NISCAIR Online Periodicals Repository Community: IJC-B Vol.51B [2012]

An efficient synthesis of lactarochromal from 6-amino-2,2-dimethylchroman-4-one

Title: An efficient synthesis of lactarochromal from 6-amino-2,2-dimethylchroman-4-one

Authors: Kamat, Vijayendra P; Asolkar, Ratnakar N; Kirtany, Janardan K

Abstract: Lactarochromal 1, a metabolite of Lactarius deliciosus, has been synthesised starting from 6-amino-2,2-dimethylchroman-4-one 3, which in turn, is prepared from paracetamol via the known intermediates. The amino compound 3 is then converted to the iodo compound 4, followed by formylation of the latter using N-formylpiperidine to provide, efficiently, the natural product 1 in good yield.

Page(s): 1761-1762

QSAR analysis on inhibitors of human dihydroorotate dehydrogenase
(hDHODH): The aryl carboxylic acid amide derivatives

Title: QSAR analysis on inhibitors of human dihydroorotate dehydrogenase
(hDHODH): The aryl carboxylic acid amide derivatives

Authors: Vyas, Vivek K; Ghate, Manjunath

Abstract: Structural and physicochemical requirements of aryl carboxylic acid amide derivatives for the inhibition of human dihydroorotate dehydrogenase (hDHODH) are explored in this QSAR study. The calculated molecular descriptors (electronic and thermodynamic) have been used to derive QSAR models between hDHODH inhibitory activity and structural properties. The best model for prediction of hDHODH inhibitory activity is obtained by applying sequential multiple linear regression (SMLR) analysis. Regression coefficient of all the descriptors is significant at more than 99% and statistically significant model with r²> 0.87 is obtained. Selected QSAR model emphasized the importance of logP, torsion energy (Et), 1,4-dihedral van der Waals interaction (1,4-VDWE) and electronic descriptor like lowest unoccupied molecular orbital (LUMO) on hDHODH inhibitory activity. Results of QSAR analysis show that logP and LUMO are the principle descriptors for inhibition of hDHODH. QSAR model has also been tested successfully for internal (q²> 0.753) and external (r²_pred> 0.621) validation criteria. It is believed that the results of this study will be helpful in the design of more potent and selective hDHODH inhibitors.

Page(s): 1749-1760

A novel alkaloid, four alkaloid precursors and a coumarin from Feronia limonia

Title: A novel alkaloid, four alkaloid precursors and a coumarin from Feronia limonia

Authors: Pitchai, P; Ulagi, R; Mohan, P S; Gengan, R M

Abstract: A new quinoline alkaloid has been isolated from the flowers of Feronia limonia along with four alkaloid precursors, one coumarin, a known steroid stigmasterol and p-coumaric acid. The structures of compounds have been elucidated on the basis of spectroscopic data and comparison with the literature.

Page(s): 1771-1775

An improved and scalable process for the synthesis of a key intermediate for Etodolac, a non-steroidal anti-inflammatory drug

Title: An improved and scalable process for the synthesis of a key intermediate for Etodolac, a non-steroidal anti-inflammatory drug

Authors: Sekharayya, M Chandra; Narayana, G Venkata; Nigam, Satish; Madhusudhan, G

Abstract: An improved and scalable method is developed for the synthesis of 7-ethyltryptophol, a key intermediate for Etodolac, a non-steroidal anti-inflammatory drug (NSAID) starting from commercially available 2-ethylphenyl hydrazine and dihydrofuran with H₂SO₄ as a catalyst in N,N-dimethylacetamide (DMAc)-H₂O (1:1) as a solvent in 69% yield. The method is easy, inexpensive and reproducible and the process is clean, high yielding and operationally simple.

Page(s): 1763-1766

NISCAIR Online Periodicals Repository Community: IJC-B Vol.51B [2012]

An efficient synthesis of lactarochromal from 6-amino-2,2-dimethylchroman-4-one

QSAR analysis on inhibitors of human dihydroorotate dehydrogenase (hDHODH): The aryl carboxylic acid amide derivatives

A novel alkaloid, four alkaloid precursors and a coumarin from Feronia limonia

An improved and scalable process for the synthesis of a key intermediate for Etodolac, a non-steroidal anti-inflammatory drug

QSAR analysis on inhibitors of human dihydroorotate dehydrogenase
(hDHODH): The aryl carboxylic acid amide derivatives