Synthesis, structure, and antibacterial activity of 4-imino-1, 4-dihydrocinnoline-3-carboxylic acid and 4-oxo-1, 4-dihydrocinnoline-3-carboxylic acid derivatives as isosteric analogues of quinolones.

abstract：:In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudo...

journal_title：Archiv der Pharmazie

authors： Mohamed B,Abdel-Samii ZK,Abdel-Aal EH,Abbas HA,Shaldam MA,Ghanim AM

更新日期：2020-05-01 00:00:00

abstract：:A new class of acetamidomethylsulfonyl bis heterocycles-oxazolyl-1,3,4-oxadiazoles, -thiazolyl-1,3,4-oxadiazoles, and -imidazolyl-1,3,4-oxadiazoles were synthesized from the synthetic intermediates, methyl 2-((4-aryloxazol-2-ylcarbamoyl)methylsulfonyl)acetate, methyl 2-((4-arylthiazol-2-ylcarbamoyl)methylsulfonyl)acet...

journal_title：Archiv der Pharmazie

authors： Mahaboob Basha N,Lavanya G,Padmaja A,Padmavathi V

更新日期：2013-07-01 00:00:00

abstract：:1-deoxy-D-xylulose-5-phosphate reductoisomerase (Dxr) represents an essential enzyme of the mevalonate-independent pathway of the isoprenoid biosynthesis. Using fosmidomycin as a specific inhibitor of Dxr, this enzyme was previously validated as target for the treatment of malaria and bacterial infections. The replace...

journal_title：Archiv der Pharmazie

authors： Ortmann R,Wiesner J,Silber K,Klebe G,Jomaa H,Schlitzer M

更新日期：2007-09-01 00:00:00

abstract：:Curcumin, a phenolic compound extracted from Curcuma longa, is commonly used in Asia as a spice and pigment and has several biological functions, particularly antioxidant properties. It has been reported that curcumin exhibits bifunctional antioxidant properties related to its capability to react directly with reactiv...

journal_title：Archiv der Pharmazie

authors： Trujillo J,Granados-Castro LF,Zazueta C,Andérica-Romero AC,Chirino YI,Pedraza-Chaverrí J

更新日期：2014-12-01 00:00:00

abstract：:Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1...

journal_title：Archiv der Pharmazie

authors： Chinthaparthi RR,Bhatnagar I,Gangireddy CS,Syama SC,Cirandur SR

更新日期：2013-09-01 00:00:00

abstract：:Despite cellular complexity, a limited number of small molecules act as intracellular second messengers. Protein kinase A (PKA) is the main transducer of the information carried by cyclic adenosine monophosphate (cAMP). Recently, cellular imaging has achieved major technical advancements, although the search for more ...

journal_title：Archiv der Pharmazie

authors： Ribaudo G,Zagotto G,Ongaro A,Ricci A,Caretta A,Mucignat-Caretta C

更新日期：2020-04-01 00:00:00

abstract：:A number of C-3 spirocyclic 2-benzazepine analogs of α-phenyl-N-tert-butyl nitrone (PBN) were synthesized and tested for their activity in protecting rat brain mitochondria and dopaminergic (DA) neurons against 6-hydroxydopamine (6-OHDA), a toxin inducing destruction of the DA nigro-striatal pathway in rodent models o...

journal_title：Archiv der Pharmazie

authors： Soto-Otero R,Méndez-Álvarez E,Sánchez-Iglesias S,Labandeira-García JL,Rodríguez-Pallares J,Zubkov FI,Zaytsev VP,Voskressensky LG,Varlamov AV,de Candia M,Fiorella F,Altomare C

更新日期：2012-08-01 00:00:00

abstract：:In the present study, a novel series of polyfunctionalized imidazopyrimidines 6a-u and 9a-d were efficiently constructed by a domino reaction between 2-imino-6-substituted-2,3-dihydropyrimidin-4(1H)-ones 4a-d or 8a-c and 2-bromoacetophenones 5a-i under mild basic conditions. The synthesized series were screened for th...

journal_title：Archiv der Pharmazie

authors： Abdel-Mohsen HT,Abood A,Flanagan KJ,Meindl A,Senge MO,El Diwani HI

更新日期：2020-03-01 00:00:00

abstract：:A series of benzamide derivatives possessing potent dopamine D2 , serotonin 5-HT1A , and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. Among them, 5-(4-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)butoxy)-N-cyclopropyl-2-fluorobenzamide (4k) held the best pharmacological profile....

journal_title：Archiv der Pharmazie

authors： Xu M,Guo S,Yang F,Wang Y,Wu C,Jiang X,Zhao Q,Chen W,Tian G,Zhu F,Xie Y,Hu T,Wang Z,He Y,Shen J

更新日期：2019-04-01 00:00:00

abstract：:A new series of 4-hydroxycoumarin derivatives 3a-d was synthesized by the reaction of 3-bromo-4-hydroxy coumarin 1 with various heteroaldehydes 2a-d in good yields. The synthesized compounds were characterized on the basis of their elemental and spectral (IR, (1)H-NMR and mass spectrometry) analysis. All target compou...

