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.

Authors :: Reddy TS
Kumar KS
Meda CL
Kandale A
Rambabu D
Krishna GR
Hariprasad C
Rao VV
Venkataiah S
Reddy CM
Naidu A
Dubey PK
Parsa KV
Pal M
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3248-55. Date of Electronic Publication: 2012 Mar 14.
Publication Year :: 2012
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Crystallography, X-Ray
Drug Design
Indazoles chemistry
Indazoles pharmacology
Models, Molecular
Molecular Conformation
Phosphodiesterase 4 Inhibitors chemical synthesis
Pyrazoles pharmacology
Indazoles chemical synthesis
Phosphodiesterase 4 Inhibitors chemistry
Pyrazoles chemistry

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