Medicinal and Process Chemistry: Recent submissions

Now showing items 321-340 of 531

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.
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 ...
Antimicrobial Evaluation of Clerodane Diterpenes from Polyalthia longifolia var. pendula

Sashidhara, K V (2009)

Phytochemical investigation of the ethanolic extract of leaves of Polyalthia longifolia var. pendula has led to the isolation of seven clerodane diterpenoids and five alkaloids. (-)-14, 15-bisnor-3, 11E-kolavadien-13-one ...
Iodine catalyzed mild and efficient method for the synthesis of chalcones

Sashidhara, K V; Rosaiah, J N; Kumar, Abdhesh (2009)

Molecular iodine is found to catalyze the condensation of acetophenones with various aromatic aldehydes to prepare chalcones.
Synthesis and antihyperlipidemic activity of novel coumarin bisindole derivatives

Sashidhara, K V; Kumar, Abdhesh; Kumar, Manoj; Srivastava, Anuj; Puri, Anju (2010)

A series of novel coumarin bisindole heterocycles were synthesized following an uncommon method and evaluated for their antihyperlipidemic activity in hyperlipidemic hamster model. Among 12 compounds tested, the compound ...
Synthesis and Biological Evaluation of Indolyl Glyoxylamides as a new class of Antileishmanial agents

Chauhan, S S; Gupta, Leena; Mittal, Monika; Vishwakarma, Preeti; Gupta, Suman; Chauhan, P M S (2010)

A series of indolylglyoxylamide derivatives have been synthesized and evaluated in vitro against amastigote form of L. donovani. Compound 8c has been identified as the most active analog of the series with IC50 value of ...
Substituted 1, 2, 3, 4-Tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: Design, synthesis, biological evaluation and pharmacophore modeling

Shakya, Neeraj; Roy, K K; Saxena, A K (2009)

In search of potent beta3-adrenergic receptor agonists, a series of novel substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes has been synthesized and evaluated for their beta3-adrenergic receptor agonistic activity ...
A new protocol for masking and unmasking of vicinal hydroxyl and formyl groups in 6- hydroxyarene-1, 3-dicarboxaldehydes

Sashidhara, K V; Rosaiah, J N; Kumar, Abdhesh (2009)

A simple and efficient protocol is revealed for the masking and unmasking of α hydroxyl benzaldehyde group in aromatic dialdehydes, by foming a keto-enamine Schiff bases and subsequent unmasking by using NaN3/ DMF.
Anti-dyslipidemic and antioxidative activities of 8-hydroxyquinoline derived novel keto-enamine Schiffs bases

Sashidhara, K V; Kumar, Abdhesh; Bhatia, Gitika; Khan, M M; Khanna, A K; Saxena, J K (2009)

8-hydroxyquinoline when subjected to duff reaction resulted in the formation of unexpected 7-methylaminomethylene-8-oxo-7, 8-dihydroquinoline-5-carbaldehyde 2, which existed in the keto- enamine form, in which the aromaticity ...
Rare dipeptide and urea derivatives from roots of Moringa Oleifera as potential anti-inflammatory and antinociceptive agents

Sashidhara, K V; Rosaiah, J N; Tyagi, Ethika; Shukla, Rakesh; Raghubir, Ram; Rajendran, S M (2009)

In the course of our studies on the isolation of bioactive compounds from the roots of Moringa Oleifera, a traditional herb in southeast Asia ,rare aurantiamide acetate 4 and 1,3-dibenzyl Urea 5 has been isolated, and its ...
Consensus Superiority of the Pharmacophore-based Alignment, Over Maximum Common Substructure (MCS): 3D-QSAR Studies on Carbamates as Acetylcholinesterase Inhibitors

Chaudhaery, S S; Roy, K K; Saxena, A K (2009)

In view of the nonavailability of complete X-ray structure of carbamates co-crystallized with AChE enzyme, the 3D-QSAR model development based on co-crystallized conformer (CCBA) as well as docked conformer-based alignment ...
Application of the Pictet-Spengler reaction to aryl amine-based substrates having pyrimidine as a pi-nucleophile: Synthesis of pyrimidoquinolines with structural analogy to benzonaphthyridines present in alkaloids

Agarwal, P K; Sharma, S K; Sawant, Devesh; Kundu, Bijoy (2009)

Synthesis of pyrimidine annulated quinolines, structurally analogous to biologically active benzonaphthyridines present in alkaloids, has been described. Our synthetic strategy is based on the modified Pictet-Spengler ...
Application of the modified Pictet-Spengler cyclization reaction for the preparation of imidazopyrazine ring: Synthesis of new pyrido- and pyrimido-imidazopyrazines

Sharma, Sunil; Kundu, Bijoy (2009)

An efficient and versatile method for the synthesis of imidazopyrazine ring using the modified Pictet-Spengler strategy has been reported. The two step strategy offers rapid assembly of drug-like core templates pyridine ...
Cassane Diterpenes from Caesalpinia bonduc

Yadava, P P; Maurya, Ranjani; Sarkar, Jayanta; Arora, Ashish; Kanojiya, Sanjeev; Sinha, Sudhir; Srivastava, M N; Raghubir, Ram (2009)

Three new cassane diterpene hemiketals, caesalpinolide-C (1), caesalpinolide-D (2), caesalpinolide-E (3) and one new cassane furanoditerpene (4) were isolated from Caesalpinia bonduc. Molecular structure of new compounds ...
Application of 7-endo trig Pictet-Spengler cyclization to the formation of benzazepine ring: Synthesis of new benzazepinoindoles

Sharma, S K; Sharma, Sunil; Agarwal, P K; Kundu, Bijoy (2009)

The preparation of benzazepinoindoles, a fused heterocycles with a benzazepine moiety was realised via an intramolecular 7-endo trig Pictet-Spengler cyclization. The precursors comprising C-3- or C-2-linked o-aminobenzyl ...
New Route to the Synthesis of Isocryptolepine Alkaloid and its Related Skeletons Using the Modified Pictet-Spengler Reaction

Agarwal, P K; Sawant, Devesh; Sharma, Sunil; Kundu, Bijoy (2009)

A new route to the synthesis of isocryptolepine alkaloid with antimalarial activity has been described using the modified Pictet-Spengler reaction. The strategy was then applied to generate libraries based on the three ...
Unprecedented ‘Bridged Annulation’ Approach to the Construction of 5,6-Dihydro-4H-benzo[kl]acridines

Goel, Atul; Singh, S P; Kumar, Amit; Kant, Ruchir; Maulik, P R (2009)

A general and novel ‘bridged annulation’ methodology for the synthesis of 5,6-dihydro-4H-benzo[kl]acridines has been developed via Michael addition of a conjugate base of 9-methyl-3,4-dihydroacridin-1(2H)-one to various ...
Natural and synthetic 2H-pyran-2-ones and their versatility in

Goel, Atul; Ram, V J (2009)

The pyran ring system is widely present in the animal and plant kingdom and possesses diverse pharmacological activities. Pyran is a six-membered oxygen heterocycle with two double bonds. Out of the five carbon atoms of ...
A Mild and Efficient Bisaldolization of Ketones and its Application towards Spirocyclic 1,3-Dioxanes and Novel 1,3,5-Trioxocanes.

Srinivas, Nagarapu; Marrapu, V K; Bhandari, Kalpana (2009)

Bis-aldolization of aryl alkyl ketones as well as cyclic ketones with paraformaldehyde in the presence of catalytic amount L-proline and low concentration of aqueous sodium hydroxide has been developed in excellent yields. ...

Now showing items 321-340 of 531

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