CSIR-CDRI Publications: Recent submissions

Now showing items 761-780 of 1093

Synthesis and in vitro evaluation of novel coumarin–chalcone hybrids as potential anticancer agents

Sashidhara, K V; Kumar, Abdhesh; Kumar, Manoj; Sarkar, Jayanta; Sinha, S (2010)

A series of coumarin-chalcone hybrids have been synthesized and evaluated for their in vitro cytotoxicity against a panel of four human cancer cell lines and normal fibroblasts (NIH3T3). Among 21 compounds screened, three ...
Neuroprotective Effect of Flurbiprofen in Focal Cerebral Ischemia: The Possible Role of ASIC1a

Mishra, Vikas; Verma, R K; Raghubir, Ram (2010)

The intracellular calcium overload resulting from glutamate excitotoxicity is considered major determinant for neuronal loss during cerebral ischemia. Moreover, acidosis mediated ASIC1a activation has also shown to promote ...
Novel Carbamates as Orally Active Acetylcholinesterase Inhibitors Found to Improve Scopolamine-Induced Cognition Impairment: Pharmacophore-Based Virtual Screening, Synthesis and Pharmacology

Chaudhaery, S S; Roy, K K; Shakya, Neeraj; Saxena, Gunjan; Sammi, Shreesh Raj; Nazir, Aamir; Nath, Chandishwar; Saxena, A K (2010)

A systematic virtual screening (VS) experiment, consisting of the development of 3D-pharmacophore, screening of virtual library, synthesis and pharmacology, is reported. The predictive pharmacophore model (correlation = ...
Utility of allylic azides for the synthesis of fused triazoles and tetrazole via intramolecular cycloaddition

Mishra, Amita; Hutait, Samiran; Bhowmik, Subhendu; Rastogi, Neeraj; Roy, Raja; Batra, Sanjay (2010)

Synthesis of a variety of annulated triazoles and tetrazoles from differently substituted allyl azides, afforded from the Baylis-Hillman adduct of acrylates, using intramolecular cycloaddition approach is described.
Discovery and synthesis of novel 3-phenylcoumarin derivatives as antidepressant agents

Sashidhara, K V; Kumar, Abdhesh; Chatterjee, Manavi; Rao, K B; Singh, S; Verma, A K; Palit, Gautam (2010)

A series of 3-phenylcoumarins were synthesized and screened for potential antidepressant activity by tail suspension test (TST) in mice. Three compounds (6, 7 and 13) exhibited impressive antidepressant activity, measured ...
Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents

Marrapu, V K; Srinivas, Nagarapu; Mittal, Monika; Shakya, Nishi; Gupta, Suman; Bhandari, Kalpana (2011)

: A novel series of trans-2-aryloxy-1,2,3,4,-tetrahydronaphthyl azoles and related cyclohexyl azoles were synthesized and evaluated in vitro against Leishmania donovani. Compound 9 identified as most active analog with ...
A QSAR study on serotonin 5-HT6 receptor ligands: indolyl and piperidinyl sulfonamides

Sharmaa, B K; Singh, P; Sarbhai, K; Prabhakar, Y S (2010)

The serotonin 5-HT6 binding affinity of indolyl- and piperidinyl-sulfonamide derivatives has been analyzed with the topological and molecular features from Dragon software. Analysis of the structural features in conjunction ...
Glutathione S-transferase (GST) Gene Variants and risk of BPH (Benign Prostatic Hyperplasia): A report in north Indian population

Konwar, Rituraj; Manchanda, P K; Chaudhary, Preeti; Nayak, V L; Singh, Vishwajeet; Bid, H K (2010)

GST is over expressed in BPH patients. Nature of association of GST polymorphism with susceptibility of BPH as a disease different from prostate is limited. The objectives of this study was to determine relationship between ...
How to improve the efficacy of existing drugs?

