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1.
Both the high molecular weight and the low molecular weight variants of urinary Y-glutamyl transpeptidase, displayed transpeptidase
(pH optimum 8.6) and autotrans-peptidase (pH optimum 9.4) activities. Iodoacetamide inhibited the transpeptidase activity
more efficiently than the autotranspeptidase activity with respect to both variants of Y-glutamyl transpeptidase. The high
molecular weight form utilized L-glutamine as a better acceptor than L-cystine during the transpeptidation reaction whereas
the reverse was the case with the low molecular weight variant. While phenylmethylsulphonyl fluoride-treated enzymes retained
full activitiesper se, addition of maleic acid to the modified enzyme was found to inhibit the catalytic activities indicating a maleic acid-induced
conformational change of the modified enzyme. 相似文献
2.
Vema A Panigrahi SK Rambabu G Gopalakrishnan B Sarma JA Desiraju GR 《Bioorganic & medicinal chemistry》2003,11(21):4643-4653
Three-dimensional quantitative structure-activity relationship (3D-QSAR) models were developed for 100 anilinoquinazolines, inhibiting epidermal growth factor receptor (EGFR) kinase. The studies included molecular field analysis (MFA) and receptor surface analysis (RSA). The cross-validated r2 (r2cv) values are 0.81 and 0.79 for MFA and RSA, respectively. The predictive ability of these models was validated by 28 test set molecules. The results of the best QSAR model were further compared with structure-based investigations using docking studies with the crystal structure of EGFR kinase domain. The results helped to understand the nature of substituents at the 6- and 7-positions, thereby providing new guidelines for the design of novel inhibitors. 相似文献
3.
D. Rambabu Guttikonda Raja B. Yogi Sreenivas G.P.K. Seerapu K. Lalith Kumar Girdhar Singh Deora Devyani Haldar M.V.Basaveswara Rao Manojit Pal 《Bioorganic & medicinal chemistry letters》2013,23(5):1351-1357
Novel N-indolylmethyl substituted spiroindoline-3,2′-quinazolines were designed as potential inhibitiors of SIRT1. These compounds were synthesized in good yields by using Pd/C–Cu mediated coupling-cyclization strategy as a key step involving the reaction of 1-(prop-2-ynyl)-1′H-spiro[indoline-3,2′-quinazoline]-2,4′(3′H)-dione with 2-iodoanilides. Some of the compounds synthesized have shown encouraging inhibition of Sir 2 protein (a yeast homologue of mammalian SIRT1) in vitro and three of them showed dose dependent inhibition of Sir 2. The docking results suggested that the benzene ring of 1,2,3,4-tetrahydroquinazolin ring system of these molecules occupied the deep hydrophobic pocket of the protein and one of the NH along with the sulfonyl group participated in strong H-bonding interaction with the amino acid residues. 相似文献
4.
Rambabu Dakarapu Ramu Errabelli Vijaya L. Manthati Adeniyi Michael Adebesin Deb K. Barma Deepan Barma Victor Garcia Fan Zhang Michal Laniado Schwartzman John R. Falck 《Bioorganic & medicinal chemistry letters》2019,29(19):126616
19-Hydroxyeicosatetraenoic acid (19-HETE, 1), a metabolically and chemically labile cytochrome P450 eicosanoid, has diverse biological activities including antagonism of the vasoconstrictor 20-hydroxyeicosatetraenoic acid (20-HETE, 2). A SAR study was conducted to develop robust analogs of 1 with improved in vitro and in vivo efficacy. Analogs were screened in vitro for inhibition of 20-HETE-induced sensitization of rat renal preglomerular microvessels toward phenylephrine and demonstrated to normalize the blood pressure of male Cyp4a14(-/-) mice that display androgen-driven, 20-HETE-dependent hypertension. 相似文献
5.
Dev Chandran Kolli Bhaktavatsala Reddy Shahana Pallichera Vijayan Parthasarthy Sugumar Gudavalli Sudha Rani Ponsekaran Santha Kumar Lingala Rajendra Villuppanoor Alwar Srinivasan 《Indian journal of microbiology》2010,50(3):266-274
Peste des Petits Ruminants (PPR) is a highly contagious animal disease caused by the Peste des Petits Ruminants virus (PPRV) belonging to the genus morbillivirus and family Paramyxoviridae. The disease results in high morbidity and mortality
in goats, sheep and in some small wild ruminants. The presence of large number of small ruminants reared in endemic areas
makes PPR a notorious disease threatening the livelihood of poor farmers. Conventional vaccination using a live, attenuated
vaccine gives adequate protection but cannot be used in case of eradication of the disease due to difficulty in differentiation
of infected animals from the vaccinated ones. 相似文献
6.
