Medicinal and Process Chemistry: Recent submissions

Now showing items 301-320 of 531

Synthetic studies towards potent cytostatic macrolide rhizopodin: stereoselective synthesis of the C16-C28 fragment†

Chakraborty, T K; Sreekanth, Midde; Pulukuri, K K (2011)

A stereoselective synthesis of the C16-C28 fragment of cytostatic C2-symmetric macrolide rhizopodin is described. Enantioselective addition of a chiral thiazolidinethione derived titanium enolate to acetal, Evans' aldol ...
RCM-based approach to 7- and 8-member ring-fused β-Carboline

Hutait, Samiran; Batra, Sanjay (2010)

RCM-based new route to the synthesis of 7- and 8-member ring-fused β-Carboline from Morita-Baylis-Hillman adduct or Barbier-allylation product of N-allyl-1-formyl-9H-β-Carboline is described.
One pot protecting group free synthesis of multifunctional biphenyl methyl-C-β-d-glycosides in aqueous medium

Misra, Mridul; Sharma, Rahul; Kant, Ruchir; Maulik, P R; Tripathi, R P (2011)

One pot reaction of the butenonyl-C-glycosides with malononitrile in the presence of K2CO3 in water under mild reaction conditions led to the formation of small library of multifunctional biphenyl methyl-C-glycosides in ...
Facile synthesis of Dihydroquinoline-fused-Canthines via intramolecular

Hutait, Samiran; Singh, Virender; Batra, Sanjay (2010)

The synthesis of dihydroquinoline-fused-canthines via intramolecular aza-Diels-Alder reaction between N-prenylated-1-formyl-9H--carbolines and substituted anilines in the presence of Lewis acid followed by oxidation is ...
Synthesis and bio-evaluation of alkylaminoaryl phenyl cyclopropyl methanones as antitubercular and antimalarial agents

Ajay, Arya; Singh, Vandana; Singh, Shubhra; Pandey, S K; Gunjan, Sarika; Dubey, Divya; Sinha, Sudhir; Singh, B N; Chaturvedi, Vinita; Tripathi, R; Ramachandran, Ravishankar; Tripathi, R P (2010)

A series of 4-alkylaminoaryl phenyl cyclopropyl methanones (6a-6u and 8a-8c) were synthesized in good yields from two 4-fluorochalcones (3a and 3b) by cyclopropanation of double bond followed by nucleophilic substitution ...
A QSAR study on 2-(4-Methylpiperazin-1-yl)quinoxalines as human histamine H4 receptor ligands

Sharma, B K; Pilania, Pradeep; Singh, P; Prabhakar, Y S (2011)

The histamine H4 receptor binding affinity of 2-(4-Methylpiperazin-1-yl)quinoxaline derivatives have been quantitatively analyzed in terms of Dragon descriptors. The derived QSAR models have provided rationales to explain ...
Expeditious Synthesis of Imidazole- and Pyrrole-Fused Benzodiazocines

Mishra, Amita; Batra, Sanjay (2010)

A straightforward strategy for the synthesis of imidazole fused-benzodiazocine from 1-(2-nitrophenyl)-1H-imidazole-2-carbaldehyde via Morita-Baylis-Hillman reaction followed by reductive intramolecular cyclization is ...
Ti (III)-mediated opening of 2, 3-epoxy alcohols to build five-membered carbocycles with multiple chiral centres†

Sreekantha, Midde; Pranitha, Gavinolla; Jagadeesh, B; Chakraborty, Tushar Kanti (2011)

Stereoselective construction of highly substituted five-membered carbocycles with multiple chiral centres is described. Sharpless kinetic resolution was applied as the key step to prepare the required 2,3-epoxy alcohols ...
Recent advances in the design and synthesis of heterocycles as anti-tubercular agents

Sunduru, Naresh; Sharma, Moni; Chauhan, P M S (2010)

Due to the unusual structure and chemical composition of the mycobacterial cell wall, effective TB treatment is difficult, which makes many antibiotics ineffective and hinders the entry of drugs. With approximately 33% of ...
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 ...
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 ...
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 ...

Now showing items 301-320 of 531

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