Abstract

A series of title compounds 2 and 3 were efficiently synthesized via the condensation of 10–hydroxycamptothecin with various symmetric (O,O′-monoaryl)-thiophosphoryl chlorides and asymmetric (O-ethyl-O′-aryl)-thiophosphoryl chlorides in sodium hydroxide powder and acetonitrile system. The structures of title compounds 2 and 3 were confirmed by elemental analysis, IR, 1H NMR, 13C NMR, 31P[1H] NMR,and mass spectral data. These symmetric [(O,O′-monoaryl)-thiophosphoryl)]-(20S)-camptothecin (2a–f) and asymmetric [(O-ethyl-O′-aryl)-thiophosphoryl)]-(20S)-camptothecin (3a–f) compounds were also tested for their in vitro antimicrobial activities against some bacterial strains, namely, S. aureus, B. Simplex, E. acetylicum, E. coli, P. aeruginosa, S. flexenari, S. aureus, S. typhi, and some fungal strains Aspergillus niger, Aspergillus flavus (molds), S. cerevisiae, C. albicans, T. longifucus, A. flavus, M. canis, F. solani, and C. glaberata (yeasts). Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the related elements to view the free supplemental file.

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