ABSTRACT
In search for a new analgesic and anti-inflammatory agent with improved potency, we designed and synthesized a series of 3,2-(4,5-dihydro-5-(4-morphilinophenyl)-1H-pyarazol-3-yl)phenols 6(a-g) and its N-phenylpyrazol-1-carbothioamide 7(a-g) by Claisan-Schmidt condensation followed by the reaction of hydrazine hydrate. All the synthesized compounds were assayed for their in vivo analgesic and anti-inflammatory activities. All the compounds synthesized showed the potential to demonstrate analgesic and anti-inflammatory activity, of particular interest compounds 6a, 6b, 6g, 7a, 7d and 7g were found comparable to Diclofenac.
Subject(s)
Analgesics/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Diclofenac , Drug Design , Edema/chemically induced , Edema/drug therapy , Hydrazines , Mice , Pain/chemically induced , Pain/drug therapy , RatsABSTRACT
1-Hexenesulphonic acid sodium salt as catalyst for green synthesis of bis(indol-3-yl)methanes was described. The reaction of indole with various aldehydes in water using ultrasound irradiation at ambient temperature for appropriate time using 1-hexenesulphonic acid sodium salt furnish the desired product in good to excellent yield. Utilization of aqueous medium, simple reaction conditions, isolation, and purification makes this manipulation very interesting from an economic and environmental perspective.
Subject(s)
Anisoles/chemical synthesis , Indoles/chemical synthesis , Sulfonic Acids/chemistry , Aldehydes/chemistry , Alkenes/chemistry , Chemistry, Organic/methods , Green Chemistry Technology , Indoles/chemistry , Methane/chemistry , Models, Chemical , Solvents/chemistry , Temperature , Time Factors , Ultrasonics , Water/chemistryABSTRACT
In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacterial activities against gram-negative and gram-positive bacteria. The preliminary structure-activity relationship, to elucidate the essential structure requirements for the antimicrobial activity that results into anti-MRSA (methicillin-resistant S. aureus) potential, has been described. Amongst the synthesized compounds 7d, 7e, 7f and 7h were found to possess activity against methicillin-resistant S. aureus in addition to the activity against other bacterial strains such as E. faecalis, S. pneumoniae, and E. coli.
