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1.
In the present study, Plumbago rosea Linn. (Plumbaginaceae), one of the folk medicinal plants commonly used as an antifertility agent, was evaluated for its antifertility effect. Five successive solvent extracts, petroleum ether, chloroform, acetone, ethanol, and water extracts, of the stems of P. rosea were studied on estrous cycle at two dose levels, 200 and 400 mg/kg respectively. Of these, the acetone extract was found to be most effective in interrupting the normal estrous cycle of rats (p < 0.05) (p < 0.01). The rats exhibited prolonged diestrous stage of the estrous cycle with consequent temporary inhibition of ovulation. The antiovulatory activity was reversible on withdrawal of the extract. The effective acetone extract was further studied on estrogenic functionality in rats. The acetone extract showed significant estrogenic and antiestrogenic activity (p < 0.05) (p < 0.001). Histological studies of the uteri further confirmed the estrogenic activity of acetone extract. The results indicated the antifertility activity of stems of Plumbago rosea in female Wistar rats. 相似文献
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Suzana S. Jovanovi?-?anta Silvana Andri? Neboj?a Andri? Gordana Bogdanovi? Julijana A. Petrovi? 《Medicinal chemistry research》2011,20(7):1102-1110
In uterotrophic assay newly synthesized compounds 2–5 showed a complete loss of estrogenic activity, whereas derivatives 2–4 exhibited slight, and compound 5 higher antiestrogenic effects. On the other hand, anti-aromatase assay showed that compounds 2, 3, and 4 possess inhibition potency, although lower than standard aromatase inhibitor aminoglutethimide. Cytotoxicity of compounds
2–5, estradiol and tamoxifen against several human tumor or healthy cell lines (MCF-7, MDA-MB-231, HT-29, and MRC-5) was evaluated
after short-time treatment. 相似文献
4.
Nazar Trotsko Urszula Kosikowska Agata Paneth Monika Wujec Anna Malm 《Saudi Pharmaceutical Journal》2018,26(4):568-577
A series of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moiety (28–65) were synthesized by the reaction of (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid chlorides with 5-(hydroxybenzylidene) thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin derivatives. Obtained compounds (28–65) were tested on reference strains of Gram-positive bacteria and ones of the Gram-negative bacteria. The antibacterial activity of target compounds was determined by broth microdilution method. These derivatives showed antibacterial activity generally against Gram-positive bacterial strains. Most active compounds possess MIC?=?3.91?mg/L. Our results suggest that presence of electron-withdrawing substituent at phenyl ring is favorable while geometry of molecule does not play important role in antibacterial response. It was confirmed the lack of direct influence of substitution pattern at phenyl ring on antibacterial activity of closely related compounds of series 1–3. The antibacterial activity of some compounds was similar or higher than the activity of commonly used reference drugs such as oxacillin and cefuroxime. 相似文献
5.