Shiva Kumar K Adepu R Sandra S Rambabu D Rama Krishna G Malla Reddy C Misra P Pal M 《Bioorganic & medicinal chemistry letters》2012,22(2):1146-1150
A rapid and direct access to N-aryl substituted fused triazinone derivatives has been accomplished via N-arylation of 1,2,3-triazin-4-one ring involving a Cu-mediated coupling between triazinone derivatives and aryl boronic acids. A combination of Cu(OAc)(2)-Et(3)N in 1,2-dichloroethane was found to be effective and various fused triazinone derivatives have been prepared by using this methodology. Molecular structure of a representative compound was confirmed by single crystal X-ray diffraction study. The scope and limitations of this reaction is discussed. Some of the compounds synthesized were tested for chorismate mutase inhibitory properties in vitro. The in vitro dose response study of an active compound is presented. 相似文献
7.
T Bhaskar Kumar Ch Sumanth S Vaishaly M Srinivasa Rao KB Chandra Sekhar CL Meda A Kandale D Rambabu G Rama Krishna C Malla Reddy K Shiva Kumar KV Parsa M Pal 《Bioorganic & medicinal chemistry letters》2012,22(17):5639-5647
Novel polysubstituted pyrroles have been designed and accessed via a one-pot multicomponent reaction followed by Pd-mediated C-C bond forming reactions. All the compounds synthesized were tested for their PDE4B inhibitory properties in vitro and two of them obtained via Heck reaction showed significant inhibition. The docking results suggested that these alkenyl derivatives containing ester moiety interact well with the PDE4B protein in silico where the ester carbonyl oxygen played a key role. The pyrrole framework presented here could be a new template for the identification of small molecule based novel inhibitors of PDE4. The single crystal X-ray data of a representative compound is presented. 相似文献
8.
K Manjulatha S Srinivas N Mulakayala D Rambabu M Prabhakar KM Arunasree M Alvala MV Basaveswara Rao M Pal 《Bioorganic & medicinal chemistry letters》2012,22(19):6160-6165
An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofuran-3(2H)-one with a range of benzaldehydes in the presence of a mild base EDDA under ultrasound. A number of aurones were synthesized (within 5-30min) and the molecular structure of a representative compound determined by single crystal X-ray diffraction study confirmed Z-geometry of the C-C double bond present within the molecule. Some of the compounds synthesized have shown SIRT1 inhibiting as well as anti proliferative properties against two cancer cell lines in vitro. Compound 3a [(Z)-2-(5-bromo-2-hydroxybenzylidene) benzofuran-3(2H)-one] was identified as a potent inhibitor of SIRT1 (IC(50)=1μM) which showed a dose dependent increase in the acetylation of p53 resulting in induction of apoptosis. 相似文献
9.
D. Rambabu Naveen Mulakayala K. Ravi Kumar G. Pavan Kumar Chaitanya Mulakayala Chitta Suresh Kumar Arunasree M. Kalle M.V. Basaveswara Rao Srinivas Oruganti Manojit Pal 《Bioorganic & medicinal chemistry letters》2012,22(21):6745-6749
A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular structures of two representative compounds, that is, 3 and 5l were confirmed by single crystal X-ray diffraction study. All the compounds synthesized were evaluated for their cyclooxygenase (COX) inhibiting properties in vitro. The compound 5i showed balanced selectivity towards COX-2 over COX-1 inhibition and good docking scores when docked into the COX-2 protein. 相似文献
10.
K Rambabu I A Shaafie A A Ansari S A Basha M M Ziu 《Biochemical medicine and metabolic biology》1991,46(2):140-144
Variations in the levels of serum gamma-glutamyl transpeptidase (GGT) were measured in control subjects and in 39 adult primary idiopathic hypothyroidism (PIH) patients. The serum GGT activity was low in PIH patients compared to that of control subjects. A more significant correlation was found between serum GGT and T3 (r = 0.766) but not with T4 (r = 0.476). The comparison of serum GGT with TSH has revealed that those two parameters are not parallel with each other (r = -0.454). No significant correlation between serum GGT activity, age, and sex in PIH patients and control subjects was observed. The present available data indicate that measurement of serum GGT might be useful as a marker index in PIH patients. 相似文献