journal_title：Archiv der Pharmazie

authors： Siddiqui ZN,N MM,Ahmad A,Khan AU

更新日期：2011-06-01 00:00:00

abstract：:Isatin and azole moieties, which have the ability to form various noncovalent interactions with different therapeutic targets, are common pharmacophores in drug development. Isatin and azole derivatives possess promising in vitro and in vivo anticancer activity, and many of them, such as semaxanib, sunitinib, and carb...

journal_title：Archiv der Pharmazie

authors： Hou Y,Shang C,Wang H,Yun J

更新日期：2020-01-01 00:00:00

abstract：:The synthesis and odour properties of the new santalol analogue, methyl-beta-santalol, are described. The additional methyl group adjacent to the hydroxyl function of the standard molecule, beta-santalol, deprives the new compound of the sandalwood note. The synthesis and the odour evaluation of this compound supports...

journal_title：Archiv der Pharmazie

authors： Buchbauer G,Zechmeister-Machhart F,Weiss-Greiler P,Wolschann P

更新日期：1997-04-01 00:00:00

abstract：:Two series of amino-1,4-benzoquinones (AQ1-18) based on the structural analogs of plastoquinones were synthesized and the structure-activity relationship against chronic myelogenous leukemia activity was examined. All of the synthesized compounds were tested for their cytotoxic effects on different leukemic cell lines...

journal_title：Archiv der Pharmazie

authors： Ciftci HI,Bayrak N,Yıldırım H,Yıldız M,Radwan MO,Otsuka M,Fujita M,Tuyun AF

更新日期：2019-12-01 00:00:00

abstract：:A number of phenylamides of 5-benzamidopyrazole-4-carboxylic acid were prepared in 50-80% yields from 1-phenyl (or methyl)-6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-ones and aniline derivatives. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their ulcerogenic potential ...

journal_title：Archiv der Pharmazie

authors： Daidone G,Plescia F,Maggio B,Raffa D,Cutuli VM,Mangano NG,Caruso A

更新日期：2001-05-01 00:00:00

abstract：:Novel sulfur-containing glutethimide derivatives, substituted with either thiol or methylsulfide groups in the ortho/para positions of the aromatic ring, were synthesized and tested for both human placental aromatase and bovine adrenocortical desmolase inhibitory activities. The synthesis was achieved by the chlorosul...

journal_title：Archiv der Pharmazie

authors： Bednarski PJ,Hartmann RW

更新日期：1993-07-01 00:00:00

abstract：:As per structural requirement essential for anticonvulsant activity, a series of new 6-(2-amino-substituted phenyl)-4-(substituted phenyl)-1,2,4-triazine-3,5-dione derivatives were designed and synthesized. All the synthesized title derivatives were assessed for in vivo anticonvulsant screening by the two most employe...

journal_title：Archiv der Pharmazie

authors： Khan AA,Siddiqui N,Akhtar MJ,Ali Z,Yar MS

更新日期：2016-04-01 00:00:00

abstract：:New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, quinazoline, 7-chloroquinoline, and 7-chloroquinazoline nuclei, have been synthesized. Their receptor binding profiles (5-HT1A, 5-HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. Th...

journal_title：Archiv der Pharmazie

authors： Rádl S,Hezky P,Proska J,Krejcí I

更新日期：2000-11-01 00:00:00

abstract：:We report on the synthesis and biological evaluation of two series of 2,4,5-polysubstituted thiazoles comprising the acid hydrazide functionality and some derived pharmacophores known to contribute to various chemotherapeutic activities. All newly synthesized compounds were subjected to in-vitro antibacterial and anti...

journal_title：Archiv der Pharmazie

authors： Al-Saadi MS,Faidallah HM,Rostom SA

更新日期：2008-07-01 00:00:00

abstract：:A novel approach to the pyridoacridine ring system of the ascididemin-type marine alkaloids is presented. This approach allows for the introduction of the ring A of the alkaloids by using a simple aromatic aldehyde building block. The viability of this approach is demonstrated with the synthesis of AK37, a bioactive d...

journal_title：Archiv der Pharmazie

authors： Raeder S,Bracher F

更新日期：2012-10-01 00:00:00

abstract：:Starting from substituted 9-chloroacridines, a series of quinacrine and spacered dimeric acridine compounds was prepared. Their ability to interrupt the protein association of prion- and Alzheimer-specific proteins and Ab peptides was explored using a fast screening system based on FACS analysis. The bis-acridines dis...

journal_title：Archiv der Pharmazie

authors： Csuk R,Barthel A,Raschke C,Kluge R,Ströhl D,Trieschmann L,Böhm G

更新日期：2009-12-01 00:00:00

abstract：:We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high...

