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Start Over Author "Parsa KV" Journal bioorganic medicinal chemistry
2 results on '"Parsa KV"'

1. Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.

Author

Reddy SV, Rao GM, Kumar BV, Meda CL, Deora GS, Kumar KS, Parsa KV, and Pal M

Subjects
Animals, Cell Line, Cyclic Nucleotide Phosphodiesterases, Type 4 metabolism, Molecular Docking Simulation, Oxazines chemical synthesis, Sulfonamides chemical synthesis, Oxazines chemistry, Oxazines pharmacology, Phosphodiesterase 4 Inhibitors chemistry, Phosphodiesterase 4 Inhibitors pharmacology, Sulfonamides chemistry, Sulfonamides pharmacology
Abstract

A number of novel imidazophenoxazine-4-sulfonamides have been designed as potential inhibitors of PDE4. All these compounds were readily prepared via an elegant multi-step method involving the initial construction of 1-nitro-10H-phenoxazine ring and then fused imidazole ring as key steps. Some of these compounds showed promising PDE4B and D inhibition when tested in vitro and good interactions with these proteins in silico. Three of these compounds showed dose dependent inhibition of PDE4B with IC50 value of 3.31 ± 0.62, 1.23 ± 0.18 and 0.53 ± 0.18 μM., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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2. C-C bond formation at C-2 of a quinoline ring: synthesis of 2-(1H-indol-3-yl)quinoline-3-carbonitrile derivatives as a new class of PDE4 inhibitors.

Author

Kumar KS, Kiran Kumar S, Yogi Sreenivas B, Gorja DR, Kapavarapu R, Rambabu D, Rama Krishna G, Reddy CM, Basaveswara Rao MV, Parsa KV, and Pal M

Subjects
Aluminum Chloride, Aluminum Compounds chemistry, Binding Sites, Carbon chemistry, Cell Proliferation drug effects, Chlorides chemistry, Computer Simulation, Crystallography, X-Ray, Cyclic Nucleotide Phosphodiesterases, Type 4 metabolism, HEK293 Cells, Humans, Indoles chemistry, Molecular Conformation, Phosphodiesterase 4 Inhibitors chemistry, Phosphodiesterase 4 Inhibitors pharmacology, Quinolines chemical synthesis, Quinolines pharmacology, Cyclic Nucleotide Phosphodiesterases, Type 4 chemistry, Phosphodiesterase 4 Inhibitors chemical synthesis, Quinolines chemistry
Abstract

A number of 2-(1H-indol-3-yl)quinoline-3-carbonitrile derivatives were synthesized via AlCl(3)-mediated C-C bond forming reaction between 2-chloroquinoline-3-carbonitrile and various indoles. The methodology does not require any N-protection of the indoles employed and provided the corresponding products in good yields. The molecular structure of a representative compound was established unambiguously by single crystal X-ray diffraction and structural elaboration of a compound synthesized has been demonstrated. Many of these compounds synthesized showed PDE4 inhibitory properties in vitro. A brief structure-activity relationship studies within the series along with docking results of a representative compound (EC(50) ∼0.89 μM) is presented., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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