Synthesis and 5-HT2A radioligand receptor binding assays of DOMCl and DOMOM, two novel 5-HT2A receptor ligands.

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：:Three ketomethylene pseudodideptide analogues [(S)Lys psi(COCH2)(R and S)Phe (14 or 15 and 15 or 14) and (S)Lys psi(COCH2)(xi Trp (19)] of natural arphamenine A [(S)Arg psi(COCH2(R,S)Phe (1)] were easily prepared by a route involving two successive main reactions: a malonic ester alkylation with Z-protected lysine iod...

journal_title：Archiv der Pharmazie

authors： García-López MT,González-Muñiz R,Hartoa JR,Gómez-Monterrey I,Pérez C,De Ceballos ML,López E,Del Río J

更新日期：1992-01-01 00:00:00

abstract：:Novel thiazolyl hydrazonothiazolamines and 1,3,4-thiadiazinyl hydrazonothiazolamines were synthesized by a facile one-pot multicomponent approach by the reaction of 2-amino-4-methyl-5-acetylthiazole, thiosemicarbazide or thiocarbohydrazide and phenacyl bromides or 3-(2-bromoacetyl)-2H-chromen-2-ones in acetic acid wit...

journal_title：Archiv der Pharmazie

authors： Sujatha K,Ommi NB,Mudiraj A,Babu PP,Vedula RR

更新日期：2019-12-01 00:00:00

abstract：:Several 2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-benzimidazole-5-carboxamidine analogues were synthesized for their antibacterial and antifungal activities against S. aureus, Methicillin-resistant S. aureus (MRSA), C. albicans, and C. krusei. MIC values of the targeted compounds 43-58 are comparabl...

journal_title：Archiv der Pharmazie

authors： Ates-Alagöz Z,Alp M,Kus C,Yildiz S,Buyukbingöl E,Göker H

更新日期：2006-02-01 00:00:00

abstract：:The synthesis and antitumor activity screening of novel isatin based conjugates with thiazolidine and pyrazoline moieties were performed. Reaction of 3,5-diaryl-4,5-dihydropyrazoles with chloroacetyl chloride yielded starting 2-chloro-1-(3,5-diaryl-4,5-dihydropyrazol-1-yl)-ethanones which were utilized in alkylation o...

journal_title：Archiv der Pharmazie

authors： Havrylyuk D,Kovach N,Zimenkovsky B,Vasylenko O,Lesyk R

更新日期：2011-08-01 00:00:00

abstract：:A series of new Mannich bases of N-[(4-arylpiperazin-1-yl)-methyl]-3-(chlorophenyl)-pyrrolidine-2,5-diones 10-23 have been synthesized and evaluated for their anticonvulsant activity in maximum electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Their neurotoxicity was determined us...

journal_title：Archiv der Pharmazie

authors： Obniska J,Kopytko M,Zagórska A,Chlebek I,Kamiński K

更新日期：2010-06-01 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：:Copper and zinc have been found to contribute to the burden of amyloid-β (Aβ) aggregations in neurodegenerative Alzheimer's disease (AD). Dysregulation of these metals leads to the generation of reactive oxygen species (ROS) and eventually results in oxidative damage and accumulation of the Aβ peptide, which are the k...

journal_title：Archiv der Pharmazie

authors： Fu CL,Hsu LS,Liao YF,Hu MK

更新日期：2016-05-01 00:00:00

abstract：:Gypsogenin (1) was obtained by acidic hydrolysis from its saponin. While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 ± 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-di...

journal_title：Archiv der Pharmazie

authors： Heller L,Schwarz S,Weber BA,Csuk R

更新日期：2014-10-01 00:00:00

abstract：:Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced th...

journal_title：Archiv der Pharmazie

authors： Kalaycı M,Türkeş C,Arslan M,Demir Y,Beydemir Ş

更新日期：2020-11-06 00:00:00

abstract：:Marine organisms play an important role in natural product-based drug research due to accumulation of structurally unique and bioactive metabolites. The exploration of marine-derived compounds may significantly extend the scientific knowledge of potential scaffolds for antibiotic drug discovery. Development of novel a...

