Synthesis, In Vitro and In Silico Antibacterial Evaluation of 4,5-Dihydro-1H-Indazoles


Khan R., Shah F., Salman M., Khan Z., Tavman A.

CHEMISTRYSELECT, cilt.2, sa.29, ss.9364-9368, 2017 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 2 Sayı: 29
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1002/slct.201701244
  • Dergi Adı: CHEMISTRYSELECT
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.9364-9368
  • İstanbul Üniversitesi Adresli: Hayır

Özet

Synthesis and evaluation of in-vitro and in-silico anti-bacterial potential of a series of 4, 5-dihydro-1H-indazoles is reported here. The synthesis of the target 4,5-dihydro-1H-indazoles was accomplished by reacting 1,5-diaryl,4-acetyl cyclohexen-3-one with hydrazine hydrate and selected hydrazides. All the synthesized compounds were evaluated for their anti-bacterial potential against Escherichia coli, Proteus vulgaris, Staphylococcus aureus and Salmonella typhimurium. Among the synthesized indazoles, N,N-dimethyl-4-(3-methyl-6-phenyl-4,5-dihydro-1H-indazol-4-yl)aniline and 3-methyl-4-(3-nitrophenyl)-1,6-diphenyl-4,5-dihydro-1H-indazole exhibited highest antimicrobial activity against Salmonella typhimurium i.e. MIC50 = 3.85 and 4.12 mg/ml respectively. Docking studies were also carried out to provide an insight into binding interaction with the active site of respective enzyme.