Novel compounds targeting InhA for TB therapy

AlMatara M., Makky E. A., VAR I., KAYAR B., KÖKSAL F.

PHARMACOLOGICAL REPORTS, cilt.70, sa.2, ss.217-226, 2018 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Derleme
  • Cilt numarası: 70 Sayı: 2
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1016/j.pharep.2017.09.001
  • Dergi Adı: PHARMACOLOGICAL REPORTS
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.217-226
  • Anahtar Kelimeler: Tuberculosis, Isoniazid resistance, Enoyl ACP reductase, InhA inhibitor, Novel drugs, CARRIER PROTEIN REDUCTASE, KILL MYCOBACTERIUM-TUBERCULOSIS, MATCHED MOLECULAR PAIRS, GALLIC ACID-DERIVATIVES, ENOYL-ACP REDUCTASE, DRUG-RESISTANCE, ANTIINFLAMMATORY ACTIVITY, ISONIAZID-RESISTANT, ANTIMYCOBACTERIAL ACTIVITY, ANTIMICROBIAL RESISTANCE
  • Çukurova Üniversitesi Adresli: Evet

Özet

Tuberculosis (TB) is described as lethal disease in the world. Resistant to TB drugs is the main reason to have unfavourable outcomes in the treatment of TB. Therefore, new agents to replace existing drugs are urgently needed. Previous reports suggested that InhA inhibitors, an enoyl-ACP-reductase, might provide auspicious candidates which can be developed into novel antitubercular agents. In this review, we explain the role of InhA in the resistance of isoniazid. Furthermore, five classes of InhA inhibitors, which display novel binding modes and deliver evidence of their prosperous target engagement, have been debated. (C) 2017 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Sp. z o. o. All rights reserved.