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Synthesis, Characterization and in Vitro Antimicrobial Journal of Saudi Chemical Society (2011) xxx, xxx–xxx King Saud University Journal of Saudi Chemical Society www.ksu.edu.sa www.sciencedirect.com ORIGINAL ARTICLE Synthesis, characterization and in vitro antimicrobial activity of some 1-(substitutedbenzylidene) -4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)- yl)phenyl)semicarbazide derivatives Govindaraj Saravanan a,*, Veerachamy Alagarsamy b, Chinnasamy Rajaram Prakash c a Medicinal Chemistry Research Laboratory, Bapatla College of Pharmacy, Jawaharlal Nehru Technological University, Hyderabad, Andhra Pradesh, India b Medicinal Chemistry Research Laboratory, M.N.R. College of Pharmacy, Sangareddy, Andhra Pradesh, India c Department of Medicinal Chemistry, DCRM Pharmacy College, Inkollu, Andhra Pradesh, India Received 19 October 2011; accepted 6 December 2011 KEYWORDS Abstract A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl) Quinazolin-4(3H)-one; phenyl)semicarbazide derivatives were synthesized with the aim of developing potential antimicro- Semicarbazide; bials. It was characterized by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In addi- Schiff base; tion, the in vitro antibacterial and antifungal properties were tested against some human pathogenic Antibacterial activity; microorganisms by employing the disc diffusion technique and agar streak dilution method. All title Antifungal activity compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well dis- cussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay. ª 2011 King Saud University. Production and hosting by Elsevier B.V. All rights reserved. * Corresponding author. Address: Dept. of Medicinal Chemistry, Bapatla College of Pharmacy, JNT University, Hyderabad, Andhra Pradesh, India. Mobile: +91 9963023257. E-mail address: [email protected] (G. Saravanan). 1319-6103 ª 2011 King Saud University. Production and hosting by Elsevier B.V. All rights reserved. Peer review under responsibility of King Saud University. doi:10.1016/j.jscs.2011.12.010 Production and hosting by Elsevier Please cite this article in press as: Saravanan, G. et al., Synthesis, characterization and in vitro antimicrobial activity of some 1- (substitutedbenzylidene) 2 G. Saravanan et al. 1. Introduction broad spectrum of in vitro and in vivo chemotherapeutic activ- ities (El-Gazzar et al., 2009). Diverse examples of few antimi- Microbial infections are a growing problem in contemporary crobial quinazolinone are indicated in Fig. 1. Quinazolinone medicine, and the use of antibiotics is inevitable. The global derivatives such as 2-((2,6-dichlorophenylamino)methyl)qui- sales of antibiotics are generally higher when compared to nazolin-4(3H)-one I exerted antibacterial effect against Staphy- other drugs which are prescribed. Antibiotic resistance is a lococcus aureus at a very low concentration (Jantova et al., major problem in hospitals as well as in community settings. 2004); while 2-(6,8-dichloro-4-oxo-2-phenylquinazolin-3(4H)- Morbidity and mortality due to enteric bacterial infection is yl)cyclopent-4-ene-1,3-dione II and 3-(benzylideneamino)-6,8- most common around the world and in specific regions such dibromo-2-phenylquinazolin-4(3H)-one III exhibited potent as the Indian subcontinent, part of South America and tropical antimicrobial activities (Zhou et al., 2004; Panneerselvam part of Africa are worst affected (Qadri et al., 2005; Devasia et et al., 2009). A significant in vivo activity, low toxicity and good al., 2006). A continuous increase in the number of infections pharmacokinetic profile were exhibited by 7-chloro-3-(3-(2,4- caused by bacterial resistance to one or multiple class of anti- difluorophenyl)-4-(1H-1,2,4-triazol-1-yl)butan-2-yl)qui nazo- biotics poses a significant threat as it may lead to treatment lin-4(3H)-one IV (Bartroli et al., 1998; Chandrika et al., failures and associated complications (Beekmann et al., 2005; 2008). Quinazolin-4(3H)-ones with substitution such as substi- Spellberg et al., 2008). Thus the treatment of bacterial infec- tuted phenyl ring moieties (Abdel-Rahman, 1997), bridged tions remains a challenging therapeutic problem. Despite the phenyl rings (Kumar et al., 1982; Hassan et al., 1991), hetero- many antibiotics and chemotherapeutics available, the emer- cyclic rings (Pandey et al., 2009) and aliphatic systems (El- gence of old and new antibiotic resistant bacterial strains in Sharief et al., 2001; Ouyang et al., 2006) at position 3, were re- the last decades constitutes a substantial need for new classes ported to be associated with antimicrobial properties (Moham- of antibacterial agents (Chopra et al., 2008). Moreover a ed et al., 2010). spread