title: Synthesis, antileishmanial activity and docking study of N'-substitutedbenzylidene-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetohydrazides.
abstract: A series of N'-substitutedbenzylidene-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetohydrazide derivatives is synthesized and evaluated for antileishmanial activity against Leishmania donovani promastigotes. Compounds 9a and 9i were shown significant antileishmanial when compared with standard sodium stilbogluconate. Antimicrobial study revealed that compound 9b has potent as well as broad spectrum antibacterial activity when compared with ampicillin and compound 9e showed promising antifungal activity when compared with miconazole. Also, none of the synthesized compounds showed cytotoxicity up to tested concentration. Further, docking study against pteridine reductase 1 enzyme of L. donovani showed good binding interactions. ADME properties of synthesized compounds were also analyzed and showed potential to develop as good oral drug candidates.
authors: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001 (M.S.), India. Electronic address: jnsangshetti@rediffmail.com.
authors: Jaiprakash N
authors: JN
authors: Sangshetti
authors: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001 (M.S.), India.
authors: Rehan I
authors: RI
authors: Shaikh
authors: Dr. Rafiq Zakaria Campus, Y.B. Chavan College of Pharmacy, Aurangabad 431001 (M.S.), India.
authors: Firoz A Kalam
authors: FA
authors: Khan
authors: Department of Biotechnology, University of Pune, Pune 411007 (M.S.), India.
authors: Rajendra H
authors: RH
authors: Patil
authors: Department of Biotechnology, University of Pune, Pune 411007 (M.S.), India.
authors: Sayali D
authors: SD
authors: Marathe
authors: Department of Biotechnology, University of Pune, Pune 411007 (M.S.), India.
authors: Wasudev N
authors: WN
authors: Gade
authors: Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431004 (M.S.), India.
authors: Devanand B
authors: DB
authors: Shinde
mesh_terms: D000284:Administration, Oral; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001597:Benzylidene Compounds / Q000737:chemistry*; D001665:Binding Sites; D015195:Drug Design; D006207:Half-Life; D006834:Hydrazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects* / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D062105:Molecular Docking Simulation; D010088:Oxidoreductases / Q000037:antagonists & inhibitors / Q000378:metabolism; D017434:Protein Structure, Tertiary; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D011725:Pyridines / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D000981:Antiprotozoal Agents; D001597:Benzylidene Compounds; D006834:Hydrazines; D015800:Protozoan Proteins; D011725:Pyridines; D010088:Oxidoreductases; C085592:pteridine reductase; C023666:pyridine
keywords: ADME properties; Antileishmanial activity; Antimicrobial activity; Docking study; L. donovani promastigotes; Thieno[3,2-c]pyridine