Radhakrishnan Mahesh Arghya Kusum Dhar Ankur Jindal Shvetank Bhatt 《Chemical biology & drug design》2014,83(5):583-591
A series of novel 1,8‐naphthyridine‐3‐carboxamides as 5‐HT3 receptor antagonists were synthesized with an intention to explore the antidepressant activity of these compounds. The title carboxamides were designed using ligand‐based approach keeping in consideration the structural requirement of the pharmacophore of 5‐HT3 receptor antagonists. The compounds were synthesized using appropriate synthetic route from the starting material nicotinamide. 5‐HT3 receptor antagonism of all the compounds, which was denoted in the form of pA2 value, was determined in longitudinal muscle myenteric plexus preparation from guinea‐pig ileum against 5‐HT3 agonist, 2‐methyl‐5‐HT. Compound 8g (2‐methoxy‐1, 8‐naphthyridin‐3‐yl) (2‐methoxy phenyl piperazine‐1‐yl) methanone was identified as the most active compound, which expressed a pA2 value of 7.67. The antidepressant activity of all the compounds was examined in mice model of forced swim test (FST); importantly, none of the compounds was found to cause any significant changes in the locomotor activity of mice at the tested dose levels. In FST, the compounds with considerably higher pA2 value exhibited promising antidepressant‐like activity, whereas compounds with lower pA2 value did not show antidepressant‐like activity as compared to the control group. 相似文献
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Krishna Challa M Vijaya Bhargavi G L David Krupadanam 《Journal of Asian natural products research》2016,18(12):1158-1168
Taking into consideration of the biological activity of betulinic acid derivatives containing a oxadiazole ring, the semisynthetic betulinic acid-1,2,4-oxadiazole esters (14–25) were synthesized starting from betulinic acid (1) and 5-(bromomethyl)-3-aryl-1,2,4-oxadiazoles (2–13) and final compounds were tested for cytotoxic activity on three human cancer cell lines in vitro. All tested compounds showed good cytotoxic activity. The structures of synthesized compounds are established based on infrared (IR), nuclear magnetic resonance (NMR), and mass spectrometry. 相似文献
7.
Synthesis,molecular docking,and pharmacological evaluation of N‐(2‐(3,5‐dimethoxyphenyl)benzoxazole‐5‐yl)benzamide derivatives as selective COX‐2 inhibitors and anti‐inflammatory agents
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8.
Maria J. Mokrosz Beata Duszyska Stanisaw Misztal Aleksandra Kodziska Ewa Tatarczyska Ewa Chojnacka-Wjcik Marta Dziedzicka-Wasylewska 《Archiv der Pharmazie》1998,331(10):325-330
A series of 1-[ω-(4-aryl-1-piperazinyl)alkyl]indolin-2(1H)-one derivatives 2–14 was synthesized in order to obtain ligands with a dual 5-HT1A/5-HT2A activity. The majority of those compounds ( 2–5, 7, 10–13 ) exhibited a high 5-HT1A (Ki = 2 – 44 nM) and/or 5-HT2A affinity (Ki = 51 and 39 for 5 and 7 , respectively). Induction of lower lip retraction (LLR) and behavioral syndrome and inhibition of these efects evoked by 8-hydroxy-2-(di-n-propyl-amino)tetralin (8-OH-DPAT) were used for determination the agonistic and antagonistic activity, respectively, at 5-HT1A receptors. The 5-HT2A antagonistic activity was assessed by the blocking effect on the head twitches induced by (±)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) in mice. Two of the tested compounds, 1-{3-[4-(3-chlorophenyl)-1-piperazinyl]propyl}-6-fluoroindolin-2(1H)-one ( 5 ) and 1-{3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl}indolin-2(1H)-one ( 7 ), demonstrated a high 5-HT1A/5-HT2A affinity and an in vivo antagonistic activity towards both receptor subtypes. 相似文献
9.
Chlorostyrenes (CSs) are primarily derived from industrial by-products and are persistent and accumulative in the environment. In this study, the estrogenic and antiestrogenic activities of CSs (o-CS, m-CS, p-CS, DiCS, octa-CS) were evaluated using in vitro bioassays. o-CS and octa-CS have both estrogenic and antiestrogenic activity in the E-SCREEN assay and the ERE-reporter gene assay, indicating effects on a classical ER-mediated pathway. m-CS showed estrogenic activity in E-SCREEN but not in ERE-reporter gene assays, indicating that it may work through a non-classical ER-mediated pathway. Finally, DiCS only showed antiestrogenic activity via an ER-independent pathway, which can be induced by depletion of endogenous E2 level by the inhibition of aromatase activity and the stimulation of E2 metabolism. Although CSs have structural similarities to dioxins/furans, they did not have AhR agonist effects. This study is the first to show the estrogenic and antiestrogenic activity of several CSs using in vitro bioassay systems, including whether the compounds work via ER-mediated or/and non-ER-mediated pathways. 相似文献
10.
