- Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4] triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives
[作者:Deng, XQ; Quan, LN; Song, MX; Wei, CX; Quan, ZS,期刊:European Journal of Medicinal Chemistry, 页码:2955-2963 , 文章类型: Article,,卷期:2011年46-7]
- Herein, we described the syntheses and anticonvulsant activities of 7-(substituted-phenyl)-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones (1a-1o) and their derivatives. Most of the synthesized compounds exhibited...
- Discovery of molecules for the treatment of neuropathic pain: Synthesis, antiallodynic and antihyperalgesic activities of 5-(4-nitrophenyl)furoic-2-acid hydrazones
[作者:Yogeeswari, P; Menon, N; Semwal, A; Arjun, M; Sriram, D,期刊:European Journal of Medicinal Chemistry, 页码:2964-2970 , 文章类型: Article,,卷期:2011年46-7]
- Neuropathic pain is a chronic pain condition that occurs and persists in a heterogeneous group of etiologically different diseases characterized by a primary lesion or dysfunction of the peripheral or central nervous sys...
- Synthesis and biological evaluation of 4-nitro-substituted 1,3-diaryltriazenes as a novel class of potent antitumor agents
[作者:Cimbora-Zovko, T; Brozovic, A; Piantanida, I; Fritz, G; Virag, A; Alic, B; Majce, V; Kocevar, M; Polanc, S; Osmak, M,期刊:European Journal of Medicinal Chemistry, 页码:2971-2983 , 文章类型: Article,,卷期:2011年46-7]
- We describe the synthesis and biological activity of a new class of 1,3-diaryltriazenes, namely 4-nitro-substituted 1,3-diaryltriazenes. Structure-activity relationship analysis reveals that 1,3-diaryltriazenes can be mo...
- Synthesis and evaluation of monoamidoxime derivatives: Toward new antileishmanial compounds
[作者:Paloque, L; Bouhlel, A; Curti, C; Dumetre, A; Verhaeghe, P; Azas, N; Vanelle, P,期刊:European Journal of Medicinal Chemistry, 页码:2984-2991 , 文章类型: Article,,卷期:2011年46-7]
- A new series of monoamidoxime derivatives was synthesized using manganese(III) acetate by microwave irradiation. Several amidoximes (27-31, 33, 38) showed valuable in vitro activities toward Leishmania donovani promastig...
- New 2-thioether-substituted apomorphines as potent and selective dopamine D(2) receptor agonists
[作者:Reinart, R; Gyulai, Z; Berenyi, S; Antus, S; Vonk, A; Rinken, A; Sipos, A,期刊:European Journal of Medicinal Chemistry, 页码:2992-2999 , 文章类型: Article,,卷期:2011年46-7]
- A set of novel apomorphine derivatives were synthesized with diversely functionalized side chains in the proximity of position 2 of the aporphine skeleton. Amino and/or carboxylic functions were introduced to this region...
- Discovery of LASSBio-772, a 1,3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-Adrenergic receptor blocking properties
[作者:Romeiro, LAS; Ferreira, MD; da Silva, LL; Castro, HC; Miranda, ALP; Silva, CLM; Noel, F; Nascimento, JB; Araujo, CV; Tibirica, E; Barreiro, EJ; Fraga, CAM,期刊:European Journal of Medicinal Chemistry, 页码:3000-3012 , 文章类型: Article,,卷期:2011年46-7]
- We described herein the discovery of 1-(2-(benzo[d] [1,3]dioxol-6-yl)ethyl)-4-(2-methoxyphenyl) piperazine (LASSBio-772), as a novel potent and selective alpha 1A/1D adrenoceptor (AR) antagonist selected after screening ...
- Synthesis, nucleic acid binding and cytotoxicity of polyethyleneimine-copper(II) complexes containing 1,10-phenanthroline and L-valine
[作者:Lakshmipraba, J; Arunachalam, S; Gandi, DA; Thirunalasundari, T,期刊:European Journal of Medicinal Chemistry, 页码:3013-3021 , 文章类型: Article,,卷期:2011年46-7]
- The polymer-copper(II) complex samples, [Cu(phen)(L-Val) BPEI]Cl center dot H(2)O, with varying degrees of coordination in the polymer chain, were prepared and characterized by elemental analysis and spectroscopic method...
