Conventional and microwave assisted synthesis of pyrazolone Mannich bases possessing anti-inflammatory, analgesic, ulcerogenic effect and antimicrobial properties.
In the present study, an efficient synthesis of some Mannich base of 5-methyl-2-[(2-oxo-2H-chromen-3-yl)carbonyl]-2,4-dihydro-3H-pyrazol-3-one (4a-j) have been described by using conventional and non-conventional (microwave) techniques. Microwave assisted reactions showed that require shorter reaction time and good yield. The newly synthesized compounds were screened for their anti-inflammatory, analgesic activity, antioxidant, and antibacterial effects were compared with standard drug. Among the compounds studied, compound (4f) showing nearly equipotent anti-inflammatory and analgesic activity than the standard drug (indomethacin), along with minimum ulcerogenic index. Compounds (4b and 4i) showing 1.06 times more active than ciprofloxacin against tested Gram-negative bacteria.
Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Kalapatti Road, Kovai Estate, Coimbatore 641 048, Tamilnadu, India. Electronic address: sivaveni2004@gmail.com.
Kullampalayam Krishnasamy
KK
Sivakumar
Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Kalapatti Road, Kovai Estate, Coimbatore 641 048, Tamilnadu, India.
Aiyalu
A
Rajasekaran
Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Kalapatti Road, Kovai Estate, Coimbatore 641 048, Tamilnadu, India.
Palaniappan
P
Senthilkumar
Department of Pharmaceutical Chemistry, KMCH College of Pharmacy, Kalapatti Road, Kovai Estate, Coimbatore 641 048, Tamilnadu, India.
Prasad P
PP
Wattamwar
D019342:Acetic Acid; D000700:Analgesics / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D002351:Carrageenan / Q000008:administration & dosage; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D051379:Mice; D008826:Microbial Sensitivity Tests; D008872:Microwaves; D015394:Molecular Structure; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy; D047069:Pyrazolones / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000700:Analgesics; D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D047069:Pyrazolones; D002351:Carrageenan; D019342:Acetic Acid
Analgesic; Anti-inflammatory; Antibacterial; Antioxidant; Coumarins; Pyrazolone