Ahmed M. Alafeefy 《Pharmaceutical biology》2013,51(10-11):751-756
A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for antimicrobial activity. The thioureide derivatives 4–6, the carbohydrazide derivatives 19–21 and 24 displayed excellent broad-spectrum antimicrobial activity. Some compounds showed moderate activity against Candida albicans and Pseudomonas aeruginosa. None of the tested compounds was as active as the reference standard drugs ampicillin and clotrimazole. The detailed synthesis, antimicrobial activity, and the minimum inhibitory concentrations (MIC) are reported. 相似文献
11.
A. Mohsen M. E. Omar Omaima M. Aboulwafa Ibrahim M. Labouta Alaa A. A. El-tombary Ahmed I. El-Mallah 《Archiv der Pharmazie》1996,329(2):61-65
4′,17-Dioxo-5′H-estra-1(10),4-dieno[3,2-b]furan ( 3 ) has been prepared by several routes starting from 2-bromoacetylestrone ( 2 ). Performance of the reaction with thiourea at elevated temperature provided compound 3 in good yield. When other reagents such as thiosemicarbazide, morpholine, sodium hydroxide or sodium hydride were treated with 2 -bromoacetylestrone at room temperature, the furano derivative 3 was also obtained as the sole product. This new type of structural modification provided an estrogen nucleus deprived of the 3-hydroxyl function which was previously thought to be an essential requisite for binding to the estrogen receptor (ER). When evaluated in vitro for binding to the ER and in vivo for uterotrophic and antifertility activities, the furano derivative 3 was capable of inhibiting[3H]E2 binding by 16% while still eliciting high uterotrophic (99%) and postcoital antimplantation (100%) activities relative to estradiol. 相似文献
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Md. Jashim Uddin Brenda C. Crews Anna L. Blobaum Philip J. Kingsley Kebreab Ghebreselasie Sam S. Saleh Jeffrey A. Clanton Ronald M. Baldwin Lawrence J. Marnett 《Journal of labelled compounds & radiopharmaceuticals》2009,52(9):387-393
A novel series of iodinated indomethacin derivatives was synthesized, and evaluated as selective inhibitors of COX‐2. Two candidate compounds N‐(p‐iodobenzyl)‐2‐(1‐(p‐chlorobenzoyl)‐5‐methoxy‐2‐methyl‐1H‐indol‐3‐yl)acetamide (3) and 1‐(p‐iodobenzyl)‐5‐methoxy‐2‐methyl‐3‐indoleacetic acid (9) possessed optimum properties suitable for potential in vivo imaging. Arylstannane precursors for radioiododestannylation were synthesized in 70–85% yield from the iodo compounds by reaction with hexabutylditin and tetrakis(triphenylphosphine)palladium(0) in refluxing dioxane. Radioiododestannylation was conducted by reaction with carrier‐added Na[123I] in the presence of Chloramine‐T in an EtOAc/H2O binary system under acidic conditions (pH 3.5), allowing direct isolation of the labeled products by separation of the organic phase. Radioiodinated products [123I]3 and [123I]9 were recovered in a decay‐corrected radiochemical yield of 86–87% and radiochemical purity of 98–99%. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
14.
