TY - JOUR
T1 - Synthesis of novel indolyl-pyrimidine antiinflammatory, antioxidant and antibacterial agents
AU - Panda, S.
AU - Chowdary, P.V.R.
N1 - Cited By :23
Export Date: 10 November 2017
CODEN: IJSID
Correspondence Address: Panda, S.; Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Mahe Manipal-576 104, India; email: sivashankarpanda@yahoo.com
Chemicals/CAS: 1,1 diphenyl 2 picrylhydrazyl, 1898-66-4; acetophenone, 98-86-2; alcohol, 64-17-5; carrageenan, 9000-07-1, 9049-05-2, 9061-82-9, 9064-57-7; guanidine, 113-00-8, 25215-10-5, 50-01-1; hydrochloric acid, 7647-01-0; ibuprofen, 15687-27-1; indole 3 aldehyde, 487-89-8; sodium hydroxide, 1310-73-2; thiourea, 62-56-6; urea, 57-13-6
References: Patel, D.H., Mistry, B.D., Desai, K.R., Synthesis and antimicrobial activity of pyrazolo[3,4-d]pyrimidines (2003) Indian J Hetero Chem, 13, pp. 179-180; Kreutzberger, A., Sellheim, M., Antimycotics, XIX, 4,6-Disubstituted 2-(cyanamino)pyrimidines Indian (1985) J Hetero Chem, 22, pp. 721-723; Shanker, K., Gupta, G.P., Singh, S., Synthesis of novel pyrimidinediones and thiazolidinones as cardiovascular agents (1985) Indian J Chem, 24, pp. 1094-1097; Lather, V., Chowdary, P.V., Synthesis and antimicrobial activity of N1(arylidine hydrazidomethyl)-indoles,2-(substituted aryl)-3-(N1-indolyl acetamidyl)-4-oxo-thiazolidines and 5-benzylidine derivatives of thiazolidinones (2003) Indian J Pharm Sci, 65, pp. 576-579; Gadaginamath, G.S., Shyadligeri, A.S., Kavali, R.R., Chemoselectivity of indoledicarboxylates towards hydrazine hydrate: Part III-synthesis and antimicrobial activity of novel 4-thiazolidinonylindoles (1999) Indian J Chem, 38, pp. 156-159; Renukadevi, P., Biradar, J.S., Synthesis and antimicrobial activity of 3,5-disubstituted-2-[1′-phenyl-5′-thioalkyl-s-triazol-2′-yl] indoles and 3,5-disubstituted-2-[1′-substituted aminomethyl-4′- phenyl-5′,4′-phenyl-5′(4′H)-thion-s-triazol-3-yl] indoles (1999) Indian J Hetero Chem, 9, pp. 107-112; Klohr, S.E., Cassady, M.J., An intramolecular photocyclization to form the azepino[3,4,5-cd]indole system (1988) Synthetic Communication, 18, pp. 671-674; Winter, C.A., Risley, E.A., Nuss, G.W., Carrageenin-induced edema in hind paw of the rat as an assay for antiiflammatory drugs (1962) Proc Soc Exp Biol, 111, pp. 544-547; Newbould, B.B., Chemotherapy of arthritis induced in rats by mycobacterial adjuvant (1963) Brit J Pharmacol, 21, pp. 127-136; Seeley, H.W., Van Denmark, P.J., (1975) Microbes in action: A laboratory manual of microbiology, , Mumbai: D B Taraporevala Sons and Co Pvt Ltd;; Kavanagh, F., (1963) Analytical microbiology, pp. 313-346. , New York
PY - 2008
Y1 - 2008
N2 - A number of chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in NaOH solution in ethanol. These chalcones were immediately reacted with urea, thiourea and guanidine hydrochloride in presence of concentrated hydrochloric acid as reagent to obtain the corresponding hydroxy, thio and amino pyrimidines. The synthesized heterocyclics were characterized on the basis of physical, chemical tests and spectroscopic data and were tested for the acute antiinflammatory activity, antioxidant, antibacterial activity using carragenan-induced rat paw oedema method, DPPH (diphenylpicrylhydrazyl) radical scavenging method and cup plate method using Muller-Hinton agar media respectively. Evaluation of the compounds revealed remarkable antiinflammatory activity reflected by their ability to reduce the carragenan-induced inflammation in rats, appreciable antioxidant activity and also antibacterial activity was observed.
AB - A number of chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in NaOH solution in ethanol. These chalcones were immediately reacted with urea, thiourea and guanidine hydrochloride in presence of concentrated hydrochloric acid as reagent to obtain the corresponding hydroxy, thio and amino pyrimidines. The synthesized heterocyclics were characterized on the basis of physical, chemical tests and spectroscopic data and were tested for the acute antiinflammatory activity, antioxidant, antibacterial activity using carragenan-induced rat paw oedema method, DPPH (diphenylpicrylhydrazyl) radical scavenging method and cup plate method using Muller-Hinton agar media respectively. Evaluation of the compounds revealed remarkable antiinflammatory activity reflected by their ability to reduce the carragenan-induced inflammation in rats, appreciable antioxidant activity and also antibacterial activity was observed.
U2 - 10.4103/0250-474X.41457
DO - 10.4103/0250-474X.41457
M3 - Article
SN - 0250-474X
VL - 70
SP - 208
EP - 215
JO - Indian Journal of Pharmaceutical Sciences
JF - Indian Journal of Pharmaceutical Sciences
IS - 2
ER -