- New condensed pyrroles of potential biological interest Syntheses and structure-activity relationship studies
[作者:Mohamed, MS; Kamel, R; Fatahala, SS,期刊:European Journal of Medicinal Chemistry, 页码:3022-3029 , 文章类型: Article,,卷期:2011年46-7]
- The Pyrrole derivatives Ia-d were prepared and utilized for the preparation of pyrrolo[2,3-d]pyrimidine derivatives IIa-c, III, IVa-e, V and VIIIa-c; pyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidine VI and pyrrolo[4,3e] [1,2,4]t...
- Novel aliphatic N-oxide of naphthalimides as fluorescent markers for hypoxic cells in solid tumor
[作者:Yin, H; Zhu, WP; Xu, YF; Dai, M; Qian, XH; Li, YL; Liu, JW,期刊:European Journal of Medicinal Chemistry, 页码:3030-3037 , 文章类型: Article,,卷期:2011年46-7]
- A series of novel aliphatic N-oxide of naphthalimides (A1-A5) were designed and prepared. The N-O group was firstly introduced into the amine side chain tailed to planar naphthalimide chromophore as hypoxic bioreductive ...
- A regioselective synthesis of some new pyrazol-1 '-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents
[作者:Aggarwal, R; Sumran, G; Garg, N; Aggarwal, A,期刊:European Journal of Medicinal Chemistry, 页码:3038-3046 , 文章类型: Article,,卷期:2011年46-7]
- An efficient and environmental benign regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a] pyrimidines (7b-h) has been accomplished via treatment of 3(5)-amino-5(3)-hydrazinopyrazole dihydrochloride (5) with...
- Buchwald reaction as the key step for the synthesis of metabolically more stable analogs of amodiaquine
[作者:Le Fur, N; Hochart, G; Larchanche, PE; Melnyk, P,期刊:European Journal of Medicinal Chemistry, 页码:3052-3057 , 文章类型: Article,,卷期:2011年46-7]
- Amodiaquine is one of the most active anti-malarial 4-aminoquinoline but its metabolization is believed to generate hepatotoxic derivatives. Previously, we described new analogs of amodiaquine and amopyroquine, in which ...
- Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors
[作者:Dolusic, E; Larrieu, P; Blanc, S; Sapunaric, F; Pouyez, J; Moineaux, L; Colette, D; Stroobant, V; Pilotte, L; Colau, D; Ferain, T; Fraser, G; Galleni, M; Frere, JM; Masereel, B; Van den Eynde, B; Wouters, J; Frederick, R,期刊:European Journal of Medicinal Chemistry, 页码:3058-3065 , 文章类型: Article,,卷期:2011年46-7]
- Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto...
- Anti-proliferative activity of aguerin B and a new rare nor-guaianolide lactone isolated from the aerial parts of Centaurea deflexa
[作者:Chicca, A; Tebano, M; Adinolfi, B; Ertugrul, K; Flamini, G; Nieri, P,期刊:European Journal of Medicinal Chemistry, 页码:3066-3070 , 文章类型: Article,,卷期:2011年46-7]
- The phytochemical investigation of the aerial parts of Centaurea deflexa led to the identification of 21 compounds, among which three phenolic acids, one sterol, ten flavonoids, one phenylpropanoid derivative, two lignan...
- Synthesis and anti-Trypanosoma cruzi activity of beta-lapachone analogues
[作者:Ferreira, SB; Salomao, K; da Silva, FD; Pinto, AV; Kaiser, CR; Pinto, AC; Ferreira, VF; de Castro, SL,期刊:European Journal of Medicinal Chemistry, 页码:3071-3077 , 文章类型: Article,,卷期:2011年46-7]
- The available chemotherapy for Chagas disease, caused by Trypanosoma cruzi, is unsatisfactory; therefore, there is an intense effort to find new drugs for the treatment of this disease. In our laboratory, we have analyze...
- Synthesis, in vitro antioxidant, anthelmintic and molecular docking studies of novel dichloro substituted benzoxazole-triazolo-thione derivatives
[作者:Satyendra, RV; Vishnumurthy, KA; Vagdevi, HM; Rajesh, KP; Manjunatha, H; Shruthi, A,期刊:European Journal of Medicinal Chemistry, 页码:3078-3084 , 文章类型: Article,,卷期:2011年46-7]
- A novel 6,8-dichloro [1,2,4]triazolo [3,4-b] [1,3]benzoxazole-3(2H)-thione 4 and its derivatives 5a and 5b are synthesized from 5,7-dichloro-2-hydrazinyl-1,3-benzoxazole 3, obtained by reaction of hydrazine hydrate with ...
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