journal_title：Archiv der Pharmazie

authors： Daletos G,Ancheeva E,Chaidir C,Kalscheuer R,Proksch P

更新日期：2016-10-01 00:00:00

abstract：:Structural feature analysis of chlorogenic acid derivatives made up of varying lengths of alkyl groups as α-glucosidases inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave one out, Y-randomization and test set methods. The predictive capaci...

journal_title：Archiv der Pharmazie

authors： Narayana Moorthy NS,Ramos MJ,Fernandes PA

更新日期：2012-04-01 00:00:00

abstract：:A series of dialkyl, dicycloalkyl, and diaryl ester analogues of nifedipine, in which the ortho-nitro phenyl group at position 4 is replaced by the 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists using the high K+ contraction of guinea pig ileal longitud...

journal_title：Archiv der Pharmazie

authors： Davood A,Mansouri N,Rerza Dehpour A,Shafaroudi H,Alipour E,Shafiee A

更新日期：2006-06-01 00:00:00

abstract：:In continuation of our effort aimed towards the development of novel aldose reductase inhibitors, several phenylacetic acids bearing an alkoxy substituent in position 3 or 4, respectively, were prepared and screened. The latter represent formal ring opening products of the cyclohexylmethyloxyphenylacetic acids IIa and...

journal_title：Archiv der Pharmazie

authors： Rakowitz D,Gmeiner A,Matuszczak B

更新日期：2006-10-01 00:00:00

abstract：:Some new N-[6-indazolyl]arylsulfonamides and N-[alkoxy-6-indazolyl]arylsulfonamides were prepared by the reduction of 2-alkyl-6-nitroindazoles with SnCl2 in different alcohols, followed by coupling the corresponding amine with arylsulfonyl chlorides in pyridine. The newly synthesized compounds were evaluated for their...

journal_title：Archiv der Pharmazie

authors： Abbassi N,Rakib el M,Chicha H,Bouissane L,Hannioui A,Aiello C,Gangemi R,Castagnola P,Rosano C,Viale M

更新日期：2014-06-01 00:00:00

abstract：:The butadiene derivatives 10a-c react with the oxa-bicyclooctanone 9 to give the cyclohexene annulated oxatropanes 11a-c. The acetoxyderivatives 11b and 11c can be transformed into the cyclohexadiene or benzene derivatives 13 and 12, respectively. 11a reacts with HN3 to afford the tricyclic oxazepanone 14 which can be...

journal_title：Archiv der Pharmazie

authors： Eiden F,Kainz A,Gebhard R

更新日期：1992-02-01 00:00:00

abstract：:A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 1...

journal_title：Archiv der Pharmazie

authors： Wang XJ,Wu N,Du GJ,Zhao SQ,Yan M,Gu LQ

更新日期：2009-07-01 00:00:00

abstract：:New analogues of nifedipine, in which the 2-nitrophenyl group at position 4 is replaced by a 1-methyl-5-nitro-2-imidazolyl substituent, were synthesized. The symmetrical dialkyl 1, 4-dihydro-2, 6-dimethyl-4-(1-methyl-5-nitro-2-imidazolyl)-3, 5-pyridinedicarboxylates were prepared by a classical Hantzsch condensation. ...

journal_title：Archiv der Pharmazie

authors： Miri R,Javidnia K,Kebriaie-Zadeh A,Niknahad H,Shaygani N,Semnanian S,Shafiee A

更新日期：2003-09-01 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：:Albumin binding for the enantiomers of four closely related N-methyl-5-phenyl-5-alkyl-barbiturates 1-4 was investigated for three different mammalian species by means of equilibrium dialysis. Lipid solubility (n-heptane/phosphate buffer distribution coefficient) increased stepwise by a factor of 56 from 1 to 4. Bovine...

