4,5-Diaryl-3-aminopyrazole derivatives as analogs of Combretastatin A-4: synthesis and biological evaluation.

abstract：:A range of novel pyridine-2,4,6-tricarbohydrazide thiourea compounds (4a-i) were synthesized in good to excellent yields (63-92%). The enzyme inhibitory potentials of these compounds were investigated against α- and β-glucosidases because these enzymes play a crucial role in treating type-2 diabetes mellitus (T2DM). A...

journal_title：Archiv der Pharmazie

authors： Rehman TU,Riaz S,Khan IU,Ashraf M,Bajda M,Gawalska A,Yar M

更新日期：2018-01-01 00:00:00

abstract：:The antioxidant and acetylcholinesterase inhibitory properties of novel symmetric sulfamides derived from phenethylamines were evaluated. Phenethylamines 8-11 were reacted with SO2Cl2 in the presence of Et3N to afford sulfamides in good yields. The synthesized sulfamides were converted to their phenolic derivatives wi...

journal_title：Archiv der Pharmazie

authors： Aksu K,Topal F,Gulcin İ,Tümer F,Göksu S

更新日期：2015-06-01 00:00:00

abstract：:Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapa...

journal_title：Archiv der Pharmazie

authors： Huang Q,Xie L,Chen X,Yu H,Lv Y,Huang X,Ying J,Zheng C,Cheng Y,Huang J

更新日期：2018-11-01 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：:3-Ethyl 5-methyl 1,4-dihydro-2-[(2-hydroxyethoxy) methyl]-6-methyl-4-(2,3-dichlorophenyl)-3,5-pyridinedicarboxylate (13), a bioisostere of amlodipine, was prepared by the reaction of ethyl 4-(2-hydroxyethoxy)acetoacetate (11) with methyl 2-(2,3-dichlorobenzylidene)acetoacetate (12) and NH4OAc. Compound 13 was elaborat...

journal_title：Archiv der Pharmazie

authors： Yiu SH,Knaus EE

更新日期：1999-10-01 00:00:00

abstract：:We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed ...

journal_title：Archiv der Pharmazie

authors： Jiang SM,Ye BJ,Liu XK,Zhang TY,Cui X,Piao HR

更新日期：2010-11-01 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：: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：: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：:Based upon molecular modeling, the pharmacophore of potential inhibitors of p38 MAPK (mitogen-activated protein kinases) is discussed and the predictive binding affinities are calculated. Syntheses of original diarylimidazo[2,1-a]phthalazines obtained by Suzuki coupling are described. ...

journal_title：Archiv der Pharmazie

authors： Mavel S,Thery I,Gueiffier A

更新日期：2002-01-01 00:00:00

abstract：:A series of bis(benzo[g]indoles) bridged by CX-(CH2)nN(Me)(CH2)n-CX (X = O, S, H2; n = 2,3) was synthesized as bifunctional antitumor agents and evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. The parent compounds 2a,b exhibited a good level of activity and de...

journal_title：Archiv der Pharmazie

authors： Pinna GA,Pirisi MA,Grella GE,Gherardini L,Mussinu JM,Paglietti G,Ferrari AM,Rastelli G

更新日期：2001-11-01 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：:A series of new positive inotropic agents was synthesized with the aim of combining the pharmacophores of the imidazolone-type phosphodiesterase (PDE) inhibitor enoximone and guanidine-type histamine H2 receptor agonists such as arpromidine. All compounds are para-substituted 4-benzoyl-5-alkyl-2-imidazolones. H2 agoni...

journal_title：Archiv der Pharmazie

authors： Glass D,Buschauer A,Tenor H,Bartel S,Will-Shahab L,Krause EG

更新日期：1995-10-01 00:00:00

abstract：:The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern o...

journal_title：Archiv der Pharmazie

authors： Dannhardt G,Bauer A,Nowe U

更新日期：1997-03-01 00:00:00

abstract：:Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2 ] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxic...

journal_title：Archiv der Pharmazie

authors： Costante R,Pinnen F,Stefanucci A,Mollica A

更新日期：2014-05-01 00:00:00

abstract：:The synthesis and biological evaluation of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124, 4), as a member of a new generation of ultra-short acting hypnotics is described. HIE-124 4 exhibited potent in-vivo activity with a very rapid onset of action and a shorter duration of action...

journal_title：Archiv der Pharmazie

authors： Kadi AA,El-Kashef HA,Abdel-Aziz AA,Hassan GS,Tettey J,Grant MH,Lehmann J,El-Subbagh HI

更新日期：2008-02-01 00:00:00

abstract：:Platensimycin is a natural product isolated from various strains of Streptomyces platensis which exhibits antimicrobial activity against Gram positive bacteria, including vancomycin- and linezolide-resistant species. Analogues of platensimycin were synthesized from 3-aminobenzoic acid or other aniline derivatives and ...

journal_title：Archiv der Pharmazie

authors： Krauss J,Knorr V,Manhardt V,Scheffels S,Bracher F

更新日期：2008-06-01 00:00:00

abstract：:Rapamycin, a potent antifungal antibiotic, was approved as immunosuppressant, and lately its derivatives have been developed into mTOR targeting anticancer drugs. Structure modification was performed at the C-42 position of rapamycin, and a novel series of rapamycin triazole hybrids (4a-d, 5a-e, 8a-e, and 9a-e) was fa...

