Shridhar G. Hegde

Discovery of imidazole glycerol phosphate dehydratase inhibitors through 3-D database searching

Imidazole glycerol phosphate dehydratase (IGPD) has become an attractive target for herbicide discovery since it is present in plants and not in mammals. Currently no knowledge is available on the 3-D structure of the IGPD active site. Therefore, we used a pharmacophore model based on known inhibitors and 3-D database searches to identify new active compounds. In vitro testing of compounds from the database searches led to the identification of a class of pyrrole aldehydes as novel inhibitors of IGPD.

Design and synthesis of β-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase

We describe the synthesis and enzymatic activity of a library of beta-carboxamido phosphonates as inhibitors of imidazole glycerol phosphate dehydratase (IGPD). Biological results suggest the presence of an enzymatic interaction site not previously observed for other inhibitors of IGPD.

AROMATIZATION OF CYCLOHEXENONES WITH IODINE/SODIUM ALKOXIDE. A REGIOSELECTIVE SYNTHESIS OF 2-IODOPHENOLS

Abstract Aromatizations of a wide variety of easily accessible 2-cyclohexenone-4-carboxylates with iodine and sodium ethoxide give the corresponding 2-iodophenols in good yield and high regioselectivity.

ANNULATION WITH METHYL 4-(TRIPHENYLPHOSPHORANYLIDENE)ACETOACETATE. APPLICATION TO THE SYNTHESIS OF A 1,3-BENZENEDICARBOXYLATE DERIVATIVE

Abstract A synthesis of cyclohexenone 3 via an annulation reaction of 4-(triphenylphosphoranylidene)acetoacetate and aromatization of 3 to a 1,3-benzenedicarboxylate derivative are described.