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Sen S.,GVK Bioscience | Kamma S.R.,GVK Bioscience | Potti V.R.,GVK Bioscience | Murthy Y.L.N.,Andhra University | Chaudhary A.B.,GVK Bioscience
Tetrahedron Letters | Year: 2011

We report a facile diversity oriented synthesis of α- and β-amino acids, by utilizing the pluripotent α-methylene group in a chiral bicyclic lactam as our key point of transformation. © 2011 Elsevier Ltd. All rights reserved.

Mamidala R.,GVK Bioscience | Babu Damerla V.S.,GVK Bioscience | Gundla R.,GVK Bioscience | Chary M.T.,Jawaharlal Nehru Technological University Anantapur | And 2 more authors.
RSC Advances | Year: 2014

A versatile stereoselective diversity oriented synthetic pathway to the possible spiro and fused diverse heterocyclic small molecules is described. The strategy involved the "build-couple-pair" approach involving an S NAr, Michael addition and Mannich reaction on chiral acyl bicyclic lactams 2a/b, followed by a cyclization onto the inbuilt scaffold electrophile, thereby leading to asymmetric fused and spirocyclic nitrogen heterocycles. A "post-pair" phase has been incorporated to generate more polar compounds. We used Principal Component Analysis (PCA) and polar moment of inertia to evaluate the shape-space diversity of our scaffolds with respect to a commercial database and observed extraordinary diversity within the scaffold network. We further calculated the polar surface area (PSA) of our molecules which is an indicator for drug cell permeability. © 2014 The Royal Society of Chemistry.

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