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1.
Venu TD Shashikanth S Khanum SA Naveen S Firdouse A Sridhar MA Shashidhara Prasad J 《Bioorganic & medicinal chemistry》2007,15(10):3505-3514
Fries rearrangement of substituted phenyl benzoates 1a-j to substituted hydroxy benzophenones 2a-j was achieved in excellent yield. Further benzoylation of 2a-j to benzoyloxy benzophenones 4a-n, a benzophenone analogue was achieved in good yield. All the newly synthesized compounds were evaluated for their anti-inflammatory activity and were compared with standard drugs. Out of the compounds studied, the compounds 4c, 4e, 4g, 4h and 4k with chloro and methyl substituents at para position showed more potent activity than the standard drugs at all doses tested. 相似文献
2.
Cognition-enhancing activity of Bacopa monniera extract (BME) was evaluated against scopolamine-induced amnesic rats by novel object recognition test (NOR), elevated plus maze (EPM) and Morris water maze (MWM) tests. Scopolamine (2 mg/kg body wt, i.p.) was used to induce amnesia in rats. Piracetam (200 mg/kg body wt, i.p.) was used as positive control. BME at three different dosages (i.e., 10, 20 and 40 mg/kg body wt.) improved the impairment induced by scopolamine by increasing the discrimination index of NOR and by decreasing the transfer latency of EPM and escape latency of MWM tests. Our results further elucidate that BME administration has normalized the neurotransmitters (acetylcholine, glutamate, 5-hydroxytryptamine, dopamine, 3,4 dihydroxyphenylacetic acid, norepinephrine) levels that were altered by scopolamine administration in hippocampus of rat brain. BME administration also ameliorated scopolamine effect by down-regulating AChE and up-regulating BDNF, muscarinic M1 receptor and CREB expression in brain hippocampus confirms the potent neuroprotective role and these results are in corroboration with the earlier in vitro studies. BME administration showed significant protection against scopolamine-induced toxicity by restoring the levels of antioxidant and lipid peroxidation. These results indicate that, cognition-enhancing and neuromodulatory propensity of BME is through modulating the expression of AChE, BDNF, MUS-1, CREB and also by altering the levels of neurotransmitters in hippocampus of rat brain. 相似文献
3.
Sajida Khanum 《Phytochemistry》1985,24(7):1625-1626
Studies on the alkaloids from the leaves of Rhazya stricta have afforded a new alkaloid to which the structure 2-methoxy-1,2-dihydrorhazimine has been assigned. 相似文献
4.
Khanum SA Murari SK Vishwanth BS Shashikanth S 《Bioorganic & medicinal chemistry letters》2005,15(18):4100-4104
Benzoylation of (hydroxy phenyl) phenyl methanone 2a-g to benzoyl phenyl benzoates 4a-g, a benzophenone analogue, was achieved in good yield. All the newly synthesized compounds were evaluated for their phospholipase A2 [E.C. 3.1.1.4] and hyaluronidase [E.C. 3.2.1.35] enzyme inhibitory activity in snake venom as source and their structure-activity relationship with respect to different groups is reported for the first time. The in vitro PLA2 enzyme inhibitory activity and in vivo anti-inflammatory activity studies of benzoyl phenyl benzoates are illustrated. 相似文献
5.
