排序方式: 共有12条查询结果,搜索用时 15 毫秒
1.
Ramakrishna V.S. Nirogi Rajeshkumar Badange Ramasastri Kambhampati Anil Chindhe Amol D. Deshpande Vinaykumar Tiriveedhi Vishwottam Kandikere Nageswararao Muddana Renny Abraham Mukkanti Khagga 《Bioorganic & medicinal chemistry letters》2012,22(24):7431-7435
4-(Piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. The lead compound 6a, from this series shows potent in vitro binding affinity, good PK profile, no CYP liabilities and activity in animal models of cognition. 相似文献
2.
Estimation of Enantiomeric Impurity in Piperidin‐3‐Amine by Chiral HPLC With Precolumn Derivatization 下载免费PDF全文
Chittabathina Venkata Raghunadha Babu Nagi Reddy Vuyyuru K. Padmaja Reddy M.V. Suryanarayana K. Mukkanti 《Chirality》2014,26(12):775-779
A simple, precise, accurate, robust chiral high‐performance liquid chromatographic (chiral HPLC) method was developed for estimation of (S)‐piperidin‐3‐amine (S‐isomer) in (R)‐piperidin‐3‐amine dihydrochloride (R‐AMP). As AMP is a high‐melting solid and nonchromophoric compound, development of a suitable chiral method is a challenging task. The proposed chiral HPLC‐UV method involves a precolumn derivatization technique with para toluene sulphonyl chloride (PTSC) in the presence of a base to introduce chromophore into analytes. It utilizes chiralpak AD‐H column with a simple mobile phase of 0.1% diethyl amine in ethanol with a 0.5 mL/min flow rate. Analytes were monitored by using a UV detector at 228 nm. The resolution between the two enantiomers was more than 4.0. The developed method was validated as per current International Conference on Harmonization (ICH) guidelines. Chirality 26:775–779, 2014. © 2014 Wiley Periodicals, Inc. 相似文献
3.
Mukesh Kumar Das Prafulla Kumar Sahu G. Srinivasa Rao K. Mukkanti L. Silpavathi 《Saudi Journal of Biological Sciences》2014,21(6):539-546
Bioprospecting of marine natural products has recently produced a substantial number of drug candidates. Ulva fasciata Delile, belonging to the family Ulvaceae, is a green marine macro alga that grows profusely on the coastal seashore of South India. In the present study, we investigated the in vitro cytotoxic potential of a methanolic extract of U.fasciata Delile (MEUF) using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay against human colon carcinoma (HT-29), human hepatocyte carcinoma (Hep-G2), and human breast carcinoma (MCF-7) cell lines. Response surface methodology (RSM) was applied using central-composite experimental design (CCD) to obtain optimum combined effect of concentration and cancer cells with highest cytotoxicity. The effect of concentration, cancer cell lines as independent variables on absorbance (OD), percent cell survival and percent cell inhibition as dependent variables was investigated. Maximum cytotoxic activity of MEUF was established for Hep-G2 with lowest OD or percent cell survival; highest percent cell inhibition with significant difference (p > 0.05) was compared to HT-29 and MCF-7. 相似文献
4.
Facile synthesis of substituted thiophenes via Pd/C-mediated sonogashira coupling in water 总被引:1,自引:0,他引:1
Raju S Kumar PR Mukkanti K Annamalai P Pal M 《Bioorganic & medicinal chemistry letters》2006,16(24):6185-6189
The first successful Pd/C-mediated Sonogashira coupling of iodothiophene with terminal alkynes in water is described here. Pd/C-CuI-PPh3 was found to be an efficient catalyst system for this coupling reaction. Using this economic and reliable process a variety of acetylenic thiophenes with a wide range of functional groups were prepared in good yields. Synthetic applications and in vitro anticancer properties of some of the compounds synthesized are described. 相似文献
5.
