TY - JOUR
AU - Talele, Tanaji T.
AB - A group of novel N‐1‐substituted indazole‐3‐carboxamide derivatives were synthesized and evaluated as inhibitors of poly(ADP‐ribose)polymerase‐1 (PARP‐1). A structure‐based design strategy was applied to a weakly active unsubstituted 1H‐indazole‐3‐carboxamide 2, by introducing a three carbon linker between 1H‐indazole‐3‐carboxamide and different heterocycles, and led to compounds 4 (1‐(3‐(piperidine‐1‐yl)propyl)‐1H‐indazole‐3‐carboxamide, IC50 = 36 μm) and 5 (1‐(3‐(2,3‐dioxoindolin‐1‐yl)propyl)‐1H‐indazole‐3‐carboxamide, IC50 = 6.8 μm). Compound 5 was evaluated in rats for its protective action against diabetes induced by a treatment with streptozotocin, a known diabetogenic agent. In addition to preserving the ability of the pancreas to secrete insulin, compound 5 was also able to attenuate the ensuing hyperglycemic response to a significant extent.
TI - Design and Synthesis of N ‐Substituted Indazole‐3‐Carboxamides as Poly(ADP‐ribose)polymerase‐1 (PARP‐1) Inhibitors
JF - Chemical Biology & Drug Design
DO - 10.1111/j.1747-0285.2011.01302.x
DA - 2012-04-01
UR - https://www.deepdyve.com/lp/wiley/design-and-synthesis-of-n-substituted-indazole-3-carboxamides-as-poly-xKT65afORV
SP - 488
VL - 79
IS - 4
DP - DeepDyve
ER -