V. Lakshmi Ranganatha B.R. Vijay Avin Prabhu Thirusangu T. Prashanth B.T. Prabhakar Shaukath Ara Khanum 《Life sciences》2013
Aim
The development of anticancer drugs with specific targets is of prime importance in modern biology. This study investigates the angiopreventive and in vivo tumor inhibition activities of novel synthetic benzophenone–benzimidazole analogs.Main methods
The multistep synthesis of novel benzophenone–benzimidazole analogs (8a–n) allowing substitution with methoxy, methyl and halogen groups at different positions on the identical chemical backbone and the variations in the number of substituents were synthesized and characterized. The newly synthesized compounds were further evaluated for cytotoxic and antiproliferative effects against Ehrlich ascites carcinoma (EAC) cells. The potent lead compounds were further assessed for antiangiogenic effects in a CAM model and a tumor-induced vasculature in vivo model. The effect of angioprevention on tumor growth was verified in a mouse model.Key findings
The cytotoxicity studies revealed that compounds 8f and 8n are strongly cytotoxic. Analyzing the structure–activity relationship, we found that an increase in the number of methyl groups in addition to methoxy substitution at the para position of the benzoyl ring in compound 8n resulted in higher potency compared to 8f. Furthermore, neovessel formation in in vivo systems, such as the chorioallantoic membrane (CAM) and tumor-induced mice peritoneum models, was significantly suppressed and reflected the tumor inhibition observed in mice.Significance
These results suggest the potential clinical application of compound 8n as an antiangiogenic drug for cancer therapy. 相似文献6.
A study was conducted to elucidate the effectiveness of exogenous estrumate (prostaglandin F(2alpha)) treatment as a synchronizing agent for Dwarf goats and to establish the progesterone levels at different reproductive stages under two different environmental and nutritional conditions. Female Dwarf goats of various ages were raised, 10 each at two sites, viz. the Bio-Saline Research Substation (BSRS), Lahore and at the Nuclear Institute for Agriculture and Biology (NIAB), Faisalabad. The animals at the NIAB farm were reared on non-saline soil under normal grazing conditions, while the other animal lot was raised on salt-affected lands at the BSRS, Lahore and was fed on non-conventional fodders produced by salt-affected lands. The animals received two intramuscular doses (0.5 ml each) of estrumate (125 microg/ml) at 10 days interval. Nineteen of the 20 animals exhibited estrus after 56-72 h of the second injection of estrumate. The mean progesterone concentration in the NIAB and BSRS lots was 2.8 and 2.4 ng/ml, respectively, at the time of second injection and declined to the basal level (estrus) within 48 h. A gradual increase in the progesterone level occurred during the metestrus, reaching maximum during the luteal phase when it was 6.3 and 6.7 ng/ml in NIAB-lot and BSRS-lot, respectively. During the proestrous phase, the progesterone level decreased to the basal level (0.1 ng/ml) at the onset of the next estrus after 22 days. The length of the induced or natural estrous cycle (20+/-1 days) was not affected by the estrumate treatment, nor by the environmental and nutritional conditions. Breeding was allowed after the natural estrous cycle at the onset of third estrus and a high fertility rate (95%) was achieved. The progesterone concentrations remained at higher level (4.5-9.4 ng/ml) throughout the gestation period, declined gradually in the prepartum period, and dropped to the basal level at the completion of parturition. The results suggested that estrumate is an efficient synchronizing agent for the Dwarf goats kept under different environmental-nutritive conditions and that the progesterone profile is a useful indicator to assess the reproductive status of the goats. 相似文献
7.
Effect of age of seedling and phytohormones on micropropagation of indica rice (Oryza sativa L.) from Meristem Culture. 总被引:1,自引:0,他引:1
An efficient protocol forin vitro micropropagation of seven indica rice varieties was developed from meristem culture. Meristem (leaf base) was isolated from
different age of seedlings and cultured on MS medium without hormones and supplemented with different concentrations of NAA
and BAP. Regeneration of plantlets from meristem was observed within five days of culture. The meristem isolated from 4-day
old seedlings gave highest regeneration on hormone free MS medium. Histological study of meristem (leaf base) from 4-day old
seedlings confirmed the presence of meristematic cells. Regenerated plants were multiplied on MS medium supplemented with
0.05 mg/L NAA and 5 mg/L BAP. An average of five plants were obtained from single regenerated meristem. The plants regenerated
from meristem showed morphological uniformity. 相似文献
8.
