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M.Ajitha * et al. /International Journal Of Pharmacy&Technologyk: R=H, R 1 =H, R 2 =C 8 H 5 N 2 O(5-phenyl-1,3,4-oxadiazole)l: R=CH 3 , R 1 =H, R 2 = C 8 H 5 N 2 O(5-phenyl-1,3,4-oxadiazole)m: R=Cl, R 1 =H, R 2 = C 8 H 5 N 2 O(5-phenyl-1,3,4-oxadiazole)n: R=Br, R 1 =H, R 2 = C 8 H 5 N 2 O(5-phenyl-1,3,4-oxadiazole)o: R=H, R 1 =CH 3 , R 2 = C 8 H 5 N 2 O(5-phenyl-1,3,4-oxadiazole)p: R=H, R 1 =H, R 2 =C 8 H 5 N 2 S(5-phenyl-1,3,4-thiadiazole)q: R=CH 3 , R 1 =H, R 2 = C 8 H 5 N 2 S(5-phenyl-1,3,4-thiadiazole)r: R=Cl, R 1 =H, R 2 = C 8 H 5 N 2 S(5-phenyl-1,3,4-thiadiazole)s: R=Br, R 1 =H, R 2 = C 8 H 5 N 2 S(5-phenyl-1,3,4-thiadiazole)t: R=H, R 1 =CH 3 , R 2 = C 8 H 5 N 2 S(5-phenyl-1,3,4-thiadiazole)The structure target compounds are depicted in Figure-1. Isatin hydrazones were obtained from an appropriateisatin in alcohol along with dropwise addition of hydrazine hydrate [6]. Isatin-3-[N 2 -(chloroacetyl)] hydrazonewere synthesized by refluxing isatin hydrazone with chloro acetyl chloride in dry benzene under anhydrousconditions using calcium chloride guard tube for 2h [7]. Isatin-3-[N 2 -(heteryl-2-thioacetyl)] hydrazones (a – t)were synthesized by refluxing Isatin-3-[N 2 -(chloroacetyl)] hydrazone with an appropriate heteryl-2-thione(Benzimidazole-2-thione; 4,5-diphenyl imidazole-2-thione; 5-phenyl-1,3,4-oxadiazole-2-thione, and 5-phenyl-1,3,4,-thiadiazole-2-thione) in dry pyridine for 30 min [8].All the newly synthesized compounds werecharacterized by physical, spectral (IR, PMR) and elemental analysis. Antibacterial and antifungal screening wascarried out using the dilution agar technique [9,10]. Test organisms Bacteria: Bacillus subtilis, Staphylococcusaureus, Escherichia coli, Bacillus macarances. Fungi:Pencillium minioluteum, Fusarium solani. Evaluation ofantimicrobial activity as follows.Since the compounds were poorly water soluble, they were dissolved in propylene glycol. In order to ensure thatthe solvent had no effect on bacterial growth, an inoculated control test was performed with only propylene glycolat the same dilutions used in our experiment and found inactive in culture media. The compound suspensions wereIJPT | March-2011 | Vol. 3 | Issue No.1 | 1449-1455 Page 1451

M.Ajitha * et al. /International Journal Of Pharmacy&Technologyadded at the desired concentration into nutrient agar medium for bacteria and potato-dextrose agar medium forfungi. After solidification, 1µl of the final suspension of 10 8 bacteria or 10 5 fungi/ml were applied with a multipointinoculator. Cultures were incubated for 24h at 37 o C for bacteria and 48 h for fungi. Ampicillin and clotrimazolewere used as reference compounds. The zone of inhibition of the compounds that completely inhibited growth wasconsidered and expressed in cm. The zone of inhibition was the mean of three measurements. Results of thecompounds of antibacterial and antifungal were presented in Table-1. The title compounds were screened for H 1 -antihistaminic activity on guinea pig ileum and antimuscarinic activity on rat jejunum by standard methods [11].Then the IC50 of all the test compounds were recorded and compared with that of the standard drugs, results arepresented in Table-2.Table-1: Antibacterial and antifungal activity of isatin-3-[N 2 -heteryl-2-thioacetyl] hydrazones:Compound* B.subtilis B.macerences E.coli S.aureus P.minioleuteum F.solania 6 6 10 6 14 15B 7 7 9 7 16 12C 12 8 11 12 12 13d 14 9 9 12 14 12e 6 6 8 8 15 10F 8 8 10 14 12 7G 10 9 10 14 12 10H 12 10 9 20 12 12I 14 11 13 22 14 10J 8 12 9 14 12 8K 4 - 6 6 8 -L 6 - 8 8 10 -M 6 - 8 9 14 -N 6 - 12 9 12 -O 6 - 14 11 10 -P 12 - 6 9 11 10Q 9 - 12 8 18 14R 8 - 11 15 15 9S - - - - 16 12T - - - - 12 7Ampicillin* 19** 18** 15** 18** ---------------- -------Clotrimazle* 20** 22***10 µg/disk**Zone of inhibition in cm - not reported.IJPT | March-2011 | Vol. 3 | Issue No.1 | 1449-1455 Page 1452

Reference:M.Ajitha * et al. /International Journal Of Pharmacy&Technology1. Debat, J.: Chem. Aastr. 72, 125053 (1970)2. Ayls, A.; Neibioglu, D.: Pak. J. Pharmacol. 6, 1 (1995)3. Johnson, R.G.; Kidd, D.: J. Chem. Soc. 34, 47 (1964)4. Grinberg, B.; Mazylis, L.; Benhena, M.; Chemya vasaka, S.; Prikulis, A.: Chemija. 2, 87 (1980)5. Mueller, M.: Med. Exptl. 7, 155 (1982)6. Bansal, R.K.: Textbook of Heterocyclic Chemistry, 2.Ed., p.271, New Age International, New York 19967. Vanallan, J.A.; Deacon, B.D.: Organic. Synthesis. Collective. 6, 569 (1993)8. Purushotham, E.; Rajashekharan, P.V.N.: Ind.J.Chem.29, 18 (1990)9. National Committee for clinical Laboratory Standards Villanova, Pa. (1983)10. Ericsson, H.M.; Sherris, J.C.: Acta.Path. Scand. Sect. B.Suppl.217, 1 (1971)11. Raghu Ram Rao, A.; Prabhakar, M.C.: Methods Find. Exp.Clin. Pharmacol. 22, 191 (2000)Corresponding Author:Dr. M. Ajitha*Center for Pharmaceuticals SciencesJNTU, Kukatpally,Hyderabad-500082Ph: 040-23158666Email:Phd03@rediffmail.comIJPT | March-2011 | Vol. 3 | Issue No.1 | 1449-1455 Page 1455