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1. Conformationally restricted novel pyrazole derivatives: synthesis of 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles as a new class of PDE4 inhibitors

Author

C. Hariprasad, G. Rama Krishna, Manojit Pal, A.Naidu, Ajit Kandale, D. Rambabu, K. Shiva Kumar, T. Shyamsunder Reddy, Kishore V. L. Parsa, C. Malla Reddy, V. Venugopala Rao, S. Venkataiah, Chandana Lakshmi T. Meda, and P. K. Dubey

Subjects
Models, Molecular, Indazoles, Molecular model, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Molecular Conformation, Pharmaceutical Science, Pyrazole, Crystallography, X-Ray, Biochemistry, Combinatorial chemistry, chemistry.chemical_compound, chemistry, Docking (molecular), Drug Design, Drug Discovery, Molecular Medicine, Pyrazoles, Phosphodiesterase 4 Inhibitors, PDE4 Inhibitors, Molecular Biology
Abstract

A number of novel 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles based on a conformationally restricted pyrazole framework have been designed as potential inhibitors of PDE4. All these compounds were readily prepared by using simple chemistry strategy. The in vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized along with the X-ray single crystal data of a representative compound is presented.

Published
2012

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