Mohamed A. Shaaban Mostafa M. Ghorab Helmy I. Heiba Mona M. Kamel Nashwa H. Zaher Mohamed I. Mostafa 《Archiv der Pharmazie》2010,343(7):404-410
New derivatives of thiophenes 2 , 12 , iminoaminothieno[2,3‐d]pyrimidines 3 , 5 , and 6 , triazolothieno[2,3‐d]pyrimidines 8–11 , pyrazolo‐ and triazinothieno[2,3‐d]pyrimidines 4 , 7 , respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2 , 3 , and 9–12 was evaluated against in‐vitro cell lines (HEPG‐2 and MCF‐7). Compounds 2 , 3 , 10 , 11 , and 12 showed significant in‐vitro cytotoxic activity against hepatocellular carcinoma (HEPG‐2) compared to the reference drug Doxorubicin. Compound 2 showed significant in‐vitro cytotoxic activity against breast cancer (MCF‐7) cells compared to the reference drug Doxorubicin. The augmenting effect of γ‐radiation was assessed; here, compounds 2 , 3 , 10 , and 11 showed the most potent in‐vitro anticancer activity. 相似文献
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Mahesh Palkar Malleshappa Noolvi Ramappa Sankangoud Veeresh Maddi Andanappa Gadad Laxmi Venkat G. Nargund 《Archiv der Pharmazie》2010,343(6):353-359
Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1‐b)‐benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti‐inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3‐diaryl‐substituted imidazo(2,1‐b)‐benzothiazoles 13a–o have been synthesized by reaction of substituted 2‐aminobenzothiazoles 1–8 and an appropriately substituted α‐bromo‐1‐(4′′‐substituted)‐phenyl‐2‐(4′‐substituted)‐phenyl‐1‐ethanones 9–12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, 1H‐NMR, and Mass) data. All the synthesized compounds were screened for their in‐vitro antibacterial activity against Gram‐positive, Gram‐negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d , 13h , and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials. 相似文献
16.
Novel series of pyrazole derivatives were synthesized and tested for their in vivo anti‐malarial activity using mice infected with chloroquine sensitive P. berghei at a dose level of 50 µmol/kg. The most active compounds were further tested in vitro against chloroquine resistant (RKL9) strain of P. falciparum. The in vivo anti‐malarial activity study indicated that compounds 2a, 2b, 8a and 8b had mean percent suppression of 85%, 83%, 95% and 97%, respectively at equimolar dose level of the standard drug chloroquine diphosphate. Moreover, compounds 2a, 2b, 8a and 8b showed in vitro IC50 values lower (p < 0.05) than that of the standard drug chloroquine phosphate (0.188 ± 0.003 µM) using the RKL9 strain. Compound 8b was the most active with IC50 of 0.033 ± 0.014 µM. Generally, among the tested compounds, those containing a free carboxylic acid functional group on the pyrazole ring were the most active and this finding was supported by the docking results performed for the active compounds. The acute toxicity studies of the active compounds revealed that they have a good safety profile. 相似文献
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Zrinka Rajić Dimitra Hadjipavlou-Litina Eleni Pontiki Marijeta Kralj Lidija Šuman Branka Zorc 《Chemical biology & drug design》2010,75(6):641-652
The novel amides of ketoprofen and its reduced derivatives (5a–f, 4a–n, 6a–g) with aromatic and cycloalkyl amines or hydroxylamines were prepared and screened for their reducing and cytostatic activity as well as for their ability to inhibit soybean lipoxygenase and lipid peroxidation. 1,1-Diphenyl-picrylhydrazyl test for reducing ability revealed that ketoprofen amides were more potent antioxidants than the amides of the reduced ketoprofen derivatives. The most active compound was benzhydryl ketoprofen amide 5f. Lipoxygenase inhibition of the tested compounds varied from strong to very weak. The most potent compound was benzhydryl derivative 6f (IC50 = 20.5 μm ). Aromatic and cycloalkyl amides 4 and 5 were more potent lipoxygenase inhibitors than derivatives with carboxylic group. Aromatic amides of series 4 and 5 showed excellent lipid peroxidation inhibition (92.2–99.9%). On the other hand, the most pronounced cytostatic activity was exerted by O-benzyl derivative 4i, although in general all tested reduced and non-reduced lipophilic derivatives showed similar activity. 相似文献
18.