Sang Keun Ha Donthabhaktuni Shobha Eunjung Moon Murugulla A. Chari Kagga Mukkanti Sung-Hoon Kim Kwang-Hyun Ahn Sun Yeou Kim 《Bioorganic & medicinal chemistry letters》2010,20(13):3969-3971
A series of 2,3-dihydro-1,5-benzodiazepines were synthesized and evaluated for anti-inflammatory effects in microglia cells. Among the 1,5-benzodiazepines tested, compound 3e strongly inhibited LPS-induced nitric oxide (NO) production, with an IC50 value of 7.0 μM in the microglia cells. Also, compound 3e significantly inhibited the enzymatic activity of inducible NO synthase (iNOS) without changes in iNOS protein expression or NO scavenging activity. This result suggests that compound 3e showed anti-neuroinflammatory effects by suppressing iNOS enzyme activity. 相似文献
6.
Balasekhara R. Challa Sai H.S. Boddu Bahlul Z. Awen Babu R. Chandu Chandrasekhar K. Bannoth Mukkanti Khagga Kanchanamala Kanala Rihana P. Shaik 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》2010,878(19):1499-1505
The present study aims at developing a simple, sensitive and specific liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the quantification of pantoprazole sodium (PS) in human plasma using pantoprazole D3 (PSD3) as internal standard (IS). Chromatographic separation was performed on Zorbax SB-C18, 4.6 mm × 75 mm, 3.5 μm, 80 Å column with an isocratic mobile phase composed of 10 mM ammonium acetate (pH 7.10): acetonitrile (30:70, v/v), pumped at 0.6 mL/min. PS and PSD3 were detected with proton adducts at m/z 384.2 → 200.1 and 387.1 → 203.1 in multiple reaction monitoring (MRM) positive mode, respectively. Precipitation method was employed in the extraction of PS and PSD3 from the biological matrix. This method was validated over a linear concentration range of 10.00–3000.00 ng/mL with correlation coefficient (r) ≥ 0.9997. Intra- and inter-day precision of PS were found to be within the range of 1.13–1.54 and 1.76–2.86, respectively. Both analytes were stable throughout freeze/thaw cycles, bench top and postoperative stability studies. This method was successfully utilized in the analysis of blood samples following oral administration of PS (40 mg) in healthy human volunteers. 相似文献
7.
Indium(III) chloride catalyzed microwave assisted acetylation of different carbohydrates is an efficient synthesis of per-O-acetyl derivatives and provides the products in good to excellent yields. 相似文献
8.
Shravankumar Kankala Ranjith Kumar Kankala Prasad Gundepaka Niranjan Thota Srinivas Nerella Mohan Rao Gangula Hanmanthu Guguloth Mukkanti Kagga Ravinder Vadde Chandra Sekhar Vasam 《Bioorganic & medicinal chemistry letters》2013,23(5):1306-1309
Regioselective synthesis of isoxazole–mercaptobenzimidazole hybrids and their efficiency in in vivo analgesic and anti-inflammatory activity was described. A comparison of structure–activity relationship for there compounds was also emphasized. 相似文献
9.
Gorja DR Shiva Kumar K Kandale A Meda CL Parsa KV Mukkanti K Pal M 《Bioorganic & medicinal chemistry letters》2012,22(7):2480-2487
The design and synthesis of 4-alkynyl pyrazole derivatives has led to the identification of new class of PDE4 inhibitors. All these compounds were accessed for the first time via a facile Pd/C-CuI-PPh(3) mediated C-C bond forming reaction between an appropriate pyrazole iodide and various terminal alkynes. In vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized indicated that 4-alkynyl pyrazole could be a promising template for the discovery of novel PDE4 inhibitors. 相似文献
10.
Total synthesis of phenylpropanoid glycosides, grayanoside A and syringalide B, through a common intermediate 总被引:1,自引:0,他引:1
Phenylpropanoid glycosides are known as bioactive natural products. Two of them, grayanoside A (1) and syringalide B (2), were synthesized through a common intermediate, using benzyl as temporary protecting group following a shorter route. 相似文献