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Research Paper Open Access
The ACAT inhibitory activity, -log IC50 (molar), of N-phenyl-6,11-dihydrodibenzo[b,e]oxepin-11- carboxamides and related derivatives, has been quantitatively correlated with structural and electronic substituent parameters; the sum of molar refraction, Î£MR for the R1, the Kier's Î” parameter and a hydrogen bond count parameter, HB for 2-R2 and the sum of Î” parameters, Î£Î”â€™ for the 3-R2, R3, X, and Y-Z. The analysis has revealed that for good ACAT inhibitory activity, the substituent R1 should have a large MR value while 2-R2 should have a higher Î” but a lower HB. The remaining variations at 3-R2, R3, X, and Y-Z parts should be such that these give a lower Î£Î”' values.
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Author(s): P Singh R Kumar