of resistance among the common respiratory pathogens On the other hand, Schiff bases have gained importance be- was recognized as one of the three major areas of concern by cause of the physiological and pharmacological activities the Infectious Diseases Society of America which creates a associated with them. Compounds containing azomethine need for the development of newer antibiotics (Spellberg group (–C‚N–) in the structure are known as Schiff bases, et al., 2008). which are usually synthesized by the condensation of primary The importance of heterocyclic compounds has long been amines and active carbonyl groups. Schiff bases are well known recognized in the field of synthetic organic chemistry and has for their pharmacological properties like antibacterial, anti- been extensively studied due to their important properties fungal, anticancer and antiviral agents (Wang et al., 2001). and applications at present. It is well known that a number Since the quinazolinone moiety seems to be a possible of heterocyclic compounds containing nitrogen exhibited a pharmacophore in various pharmacologically active agents, we wide variety of biological activity. Among these compounds, decided to synthesize compounds with this functionality quinazolinone derivatives have become especially noteworthy coupled with Schiff base as possible antimicrobial agents which in recent years. The quinazolinone derivatives have emerged could furnish better therapeutic results. In view of the facts as antimicrobial agents of an immense interest because of their mentioned above and as part of our efforts to discover O O O Cl H Cl N N H N O N N Cl Cl 2-((2,6-dichlorophenylamino)methyl) quinazolin-4(3H)-one (I) 2-(6,8-dichloro-4-oxo-2-phenylquinazolin- 3(4H)-yl)cyclopent-4-ene-1,3-dione (II) O CH3 O N Br N C H N N N N Cl N N F Br 3-(benzylideneamino)-6,8-dibromo- F 2-phenylquinazolin-4(3H)-one (III) 7-chloro-3-(3-(2,4-difluorophenyl)-4-(1H-1,2,4- triazol-1-yl)butan-2-yl)quinazolin-4(3H)-one (IV) Figure 1 Diverse examples of antimicrobial quinazolinone. Please cite this article in press as: Saravanan, G. et al., Synthesis, characterization and in vitro antimicrobial activity of some 1- (substitutedbenzylidene) Synthesis, characterization and in vitro antimicrobial activity 3 potentially active new agents, various quinazolin-4(3H)-ones obtained was filtered, dried and recrystallized from ethanol derivatives 5a–n were synthesized and evaluated for their antimi- (Alagarsamy et al., 2002). crobial activity. 2.3.1.1. 2-Methyl-4H-benzo-(1,3)-oxazin-4-one (1a). Yield: 2. Materials and methods 71% m.p. 182 °C. IR: (KBr, cmÀ1) 3096 (Ar C–H), 2882 (CH3 C–H), 1712 (C‚O), 1636 (C‚N), 1600 (C‚C), 1055 1 2.1. General (C–O–C). H NMR (CDCl3, 300 MHz) d ppm: 2.38 (3H, s, CH3), 6.92–7.40 (4H, m, Ar–CH). ESI–MS: MS: m/z 161 + All solvents used were of laboratory grade and were obtained (M ). Anal. Cald for C9H7NO2: C, 67.07; H, 4.38; N, 8.69. from SD fine chemicals (Mumbai, India), and Merck (Mumbai, Found: C, 67.16; H, 4.40; N, 8.66. India). Melting points were determined in open glass capillary tubes and were uncorrected. Compounds were routinely 2.3.1.2. 2-Phenyl-4H-benzo-(1,3)-oxazin-4-one (1b). Yield: À1 checked for their purity on Silica gel G (Merck) thin layer chro- 80% m.p. 120 °C. IR: (KBr, cm ) 3077 (Ar C–H), 1751 1 matography (TLC) plates. Iodine chamber and UV lamp were (C‚O), 1625 (C‚N), 1616 (C‚C), 1038 (C–O–C). H used for visualization of TLC spots. The IR spectra were re- NMR (CDCl3, 300 MHz) d ppm: 6.95–7.78 (9H, m, Ar–CH). + corded in KBr pellets on (BIO-RAD FTS) FT-IR spectropho- ESI–MS: MS: m/z 223 (M ). Anal. Cald for C14H9NO2:C, tometer. 1H NMR spectra were recorded on Bruker DPX-300 75.33; H, 4.06; N, 6.27. Found: C, 75.42; H, 4.05; N, 6.29. NMR spectrometer in CDCl3 using tetramethylsilane (TMS) as an internal standard. The chemical shifts were reported in 2.3.2. Synthesis of 3-(4-aminophenyl)-2-(methyl/phenyl)- ppm scale. Mass spectra were obtained on a JEOL-SX-102 quinazolin-4(3H)-one (2a–2b) instrument using electron impact ionization. Elemental analyses 4H-benzo-(1,3)-oxazin-4-one 1a/1b (1.61/2.23 g, 0.01 mol) and for C, H, and N were performed on a Perkin Elmer model 240C p-phenylenediamine (1.08 g, 0.01 mol) were dissolved in 50 ml analyzer and were within ±0.4% of the theoretical values. of anhydrous pyridine and heated on sand bath for 6 h. The resulting solution was cooled in ice bath and treated with 2.2. Test microorganisms and medium 100 ml of dilute hydrochloric acid. The products thus sepa- rated 2a/2b were filtered, washed with water, and recrystallized All the microorganisms used in this study were purchased from from ethanol. CL laboratories, Chennai, India.
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