title: Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening.
abstract: A novel series of fluoro substituted pyrazolylpyrazolines 7a-l was synthesized in good to excellent yield (77-88%) from pyrazole chalcones 5a-d and substituted phenyl hydrazine hydrochlorides 6a-c under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic stains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Compounds 7a, 7b, 7g, 7h, 7j and 7k displayed excellent activity against P. falciparum stain as compared to quinine IC50 0.268. Good antitubercular activity was exhibited by compounds 7a, 7e, 7h and 7k. Some of them also exhibited superior antibacterial activity as compared to the first line drugs.
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388 120 Gujarat, India. Electronic address: krdsharad1126@gmail.com.
authors.forename: Sharad C
authors.initials: SC
authors.lastname: Karad
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388 120 Gujarat, India.
authors.forename: Vishal B
authors.initials: VB
authors.lastname: Purohit
authors.affiliation: Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, 388 120 Gujarat, India. Electronic address: dipanalka@yahoo.com.
authors.forename: Dipak K
authors.initials: DK
authors.lastname: Raval
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000962:Antimalarials; D011720:Pyrazoles
keywords: Antimalarial activity; Antimicrobial activity; Antituberculosis activity; Microwave irradiation; Pyrazolylpyrazolines