204527-99-1Relevant academic research and scientific papers
Analogues of azepinomycin as inhibitors of guanase
Rajappan, Vasanthakumar P.,Hosmane, Ramachandra S.
, p. 1141 - 1151 (1998)
Synthesis and biochemical screening against guanase of analogues of the naturally occurring guanase inhibitor azepinomycin (2) are reported. Compound 6-amino-5,6,7,8,-tetrahydro-4H-imidazo[4,5-e][1,4]diazepine-5,8-dione (3) was synthesized in six steps commencing with 1-benzyl-5-nitroimidazole-4- carboxylic acid (5). Compound 3 and its synthetic precursor 3-benzyl-6-(N- benzyloxycarbonyl)amino-5,6,7,8-tetrahydro-4H-imidazo[4,5-e][1,4]diazepine- 5,8-dione (12) were screened against rabbit liver guanase. Both were found to be moderate inhibitors of the enzyme with K(l)'s in the range of 10-4 M.
Synthesis and guanase inhibition studies of a novel ring-expanded purine analogue containing a 5:7-fused, planar, aromatic heterocyclic ring system
Rajappan, Vasanthakumar,Hosmane, Ramachandra S.
, p. 3649 - 3652 (2007/10/03)
The synthesis of a novel planar, potentially aromatic, ring-expanded xanthine analogue (1), containing the 5:7-fused imidazo[4,5-e][1,4]diazepine ring system, along with guanase inhibition studies are reported. The compound was synthesized in six steps, starting from 1-benzyl-5-nitroimidazole-4- carboxylic acid (2), and was biochemically screened against rabbit liver guanase. Compound 1 is a moderate competitive inhibitor of the enzyme with a K(i) of 2.27 ± 0.66 x 10-4 M.
Pentafluorophenol: A superior reagent for condensations in heterocyclic chemistry
Rajappan, Vasanthakumar P.,Hosmane, Ramachandra S.
, p. 753 - 764 (2007/10/03)
The use of pentafiuorophenol as a superior reagent for heterocyclic condensations, where other traditional condensing agents such as DCC and CDI failed, has been demonstrated.