journal_title：Archiv der Pharmazie

authors： Antipenko LN,Karpenko AV,Kovalenko SI,Katsev AM,Komarovska-Porokhnyavets EZ,Novikov VP

更新日期：2009-11-01 00:00:00

abstract：:A series of 5-(o-tolyl)-1H-tetrazole derivatives were synthesized and evaluated for their anticonvulsant activities. 1-(2-Methylbenzyl)-5-(o-tolyl)-1H-tetrazole (3h) showed important anticonvulsant activity against the MES-induced seizures, as well as lower neurotoxicity with an ED50 value of 12.7 mg/kg and a TD50 val...

journal_title：Archiv der Pharmazie

authors： Dong S,Wang T,Wang H,Qian K,Zhang Z,Zuo Y,Luo G,Jin Y,Wang Z

更新日期：2017-05-01 00:00:00

abstract：:(2S,3R)-3,7-Diamino-2-hydroxy-heptanoyl-Leu-Pro-OH [(2S,3R)-DAHHA-Leu-Pro-OH, 4], analogue of the N-terminal tripeptide of probestin, has been synthesized, and tested as inhibitor of AP-B, Leu-AP, AP-M, and enkephalin-degrading APs, and as analgesic. In order to establish structure-activity relationships the dipeptide...

journal_title：Archiv der Pharmazie

authors： Herranz R,Vinuesa S,Pérez C,García-López MT,De Ceballos ML,Murillo FM,del Río J

更新日期：1992-08-01 00:00:00

abstract：:N-Methoxyquinolinium salts 3 are prepared as potential cardiotonic agents by alkylation of the corresponding N-oxides 2 synthesized by two different methods. 1. Oxidation of some quinoline derivatives 1 using 30% H2O2 or 3-chloroperbenzoic acid. 2. Nitration of the quinoline-N-oxides 2a, 2c, and 2m. Preparation of 2h ...

journal_title：Archiv der Pharmazie

authors： Bünz C,Heber D,Ravens U

更新日期：1993-04-01 00:00:00

abstract：:A set of 40 derivatives of 3-hydroxypicolinic acid and 2-sulfanylbenzoic acid, isosteric to salicylanilides was synthesized. The compounds were evaluated for in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium, Candida albicans, Candida tropicalis, Candida krusei, Candi...

journal_title：Archiv der Pharmazie

authors： Waisser K,Pesina M,Holý P,Pour M,Bures O,Kunes J,Klimesová V,Buchta V,Kubanová P,Kaustová J

更新日期：2003-08-01 00:00:00

abstract：:The synthesis of tacrine-thiadiazolidinone hybrids is described. These compounds are designed as dual acetylcholinesterase inhibitors binding simultaneously to the peripheral and catalytic sites of the enzyme. All tested compounds exhibit significant AChE inhibitory activity. Competition assays using propidium as refe...

journal_title：Archiv der Pharmazie

authors： Dorronsoro I,Alonso D,Castro A,del Monte M,García-Palomero E,Martínez A

更新日期：2005-01-01 00:00:00

abstract：:Synthesis and biological assays of a series of 2-phenylpteridine derivatives are described to compare their affinities to adenosine receptors with those of the corresponding adenines, purposely prepared, and 8-azaadenines previously described. This study demonstrates that the enlargement of the five-membered ring of t...

journal_title：Archiv der Pharmazie

authors： Giorgi I,Biagi G,Livi O,Leonardi M,Scartoni V,Pietra D

更新日期：2007-02-01 00:00:00

abstract：:A short series of arylhydrazones of 4-[(2-methylimidazo[1,2-a]pyridine-3-yl)azo]benzoic acid hydrazide was synthesized and tested for antimicrobial activity. All of the compounds show antimicrobial activity against Escherichia coli. A few members were also active against Klebsiella pneumoniae, Staphylococcus aureus an...

journal_title：Archiv der Pharmazie

authors： Cesur Z,Büyüktimkin S,Büyüktimkin N,Derbentli S

更新日期：1990-03-01 00:00:00

abstract：:The photochemical stability of 2, 6, 6-trimethyl-3-carbmethoxy-4-phenyl-5-oxo-1, 4, 5, 6, 7, 8-hexahydroquinoline (HHQ) derivatives with different substituents on the phenyl ring (-Cl, -NO(2), -CF(3), -CH(3), -OCH(3)) has been studied.The process of photodegradation was studied by UV spectrophotometry. The rate of pho...

journal_title：Archiv der Pharmazie

authors： Mielcarek J,Safak C,Simsek R,Matloka A

更新日期：2002-05-01 00:00:00

abstract：:We describe a method to determine the affinity constant values between Ketoprofen and beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin in semisolid vehicles. The method is based on the diffusion of the drug, released from semisolid vehicles, through a lipidic non porous membrane. The affinity constants of Ketopro...

journal_title：Archiv der Pharmazie

authors： Orienti I,Zecchi V,Bertasi V,Fini A

更新日期：1991-12-01 00:00:00