journal_title：Archiv der Pharmazie

authors： Büch HP,Krug R,Knabe J

更新日期：1996-08-01 00:00:00

abstract：:The combined effects of amino acid antagonists with proven or potential inhibitory activities on aminoacyl-tRNA synthetases were investigated on the murine leukemic cell line P388 D1. As the best result a summation of the antiproliferative effects was observed. Combinations with established cytostatic agents like plat...

journal_title：Archiv der Pharmazie

authors： Laske R,Schönenberger H,Holler E

更新日期：1991-03-01 00:00:00

abstract：:A series of hydroxy-substituted chalcone oxime derivatives were synthesized. These compounds were then evaluated for their inhibitory activities on tyrosinase and melanogenesis in murine B16F10 melanoma cells. The structures of the synthesized compounds were confirmed by (1) H NMR, (13) C NMR, FTIR, and HRMS. Two of t...

journal_title：Archiv der Pharmazie

authors： Radhakrishnan SK,Shimmon RG,Conn C,Baker AT

更新日期：2016-01-01 00:00:00

abstract：:The reaction of ethyl 4-(benzofuran-2-yl)-2,4-dioxobutanoate 2 with two moles of hydrazine hydrate afforded 5-(benzofuran-2-yl)-1H-pyrazole-3-carbohydrazide 4a, while its reaction with equimolar amount of phenylhydrazine gave ester 3b which then converted to 5-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazide 4b...

journal_title：Archiv der Pharmazie

authors： Abdel-Wahab BF,Abdel-Aziz HA,Ahmed EM

更新日期：2008-11-01 00:00:00

abstract：:A series of hydantoin prostaglandin analogues, in which the hexamethylene moiety of the acid side chain was replaced by other spacing groups possessing either ether, sulphide and/or olefin functionality, were prepared and evaluated for platelet aggregation inhibiting activity. The 4-thia analogue 13*) proved to be the...

journal_title：Archiv der Pharmazie

authors： Barraclough P,Caldwell AG,Glen RC,Harris CJ,Stepney R,Whittaker N,Whittle BJ

更新日期：1993-02-01 00:00:00

abstract：:Several 4-cyano-1,5-diphenylpyrazoles attached to different heterocyclic ring systems at position 3 were synthesized starting from ethyl 4-cyano-1,5-diphenyl-1H-pyrazole-3-carboxylate 1. The newly synthesized compounds were tested in vivo for their anti-estrogenic effects and evaluated in vitro for their cytotoxic pro...

journal_title：Archiv der Pharmazie

authors： Farag AM,Mayhoub AS,Eldebss TM,Amr AG,Ali KA,Abdel-Hafez NA,Abdulla MM

更新日期：2010-07-01 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：:The key step in the synthesis of the pharmacologically interesting 1-phenyltetrahydro-3-benzazepine skeleton is the Michael addition of (2-lithiophenyl)acetaldehyde acetals, which are generated in situ upon treatment of the bromo acetals 5a,b with n-butyllithium, to beta-nitrostyrene (6). The reductive ring closure of...

journal_title：Archiv der Pharmazie

authors： Wünsch B,Nerdinger S,Bauschke G,Höfner G

更新日期：1997-07-01 00:00:00

abstract：:Prevention of the formation of advanced glycation end-products (AGEs) is a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In these terms, new synthetic approaches to 6-nitroazolo[1,5-a]pyrimidines have been developed on the basis of the promi...

journal_title：Archiv der Pharmazie

authors： Spasov AA,Babkov DA,Sysoeva VA,Litvinov RA,Shamshina DD,Ulomsky EN,Savateev KV,Fedotov VV,Slepukhin PA,Chupakhin ON,Charushin VN,Rusinov VL

更新日期：2017-12-01 00:00:00

abstract：:A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell ...

journal_title：Archiv der Pharmazie

authors： Mokenapelli S,Thalari G,Vadiyaala N,Yerrabelli JR,Irlapati VK,Gorityala N,Sagurthi SR,Chitneni PR

更新日期：2020-06-01 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