Batra, Sanjay (2010)

Pharmaceutical drugs have greatly contributed to public health across the globe. Yet there are evidence that drugs may perform differently in everyday clinical practice than in clinical trials which is the basis for licensing ...
Efficient Synthesis of Congeners based on a Naturally occurring Skeleton 5−7−6 Efficient Synthesis of Congeners based on a Naturally occurring Skeleton 5−7−6 Tricyclic Pyrrolo[2,1-c][1,4] Benzodiazepin-5-one via pi-cyclization

Sharma, S K; Mandadapu, A K; Kumaresan, K; Arora, Ashish; Kundu, Bijoy (2010)

An efficient method for the synthesis of a library based on a naturally occurring 5-7-6 tricyclic benzo[e]pyrrolo[1,2-a][1,4]diazepin-5-one skeleton and its derivatives via 7-endo trig Pictet–Spengler pi-cyclization is described.
4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents

Kumar, Ashok; Srivastava, Kumkum; Rajakumar, S; Siddiqi, M I; Puri, S K; Sexana, J K; Chauhan, P M S (2010)

A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity towards ...
Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents

Kumar, Ashok; Srivastava, Kumkum; Rajakumar, S; Puri, S K; Chauhan, P M S (2010)

Despite emergence of resistance to CQ and other 4-aminoquinoline drugs in most of the endemic regions, research findings provide considerable support that there is still significant potential to discover new affordable, ...
Copper-catalyzed cascade reactions of substituted 4-iodo-pyrazolecarbaldehydes with 1,2-phenylenediamines and 2-aminophenols

Nayak, Maloy; Batra, Sanjay (2010)

A new approach for the synthesis of novel annulated-pyrazoles is presented. This protocol includes an intermolecular condensation followed by a copper-mediated intramolecular C-N or C-O coupling reaction. The method is ...
Compactin production studies using Penicillium brevicompactum under solid-state fermentation conditions

Shaligram, N S; Singh, S K; Singhal, R S; Ashok, Pandey; George, Szakacs (2009)

In the present study, compactin production by Penicillium brevicompactum WA 2315 was optimized using solid-state fermentation. The initial one factor at a time approach resulted in improved compactin production of 905 μg ...
An efficient total synthesis of the anticancer agent (+)-spisulosine (ES-285) from Garner’s aldehyde

Ghosal, Partha; Shaw, A K (2010)

An efficient total synthesis of (+)-spisulosine (ES-285) was completed in nine steps from (S)-Garner’s aldehyde. The vicinal amino alcohol moiety with anti-configuration was achieved by a highly diastereoselective addition ...
RCM-based approach to 7- and 8-member ring-fused beta-carbolines

Hutait, Samiran; Batra, Sanjay (2010)

RCM-based new route to the synthesis of 7- and 8-member ring-fused beta-carboline from Morita-Baylis-Hillman adduct or Barbier-allylation product of N-allyl-1-formyl-9H-beta-carboline is described.
Role of phytochemicals in the prevention of menopausal bone loss: evidence from in vitro and in vivo, human interventional and pharmacokinetic studies

Sharan, Kunal; Siddiqui, J A; Swarnkar, Gaurav; Maurya, Rakesh; Chattopadhyay, Naibedya (2009)

Substantial body of data generated from cultured bone cells and rat models of osteoporosis support a significant bone-conserving effect of phytochemicals. Flavonoids including isoflavones, stilbenes and lignans with variable ...
TFIIH kinase places bivalent marks on the carboxyl-terminal domain of RNA polymerase II

Akhtar, M S; Heidemann, Martin; Tietjen, Joshua; Zhang, David; Chapman, R D; Eick, Dirk; Ansari, A Z (2009)

Post-translational modifications of the carboxyl-terminal domain (CTD) of the largest subunit of RNA polymerase II (Pol II) specify a code that is deciphered by proteins involved in RNA biogenesis. The CTD is comprised ...
Application of Response Surface Method For Studying the Role of Dissolved Oxygen and Agitation Speed on Gamma-Linolenic Acid Production

Ahmed, S U; Singh, S K; Pandey, Ashok; Kanjilal, Sanjit; Prasad, R B N (2009)

To study the effect of agitation speed (rpm) and dissolved oxygen concentration (DO) on the production of gamma linolenic acid by a Mucor sp. a central composite design experiment was performed in a 5-L stirred tank ...
Novel Coumarin derivatives as potential antidyslipidemic agents

Sashidhara, K V; Kumar, Abdhesh; Kumar, Manoj; Sonkar, Ravi; Bhatia, Gitika; Khanna, A K (2010)

A series of novel benzocoumarin derivatives were synthesized and evaluated for their in vivo antidyslipidemic and in vitro antioxidant activities. Among 11 compounds tested, 2 compounds showed potent antidyslipidemic ...

Now showing items 761-780 of 1093

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