title: Synthesis and biological evaluation of pyrazolylthiazole carboxylic acids as potent anti-inflammatory-antimicrobial agents.
abstract: Current Letter presents design, synthesis and biological evaluation of a novel series of pyrazolylthiazole carboxylates 1a-1p and corresponding acid derivatives 2a-2p. All 32 novel compounds were tested for their in vivo anti-inflammatory activity by carrageenan-induced rat paw edema method as well as for in vitro antimicrobial activity. All the tested compounds exhibited excellent AI activity profile. Three compounds 1p (R=Cl, R(1)=Cl), 2c (R=H, R(1)=F) and 2n (R=Cl, R(1)=OCH3) were identified as potent anti-inflammatory agents exhibiting edema inhibition of 93.06-89.59% which is comparable to the reference drug indomethacin (91.32%) after 3h of carrageenan injection while most of the other compounds displayed inhibition ⩾80%. In addition, pyrazolylthiazole carboxylic acids (2a-2p) also showed good antimicrobial profile. Compound 2h (R=OCH3, R(1)=Cl) showed excellent antimicrobial activity (MIC 6.25μg/mL) against both Gram positive bacteria comparable with the reference drug ciprofloxacin (MIC 6.25μg/mL).
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Poonam
authors.initials: P
authors.lastname: Khloya
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Satish
authors.initials: S
authors.lastname: Kumar
authors.affiliation: Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Pawan
authors.initials: P
authors.lastname: Kaushik
authors.affiliation: Department of Microbiology, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Parveen
authors.initials: P
authors.lastname: Surain
authors.affiliation: Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Dhirender
authors.initials: D
authors.lastname: Kaushik
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India. Electronic address: pksharma@kuk.ac.in.
authors.forename: Pawan K
authors.initials: PK
authors.lastname: Sharma
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D002264:Carboxylic Acids / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005658:Fungi / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007213:Indomethacin / Q000494:pharmacology / Q000627:therapeutic use; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000737:chemistry; D051381:Rats; D013844:Thiazoles / Q000737:chemistry
chemical_list: D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D002264:Carboxylic Acids; D011720:Pyrazoles; D013844:Thiazoles; D007213:Indomethacin
keywords: Anti-inflammatory activity; Antimicrobial activity; Pyrazole; Thiazole