed to project functional groups with spatial and angular geometries that accurately mimic the i, i+3, i+5, and i+7 side chains on a two-turn, two-face section of an α-helix. The binding mode of the most potent compound, 3-d, to Mcl-1 was confirmed by 1H, 15N HSQC NMR.
Li, Xiangqian,Wang, Ziqian,Feng, Yingang,Song, Ting,Su, Pengchen,Chen, Chengbin,Chai, Gaobo,Yang, Ying,Zhang, Zhichao
p. 1280 - 1285
(2014/06/24)

Quinoline Compounds, Intermediates, Preparation Methods and Uses Thereof
A kind of quinoline compounds as formula A, pharmaceutical accepted solvates, optical isomers or polymorphisms thereof. The intermediates of formula D. in which, R1, R2 and R3 is independently H, halo or the subustitents o
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Page/Page column 5

(2011/04/14)

Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)- 8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones
A series of 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c] quinolin-3(5H)-ones (3a-g) have been synthesized and evaluated for their in vitro antiproliferative activities against four human cancer cell lines: MDA-MB-435 (breast), HL-60 (leukemia), HCT-8 (colon) and SF-295 (central nervous system). The results showed that the compounds 3b (2-(benzo[d]thiazol-2-yl)-8- methyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-one) and 3c (2-(benzo[d]thiazol-2-yl)-8- bromo-2H-pyrazolo[4,3-c]quinolin-3(5H)-one) exhibited good cytotoxicity for three cell lines with IC50 values lower than 5 μg/mL. Analysis of theoretical toxicity risks have shown medium tumorigenic and irritant risks related to 3b and 3c in contrast to doxorubicin, the positive control.
Reis, Raísa Da R.,Azevedo, Elisa C.,De Souza, Maria Cecília B.V.,Ferreira, Vitor Francisco,Montenegro, Raquel C.,Araújo, Ana Jérsia,Pessoa, Cláudia,Costa-Lotufo, Letícia V.,De Moraes, Manoel O.,Filho, José D.B.M.,De Souza, Alessandra M.T.,De Carvalho, Natasha C.,Castro, Helena C.,Rodrigues, Carlos R.,Vasconcelos, Thatyana R.A.
p. 1448 - 1452
(2011/04/24)

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRβ and low blood-brain penetration
A series of quinoline-3-carboxamide containing sulfones was prepared and found to have good binding affinity for LXRβ and moderate binding selectivity over LXRα. The 8-Cl quinoline analog 33 with a high TPSA score, displayed 34-fold binding selectivity for LXRβ over LXRα (LXRβ IC50 = 16 nM), good activity for inducing ABCA1 gene expression in a THP macrophage cell line, desired weak potency in the LXRα Gal4 functional assay, and low blood-brain barrier penetration in rat.
Hu, Baihua,Bernotas, Ron,Unwalla, Rayomand,Collini, Michael,Quinet, Elaine,Feingold, Irene,Goos-Nilsson, Annika,Wilhelmsson, Anna,Nambi, Ponnal,Evans, Mark,Wrobel, Jay
scheme or table
p. 689 - 693
(2010/06/14)

PYRAZOLOQUINOLINE AND PYRAZOLONAPHTHYRIDINE DERIVATIVES AS GABA ALPHA LIGANDS
The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free base form or in acid addition salt form; to its preparation, to its use as medicament and to medicaments comprising it.
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Page/Page column 19

(2009/04/25)

THERAPEUTIC PYRAZOLOQUINOLINE UREA DERIVATIVES
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment
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Page/Page column 17

(2009/01/20)

New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists
A series of new 1,8-naphthyridine and quinoline derivatives were synthesized and evaluated for their cannabinoid receptor affinity. In particular, compounds 2, 5, 11, and 13 showed a high CB2 affinity and CB2 versus CB1 selectivity, in agreement with molecular modeling studies. Furthermore, compound 2 also exhibited in vivo antinociceptive effects.
Manera, Clementina,Cascio, Maria Grazia,Benetti, Veronica,Allara, Marco,Tuccinardi, Tiziano,Martinelli, Adriano,Saccomanni, Giuseppe,Vivoli, Elisa,Ghelardini, Carla,Di Marzo, Vincenzo,Ferrarini, Pier Luigi
p. 6505 - 6510
(2008/09/20)