journal_title：Archiv der Pharmazie

authors： Xie L,Huang J,Chen X,Yu H,Li K,Yang D,Chen X,Ying J,Pan F,Lv Y,Cheng Y

更新日期：2016-06-01 00:00:00

abstract：:A series of 5-amino-3-methylisoxazole-4-carboxylic acid amides has been prepared by condensation of 5-amino-3-methylisoxazole-4-carboxylic acid with ethyl chloroformate. The resulting mixed anhydride undergoes condensation with appropriate phenylamides to form the corresponding amides 6-16. The compounds obtained were...

journal_title：Archiv der Pharmazie

authors： Ryng S,Zimecki M,Sonnenberg Z,Mokrosz MJ

更新日期：1999-05-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common type of dementia and related to the degeneration of hippocampal cholinergic neurons, which dramatically affects cognitive ability. Acetylcholinesterase (AChE) inhibitors are employed as drugs for AD therapy. Three series of sulfonylhydrazone compounds were designed, and thei...

journal_title：Archiv der Pharmazie

authors： Fernandes TB,Cunha MR,Sakata RP,Candido TM,Baby AR,Tavares MT,Barbosa EG,Almeida WP,Parise-Filho R

更新日期：2017-11-01 00:00:00

abstract：:Chemical modification of cinnoxacin was studied with the aim of improving its antibacterial activity and spectrum. A series of 4-imino-1, 4-dihydrocinnoline-3-carboxylic acid derivatives was synthesized and their in vitro antibacterial activity was evaluated. These derivatives were designed as isosteric analogues of f...

journal_title：Archiv der Pharmazie

authors： Stańczak A,Ochocki Z,Martynowski D,Główka M,Nawrot E

更新日期：2003-03-01 00:00:00

abstract：:Schistosoma mansoni histone deacetylase 8 (SmHDAC8) has been recently identified as a new potential target for the treatment of schistosomiasis. A series of newly designed and synthesized alkoxyamide-based and hydrazide-based HDAC inhibitors were tested for inhibitory activity against SmHDAC8 and human HDACs 1, 6, and...

journal_title：Archiv der Pharmazie

authors： Stenzel K,Chakrabarti A,Melesina J,Hansen FK,Lancelot J,Herkenhöhner S,Lungerich B,Marek M,Romier C,Pierce RJ,Sippl W,Jung M,Kurz T

更新日期：2017-08-01 00:00:00

abstract：:Twelve ethoxycarbonyl or phenylsulfonyl derivatives as prodrugs of hydroxylamine or phenylhydroxylamine were prepared and tested for antiplatelet (in vitro, Born test) antithrombotic (in vivo thrombosis model), and antihypertensive (in vivo, SHR rats) effects. In the Born test N,N-bisphenylsulfonylhydroxylamine (10) w...

journal_title：Archiv der Pharmazie

authors： Rehse K,Shahrouri T

更新日期：1998-11-01 00:00:00

abstract：:The active form of vitamin D3 , calcitriol, is a potent antiproliferative compound. However, when effective antitumor doses of calcitriol are used, hypercalcemic effects are observed, thus blocking its therapeutic application. To overcome this problem, structural analogues have been designed with the aim of retaining ...

journal_title：Archiv der Pharmazie

authors： Obiol DJ,Martínez A,Ferronato MJ,Quevedo MA,Grioli SM,Alonso EN,Gómez G,Fall Y,Facchinetti MM,Curino AC

更新日期：2019-05-01 00:00:00

abstract：:The new chemical entities febuxostat and topiroxostat have been approved by the US Food and Drug Administration, opening new avenues for exploiting different heterocycles other than purines as xanthine oxidase (XO) inhibitors. A different series of substituted 2-benzamido-4-methylthiazole-5-carboxylic acid derivatives...

journal_title：Archiv der Pharmazie

authors： Ali MR,Kumar S,Afzal O,Shalmali N,Ali W,Sharma M,Bawa S

更新日期：2017-02-01 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：:The design, synthesis, and investigation of antitumor and anti-lipase activities of some coumarin-triazole hybrid molecules are reported. The synthesis of these hybrid molecules was performed under microwave irradiation and conventional heating procedures. The newly synthesized hybrid molecules were investigated as in...

journal_title：Archiv der Pharmazie

authors： Kahveci B,Yılmaz F,Menteşe E,Ülker S

更新日期：2017-08-01 00:00:00

abstract：:The newly synthesized analogs of NAN-190 containing m-Cl and m-CF(3) substituents in the arylpiperazine moiety and their conformationally restricted counterparts showed a very high 5-HT(1A )receptor affinity. In the LLR test, the flexible compounds 4a and 5a displayed features of a partial agonist and agonist, respect...

journal_title：Archiv der Pharmazie

authors： Paluchowska MH,Bugno R,Charakchieva-Minol S,Bojarski AJ,Tatarczyńska E,Chojnacka-Wójcik E

更新日期：2006-09-01 00:00:00

abstract：:New phosphoramide mustards (6-8) have been prepared from the antibiotics 2 and 3, and from 5. The mixture of cyclophosphamides could be separated by preparative layer and column chromatography. The assignments of configuration to the isomeric phosphoramidates was based on the magnetic anisotropy of the P = O bond. The...

journal_title：Archiv der Pharmazie

authors： Csorvási A,Kövér KE,Menyhárt MM,Sztaricskai F,Dobrynin YV,Nikolaeva TG

更新日期：1998-09-01 00:00:00

abstract：:Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomyc...

journal_title：Archiv der Pharmazie

authors： Orienti I,Treré R,Luppi B,Bigucci F,Cerchiara T,Zuccari G,Zecchi V

更新日期：2002-03-01 00:00:00