International Science Community Association Research Journal of Chemical Sciences 2231 - 606X 6 1 2016 January 18 Synthesis and Biological activities of 1,2-Benzisoxazoles and their N-Glucosides 61 68 EN A Ewais Hassan 1 Chemistry Department, Faculty of Science, King Abdulaziz University, P.O Box.80203, Jeddah, 21589, SAUDI ARABIA Abdel-Salam Ahmed H 2 Chemistry Department, Faculty of Science, Alexandria University, Alexandria, EGYPT Ismail Mohamed K 3 Chemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef City, EGYPT S.B. Dare 1 Department of Chemistry, New Arts Commerce and Science College, Ahmednagar, Maharashatra, INDIA A. Vijayalakshmi 1 Department of Chemistry, RMK Engineering College, Chennai, Tamilnadu, India Balraj Vidyavathy 2 Department of Chemistry, Velammal Engineering College, Chennai, Tamilnadu, India B. Chithra 3 Department of Chemistry, RMK Engineering College, Chennai, Tamilnadu, India V.S. Gavhane 1 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, MS, India D.M. Suryawanshi 2 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, MS, India A.S. Rajbhoj 3 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, MS, India S.T Gaikwad 4 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, MS, India Habeeb Jabrail Fawzi 1 Polymer Research Lab. Chemistry Department, Science College, Mosul University, Mosul, IRAQ E. Mahmood Mahmood 2 Polymer Research Lab. Chemistry Department, Science College, Mosul University, Mosul, IRAQ O.A. Ogbonna 1 Department of Environmental Management and Toxicology, Michael Okpara University of Agriculture, Umudike, Abia State, NIGERIA P.C. Ogbonna 2 Department of Environmental Management and Toxicology, Michael Okpara University of Agriculture, Umudike, Abia State, NIGERIA M.C. Dike 3 Department of Forestry and Environmental Management, Michael Okpara University of Agriculture, Umudike, Abia State, NIGERIA F.C. Ibe 1 Department of Chemistry, Imo State University P.M.B 2000, Owerri, Imo State, NIGERIA P.C. Njoku 2 Department of Chemistry, Federal University of Technology P. M.B. 1526, Owerri, Imo State, NIGERIA Jude I. Alinnor 3 Department of Chemistry, Federal University of Technology P. M.B. 1526, Owerri, Imo State, NIGERIA A.I. Opara 4 Department of Geology, Federal University of Technology 1526, Owerri, Imo State, NIGERIA Harish Kumar 1 Electrochem. and Mat. Sci. Lab., Dept. of Chemistry, Ch. Devi Lal University, Sirsa, 125 055, Haryana, INDIA Vikas Yadav 2 Electrochem. and Mat. Sci. Lab., Dept. of Chemistry, Ch. Devi Lal University, Sirsa, 125 055, Haryana, INDIA V. Punatkar Yogesh 1 Department of Chemistry, Mahatma Jyotiba Phule, Educational Campus, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, INDIA Rajendra K. Wanare 2 Department of Chemistry, Mahatma Jyotiba Phule, Educational Campus, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, INDIA Ravin M. Jugade 3 Department of Chemistry, Mahatma Jyotiba Phule, Educational Campus, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, INDIA > Research Paper 2015 8 30 2016 January 18 2-oximinoacetyl-4-acetyl phenol 2 was prepared by the interaction of 2,4-diacetyl phenol 1 with hydroxylamine hydrochloride using suitable solvent. Cyclization of product 2 with acetic anhydride using N,N-Dimethylformamide afforded 3-methyl-5-acetyl-1,2-benzisoxazole 3. Nitration of compound 3 with nitrating mixture produces 3-methyl-5-acetyl-7-nitro-1,2-benzisoxazole 4. 3-Methyl-5-acetyl-7-amine-1,2-benzisoxazole 5 was prepared by the reduction of product 4 using tin and hydrochloric acid. Different 3-methyl-5-(3̍-aryl prop-2̍-enoyl)-7-amine-1,2-benzisoxazoles 6a-j have been synthesized by the interaction of appropriate 3-methyl-5-acetyl-7-amine-1,2-benzisoxazole 5 with different aromatic aldehydes using piperidine. The reaction of 3-methyl-5-(3̍-aryl prop-2̍-enoyl)-7-amine-1,2-benzisoxazoles 6a-j with hydrazine hydrate in alcoholic KOH to obtained 3-methyl-5-(3̍-aryl-1H- pyrazol-5̍-yl)-7-amine-1,2-benzisoxazoles 7a-j. Condensation of tetra-O-acetyl-α-D-glucopyranosyl bromide with compounds 7a-j furnishes 3-methyl-5-(3̍-aryl-1H-pyrazol-5̍-yl)-7-amine-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-1,2-benzisoxazoles 8a-j which on deprotection to get 3-methyl-5-(3̍̍-aryl-1H- pyrazol-5̍-yl)-7-amine-(β-D-glucopyranosyl)-1,2-benzisoxazoles 9a-j. The synthesized compounds were characterized on the basis of IR, 1H NMR, 13C NMR and Mass Spectroscopy, Elemental analysis, TLC, chemical properties and Polarographic studies. All compounds have been screened for antimicrobial activities and some compounds show potent activities. Copyright@ International Science Community Association