Pyrazoline based MAO inhibitors: Synthesis, biological evaluation and SAR studies


JAGRAT M., BEHERA J., YABANOGLU S., ERCAN A. , UÇAR G. , SINHA B. N. , ...Daha Fazla

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, cilt.21, ss.4296-4300, 2011 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 21 Konu: 14
  • Basım Tarihi: 2011
  • Doi Numarası: 10.1016/j.bmcl.2011.05.057
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
  • Sayfa Sayıları: ss.4296-4300

Özet

Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of hMAO-A isoform with SI(MAO-A) in the order 10(3) and 10(4). Ten molecules with unsubstituted ring A and without ring C (21-30), in which eight molecules (21, 23-26, and 28-30) were selective for hMAO-A, one for hMAO-B (22) and the other one non-selective (27). Presence of ring C increases potency as well as SI towards hMAO-A; however its absence decreases both potency and SI towards hMAO-A and hMAO-B. (C) 2011 Elsevier Ltd. All rights reserved.