Heba T. Abdel-Mohsen Amira Abood Keith J. Flanagan Alina Meindl Mathias O. Senge Hoda I. El Diwani 《Archiv der Pharmazie》2020,353(3):1900271
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 their antibacterial activity against Staphylococcus aureus and Bacillus subtilis as Gram-positive (+) bacteria, as well as against Gram-negative (−) bacteria Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Salmonella typhi. Most of the synthesized derivatives of imidazopyrimidines 6 and 9 showed remarkable selectivity against Gram(−) bacteria over the Gram(+) ones. Compounds 6c , 6f , and 6g displayed potent and broad-spectrum antibacterial activity against all tested strains. Compounds 6f and 6g displayed promising inhibitory activity on GryB ATPase from E. coli with IC50 = 1.14 and 0.73 μM, respectively. Simultaneously, some of the synthesized imidazopyrimidines were screened for their antiproliferative activity against 60 cancer cell lines at a concentration of 10 μM. Compound 9d showed potent activity against most of the tested cell lines, with a mean growth inhibition of 37%. The ADME (absorption, distribution, metabolism, and excretion) prediction study demonstrated that the synthesized hits have, in addition to their promising chemotherapeutic activity, acceptable pharmacokinetic properties, and a drug-likeness nature to be further developed. 相似文献
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Gabriela Mazur Katarzyna Pańczyk-Straszak Anna Rapacz Jan Kiszela Magdalena Smolik Maciej Gawlik Maria Walczak Joanna Czekajewska Celina Poloczek Elżbieta Karczewska Ewa Żesławska Wojciech Nitek Anna Niedbał Joanna Leśniak Katarzyna Ciapala Katarzyna Pawlik Joanna Mika Anna M. Waszkielewicz 《Chemical biology & drug design》2023,101(2):278-325
A series of 10 aminoalkanol derivatives of 5-chloro-2- or 5-chloro-4-methylxanthone was synthetized and evaluated for anticonvulsant properties (MES test, mice, intraperitoneal) and compared with neurotoxicity rotarod test (NT, mice, i.p.). The best results both in terms of anticonvulsant activity and protective index value were obtained for 3 : 5-chloro-2-([4-hydroxypiperidin-1-yl]methyl)-9H-xanthen-9-one hydrochloride. Compounds: 1 – 3 , 7 and 10 revealed ED50 values in MES test: 42.78, 31.64, 25.76, 46.19 and 52.50 mg/kg b.w., respectively. 3 showed 70% and 72% of inhibition control specific binding of sigma-1 (σ1) and sigma-2 (σ2) receptor, respectively. 3 exhibited also antinociceptive activity at dose 2 mg/kg b.w. after chronic constriction injury in mice. 1 , 3 , 7 and 10 were evaluated on gastrointestinal flora and proved safe. In genotoxicity test (UMU-Chromotest) compounds 1 , 7 and 10 proved safe at dose 150–300 μg/ml. The pharmacokinetic analysis showed rapid absorption of all studied molecules from the digestive tract (tmax = 5–30 min). The bioavailability of the compounds ranged from 6.6% ( 1 ) to 16% ( 10 ). All studied compounds penetrate the blood–brain barrier with brain to plasma ratios varied from 4.15 ( 3 ) to 7.6 (compound 7 ), after i.v. administration, and from 1 ( 7 ) to 5.72 ( 3 ) after i.g. administration. 相似文献
20.
In an ongoing effort to develop novel non-nucleoside human immunodeficiency virus inhibitors, a series of substituted 2-(1H-benzimidazol-2-ylamino)pyrimidin-4(3H)-ones and related derivatives were synthesized via cyclocondensation of 2-guanidino-1H-benzimidazole with diethyl ethoxymethylenemalonate, substituted diethyl malonates, some β-keto esters and 2-acetylbutyrolactone. From these series of compounds, 2-(1H-benzimidazol-2-ylamino)-6-hydroxy-5-phenylpyrimidin-4(3H)-ones ( 5f , NSC 666286) was confirmed to have a moderate in vitro anti-HIV activity. 相似文献