Abstract:A new series of 27 diethyl 2-(phenylcarbamoyl)phenyl phosphorothioates (thiophosphates) was synthesized, characterized by NMR, IR and CHN analyses and evaluated against Mycobacterium tuberculosis H 37 Rv, Mycobacterium avium and two strains of Mycobacterium kansasii. The best activity against M. tuberculosis was found for O- {4-bromo-2-[(3,4-dichlorophenyl)carbamoyl]phenyl} O,O-diethyl phosphorothioate (minimum inhibitory concentration of 4 µM). The highest activity against nontuberculous mycobacteria was exhibited by O-(5-chloro-2-{[4-(trifluoromethyl)phenyl]carbamoyl}-phenyl) O,O-diethyl phosphorothioate with MIC values from 16 µM. Prepared thiophosphates were also evaluated against acetylcholinesterase from electric eel and butyrylcholinesterase from equine serum. Their inhibitory activity was compared to that of the known cholinesterases inhibitors galanthamine and rivastigmine. All tested compounds showed a higher (for AChE inhibition) and comparable (for BChE inhibition) activity to that of rivastigmine, with IC 50 s within the 8.04 to 20.2 µM range.

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A new class of phosphorus macrocycles were synthesized from 2-[(E)-2-2 [(hydroxymethyl) phenyl] imino ethylidene) amino] phenyl methanol 1 with various phenylphosphorodichloridates, phenyldichlorophosphine, and ethyldichlorophosphite in the presence of triethylamine at 0-10 C under N 2 atmosphere in THF. All the title compounds were confirmed by analytical and spectral data (IR, 1 H-, 13 C-, 31 P-NMR, and mass). The title compounds exhibited promising anti-oxidant activity.

A phosphorus-containing dendrimer of up to four generations with phloroglucinol as a core unit was synthesised using a divergent growth method. A repetitive synthetic sequence of several types of reactions was performed by using P(O)Cl 3 , 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde and p-phenylenediamine for the synthesis of this dendritic molecule G 4 involving simple condensation reactions. This Schiff's base macromolecule possesses 12 imine bonds and 6-OH groups on the periphery. The structures of the intermediate generations G 1 , G 2 , G 3 were confirmed by IR, 1 H, 13 C, 31 P NMR and LC/EI MS. The final dendrimer G 4 was characterised by IR, 1 H, 13 C, 31 P NMR, Maldi-tof mass spectrometer and C, H, N analysis. The scanning electronic microscopic study and thermogravimetric analysis were also performed for the final dendrimer (G 4 ).

Polyethylene Glycol Promoted Dialkyl, Aryl/Heteroaryl Phosphonates -An efficient, ecofriendly synthesis of novel phosphonates (III) (12 examples) in polyethylene glycol, which serves as reaction medium and catalyst, is achieved. -(NAIDU, K. R. M.; DADAPEER, E.; REDDY, C. B.; RAO, A. J.; REDDY, C. S.; RAJU*, C. N.; Synth. Commun. 41 (2011) 23, 3462-3468, http://dx.