Hydrogen peroxide (H2O2), a major reactive oxygen species produced during oxidative stress, has been implicated in the pathophysiology of various neurodegenerative conditions. Cyperus rotundus is a traditional medicinal herb that has recently found applications in food and confectionary industries. In the current study, the neuroprotective effects of Cyperus rotundus rhizome extract (CRE) through its antioxidant and anti-apoptotic machinery to attenuate H2O2-induced cell damage on human neuroblastoma SH-SY5Y cells have been explored. The results obtained demonstrate that pretreatment of cells with CRE for 2 h before administration of H2O2 for 24 h ameliorates the cytotoxicity induced by H2O2 as evidenced by MTT and LDH assays. CRE exhibited potent antioxidant activity by regulating the enzymes/proteins levels such as SOD, CAT, GPx, GR, HSP-70, Caspase-3, and Bcl-2. The pretreatment restored H2O2-induced cellular, nuclear, and mitochondrial morphologies as well as increased the expression of Brain derived nerve growth factor (BDNF). The anti-oxidant and anti-apoptotic potentials of the plant extract may account for its high content of phenolics, flavonoids, and other active principles. Taken together, our findings suggest that CRE might be developed as an agent for neurodegeneration prevention or therapy. 相似文献
9.
Angiotensin II receptors and inhibitory actions in Leydig cells 总被引:2,自引:0,他引:2
Rat Leydig cells possess functional high-affinity receptors for angiotensin II (AII). AII inhibits adenylate cyclase activity in Leydig cell membranes and reduces basal and human chorionic gonadotropin (hCG)-stimulated cAMP pools and testosterone production in intact cells. Treatment of cells with an inhibitory dose of forskolin (10(-9) M) and a submaximal dose of AII caused additive inhibition of hCG-stimulated events. The inhibitory action of AII was largely prevented by pertussis toxin prior to the addition of AII alone or in the presence of hCG. This study and our recent report on inhibitory action of low doses of forskolin, 10(-12)-10(-9) M (Khanum, A., and Dufau, M.L. (1986) J. Biol. Chem. 261, 11456-11459) are indicative of a pertussis toxin-sensitive subunit of adenylate cyclase available for acute regulation of Leydig cell function. 8-bromo-cAMP bypasses the inhibitory effect of forskolin as well as AII. We have, therefore, demonstrated functional AII high-affinity receptor and an acute inhibitory effect of AII on hCG action in Leydig cells. Our results have provided evidence for a pertussis toxin-sensitive guanine nucleotide inhibitory protein as mediator of the effect of AII. These findings further emphasized the importance of the cAMP pathway in the Leydig cells, and studies also suggest that tubular and locally produced AII could negatively modulate luteinizing hormone stimulation of Leydig cells. 相似文献
10.
Prabhakar BT Khanum SA Jayashree K Salimath BP Shashikanth S 《Bioorganic & medicinal chemistry》2006,14(2):435-446
A series of substituted benzophenone analogues, (2-aroyl-4-methylphenoxy)acetamides 4a-e, have been synthesized via three-step synthesis sequence beginning with the 2-hydroxybenzophenones 1a-e in excellent yield. 1a-e on reaction with ethyl chloroacetate afford ethyl (2-aroyl-4-methylphenoxy)acetates 2a-e which on alkaline hydrolysis afforded (2-aroyl-4-methylphenoxy)ethanoic acid 3a-e. Compounds 3a-e on condensation with p-chloroaniline furnished benzophenone analogues 4a-e. In the present report, we investigated the anti-tumor and proapoptotic effect of benzophenones in Ehrlich ascites tumor (EAT) cells. Treatment of benzophenones in vivo resulted in inhibition of proliferation of EAT cells and ascites formation. Further, we demonstrate that the induction of apoptosis in EAT cells is mediated through activation of caspase-3. These results suggest a further possible clinical application of these synthetic compounds as potent anti-tumor and proapoptotic compounds. 相似文献