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

A simple synthesis of novel 4,5-dihydro-1H-benzo[g]indazoles, their PDE4B inhibitory properties, docking studies of few compounds and X-ray single crystal data of one compound are presented. A number of novel 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles based on a conformationally...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 22; no. 9; pp. 3248 - 3255
Main Authors:	Shyamsunder Reddy, T., Shiva Kumar, K., Meda, Chandana L.T., Kandale, Ajit, Rambabu, D., Rama Krishna, G., Hariprasad, C., Venugopala Rao, V., Venkataiah, S., Malla Reddy, C., Naidu, A., Dubey, P.K., Parsa, Kishore V.L., Pal, Manojit
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 01-05-2012 Elsevier
Subjects:	Benzo[g]indazole Biological and medical sciences chemical derivatives Crystallography, X-Ray Docking Drug Design enzyme inhibitors General pharmacology in vitro studies Indazoles - chemical synthesis Indazoles - chemistry Indazoles - pharmacology Medical sciences Models, Molecular Molecular Conformation PDE4 Pharmacology. Drug treatments Phosphodiesterase 4 Inhibitors - chemical synthesis Phosphodiesterase 4 Inhibitors - chemistry phosphoric diester hydrolases Physicochemical properties. Structure-activity relationships Pyrazole pyrazoles Pyrazoles - chemistry Pyrazoles - pharmacology structure-activity relationships X-radiation X-ray Docking Benzo[g]indazole X-ray PDE4 Pyrazole Molecular rigidity Enzyme Enzyme inhibitor Steric hindrance Molecular interaction Esterases Phosphoric diester hydrolases Modeling Phosphodiesterase 4 inhibitor Structure activity relation Molecular model Pyrazole derivatives Hydrolases Chemical synthesis 3',5'-cyclic AMP phosphodiesterase
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Summary:	A simple synthesis of novel 4,5-dihydro-1H-benzo[g]indazoles, their PDE4B inhibitory properties, docking studies of few compounds and X-ray single crystal data of one compound are presented. 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.
Bibliography:	http://dx.doi.org/10.1016/j.bmcl.2012.03.029 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.03.029