Structure-activity relationship of quinoline derivatives as potent and selective α2c-adrenoceptor antagonists
Starting from two acridine compounds identified in a high-throughput screening campaign (1 and 2, Table 1), a series of 4-aminoquinolines was synthesized and tested for their properties on the human α2- adrenoceptor subtypes (α2A, α2B, and α2C). A number of compounds with good antagonist potencies against the α2C-adrenoceptor and excellent subtype selectivities over the other two subtypes were discovered. For example, (R)-{4-[4-(3,4-dimethylpiperazin-1-yl)phenylamino]quinolin-3-yl}methanol 6j had an antagonist potency of 8.5 nM against, and a subtype selectivity of more than 200-fold for, the α2c-adrenoceptor. Investigation of the structure-activity relationship identified a number of structural features, the most critical of which was an absolute need for a substituent in the 3-position of the quinoline ring. The 3-position on the piperazine ring was also found to play an appreciable role, as substitutions in that position exerted a significant and stereospecific beneficial effect on the α2C- adrenoceptor affinity and potency. Replacing the piperazine ring proved difficult, with 1,4-diazepanes representing the only viable alternative.
H?glund, Iisa P. J.,Silver, Satu,Engstr?m, Mia T.,Salo, Harri,Tauber, Andrei,Kyyr?nen, Hanna-Kaisa,Saarenketo, Pauli,Hoffrén, Anna-Marja,Kokko, Kurt,Pohjanoksa, Katariina,Sallinen, Jukka,Savola, Juha-Matti,Wurster, Siegfried,Kallatsa, Oili A.
p. 6351 - 6363
(2007/10/03)

HETEROCYCLIC DERIVATIVES FOR TREATMENT OF HYPERLIPIDEMIA AND RELATED DISEASES
The present invention provides compositions adapted to enhance reverse cholesterol transport in mammals. The compositions are suitable for oral delivery and useful in the treatment and/or prevention of hypercholesterolemia, atherosclerosis and associated
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Page/Page column 75-76

(2010/02/15)

PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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(2008/06/13)

Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors
Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.
Zask,Gu,Albright,Du,Hogan,Levin,Chen,Killar,Sung,DiJoseph,Sharr,Roth,Skala,Jin,Cowling,Mohler,Barone,Black,March,Skotnicki
p. 1487 - 1490
(2007/10/03)

Synthesis and biological evaluation of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones, a novel series of PDE 4 inhibitors with low emetic potential and antiasthmatic properties
A novel series of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones has been prepared. These compounds showed good PDE 4 inhibitory activity and weak affinity for rolipram's binding site. They also exhibited a good anti-inflammatory profile without emetic side effects. (C) 2000 Published by Elsevier Science Ltd.
Crespo, Maria I.,Gracia, Jordi,Puig, Carles,Vega, Armando,Bou, Josep,Beleta, Jordi,Domenech, Teresa,Ryder, Hamish,Segarra, Victor,Palacios, Jose M.
p. 2661 - 2664
(2007/10/03)

Structure-activity relationship studies at the benzodiazepine receptor (BZR): A comparison of the substituent effects of pyrazoloquinolinone analogs
The synthesis of a series of 2-phenylpyrazolo[4,3-c]quinolin-3-one derivatives and their in vitro biological evaluation as ligands for the benzodiazepine receptor are described. The in vitro activities, as determined by an analysis of GABA shift ratios, a
Fryer,Zhang,Rios,Gu,Basile,Skolnick
p. 1669 - 1673
(2007/10/02)

Pyrazoloquinolines
2-Aryl-pyrazolo[4-3-c]quinolin-3-ones, e.g. those of the formula STR1 and pharmaceutically acceptable acyl derivatives or salts thereof, are psychoactive agents useful in the treatment of anxiety or depression.
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(2008/06/13)