- An efficient and facile synthesis of D-cycloserine substantially free from potential impurities
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An efficient and facile synthesis of D-cycloserine has been developed from D-serine with 61% overall yield employing protectiondeprotection strategy. Different parameters affecting the impurities content and yield of D-cycloserine have been studied. Mild reaction conditions provided the product with remarkable purity (>99%) and high stability.
- Awasthi, Arun Kumar,Kumar, Brijesh,Aga, Mushtaq A,Tripathi, Punit,Reddy, Cirandur Suresh,Kumar, Pramod
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p. 1248 - 1253
(2018/02/14)
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- Pharmacophore assessment through 3-D QSAR: Evaluation of the predictive ability on new derivatives by the application on a series of antitubercular agents
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Pharmacophoric mapping is a useful procedure to frame, especially when crystallographic receptor structures are unavailable as in ligand-based studies, the hypothetical site of interaction. In this study, 71 pyrrole derivatives active against M. tuberculosis were used to derive through a recent new 3-D QSAR protocol, 3-D QSAutogrid/R, several predictive 3-D QSAR models on compounds aligned by a previously reported pharmacophoric application. A final multiprobe (MP) 3-D QSAR model was then obtained configuring itself as a tool to derive pharmacophoric quantitative models. To stress the applicability of the described models, an external test set of unrelated and newly synthesized series of R-4-amino-3-isoxazolidinone derivatives found to be active at micromolar level against M. tuberculosis was used, and the predicted bioactivities were in good agreement with the experimental values. The 3-D QSAutogrid/R procedure proved to be able to correlate by a single multi-informative scenario the different activity molecular profiles thus confirming its usefulness in the rational drug design approach.
- Friggeri, Laura,Ballante, Flavio,Ragno, Rino,Musmuca, Ira,De Vita, Daniela,Manetti, Fabrizio,Biava, Mariangela,Scipione, Luigi,Di Santo, Roberto,Costi, Roberta,Feroci, Marta,Tortorella, Silvano
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p. 1463 - 1474
(2013/07/26)
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