Indian Journal of Chemistry

Sect. B: Organic Chemistry including Medicinal Chemistry

http://www.niscair.res.in; http://nopr.niscair.res.in

Total visitors:9325 since 07-02-2011

VOL. 50B

NUMBER 2

February 2011

CONTENTS

Papers

 

 

 

196

Synthesis and in vitro antibacterial activity of N-alkyl and N-aryl piperazine derivatives

 

Synthesis and antibacterial evaluation of N-alkyl and N-aryl substituted piperazine derivatives against S. mutans, S. aureus, B. subtilis, S. epidermidis and E. coli bacterial strains have been carried out.

 

 

 

 

 

Krishna K Singh, Subhash C Joshi & Chandra S Mathela*

 

Department of Chemistry, Kumaun University, Nainital 263 002, India

 

 

 

 

 

 

201

Montmorillonite-KSF induced Fischer indole cycli­za­tion under microwave towards a facile entry to 1-keto-1,2,3,4-tetrahydrocarbazoles

 

 

 

 

 

Suchandra Chakraborty, Gautam Chattopadhyay & Chandan Saha*

 

Department of Clinical and Experimental Pharmacology, School of Tropical Medicine, Kolkata 700 073, India

 

 

 

 

 

 

 

 

 

 

207

Design and synthesis of some azole derivatives containing 2,4,5-triphenyl imidazole moiety as anti-inflammatory and antimicrobial agents

 

A series of azole derivatives (5a-d, 6a-d and 7a-d) have been synthesized from (2,4,5-triphenyl-imidazole-1-yl)-acetic acid hydrazide under various reaction conditions. Elemental analysis, IR, 1H NMR and mass spectral data confirmed the structure of the newly synthesized compounds. All the synthesized azole derivatives have been investigated for their anti-inflammatory, antibacterial and antifungal activities and showed moderate to good activity.

 

 

 

  

 

 

 

Mohd Amir*, Iftikhar Ahsan, Wasim Akhter, S A Khan & Israr Ali

 

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, New Delhi 110 062, India

 

 

 

 

 

 

 

214

Synthesis of novel 3, 5-disubstituted-4,5-dihydro­isoxazoles and 3,4,5-trisubstituted isoxazoles and their biological activity

 

1,3-Dipolar cycloaddition of nitrile oxide generated from substituted pyridinyloxy benzaldoximes with styrene or α,β-unsaturated ketones produces a series of 3,5-disubstituted-4,5-dihydroisoxazoles and 3,4,5-trisubstituted isoxazoles. On the other hand C-chlorooxime reacts with α-unsaturated ketones yielding 3,4,5-trisubstituted isoxazoles. The compounds are tested for antimicrobial activity and action on isolated frog heart.

 

 

 

 

 

M Shailaja, A Manjula, B Vittal Rao*, B Praseeda & B Madhava Reddy

 

Organic Chemistry Division II, Indian Institute of Chemical Technology, Hyderabad 500 607, India

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

223

Synthesis and antimicrobial activity of 1-(5-methyl-3-isoxazolyl)-3,6-diaryl-4-thioxo-1,3,5-tria­zi­nan-2-ones

 

Treatment of 3-benzalamino-5-methylisoxazoles 1 with ammo­nium thiocyanate in hot acetic acid affords the corresponding N-isothiocyanato(phenyl)methyl-N-(5-methyl-3-isoxazolyl)­ami­nes 2a-j in excellent yields. N-Isoxazolyl-α-amino­iso­thiocyanates 2a-j on reaction with aryl isocyanates undergoes cyclization to give the corresponding isoxazolyl-4-thioxo-1,3,5-triazinan-2-ones 3a-l in good yields. The compounds 2a-j and 3a-l have been screened for their antimicrobial activity.

 

 

 

 

 

 

 

 

 

 

E Rajanarendar*, S Raju, M Nagi Reddy & K Govardhan Reddy

 

Department of Chemistry, Kakatiya University, Warangal 506 009, India

 

 

 

 

 

 

 

 

Notes

 

 

 

 

 

 

229

Niobium(V) pentachloride-catalyzed efficient and highly rapid synthesis of bis(indolylmethanes under mild conditions

 

NbCl5 has been found to be an extremely efficient catalyst for electrophilic substitution reaction of indole with various aromatic aldehydes at room temperature, to afford the corresponding bis(indolyl)methanes in good yields.

 

 

 

 

 

 

 

 

 

 

 

 

Mazaahir Kidwai*, Nisha Bura & Neeraj Kumar Mishra

 

Green Chemistry Research Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India

 

 

 

 

 

 

 

 

 

 

 

 

 

233

Synthesis and antimalarial activity of novel N-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-7-chloroquino­lin-4-amine and its derivatives

 

A number of N-{2-[2-(2-aminoethoxy)ethoxy]ethyl}-7-chloroquinolin-4-amine derivatives have been prepared by condensation of N-{2-[2-(2-aminoethoxy) ethoxy] ethyl}-7-chloroquinolin-4-amine with substituted aldehyde and characterized by IR, ¹H and ¹³C NMR, and mass spectral data. These compounds have been screened for in vitro antimalarial activity using the Sybr Green assay of P. falciparum in culture and the heme detoxification based Heme-HRP assay. 7-Chloro-N-[2-(2-{2-[(2,4-difluoro benzyl) amino] ethoxy} ethoxy) ethyl] quinolin-4-amine has been found to be the most effective with IC50 value 60 μM (in Heme-HRP assay) and 48 nM (in P. falciparum culture assay). These values compare well with the potency of chloroquine in the respective assays.

 

 

 

 

 

 

 

Pooja Tanwar, Gyan Chand Yadav*, U K Jaitley, Naveen Kaushik & Dinkar Sahal

 

Ranbaxy Research Laboratories, Process Research & NCE Scale Up, Gurgaon 122 001, India

 

 

 

 

 

 

 

242

Synthesis of 4-(substituted benzyl)-1H, 3H-benzo­[f]1,3,5-triazepin-2-ones

 

 

 

 

 

 

 

T Venkata Maruthikumar, G V Panakala Rao, V Prabhakar Reddy & P Hanumantha Rao*

 

Department of Chemistry, Post Graduate College of Science, Saifabad, Osmania University, Hyderabad 500 004, India

 

 

 

 

 

 

 

 

 

 

 

 

 

245

An efficient one-pot three component synthesis of new isoxazolyl polyhydroacridine-1,8-diones in an ionic liquid medium

 

A facile and convenient protocol was developed for the fast and high yielding one-pot three component synthesis of isoxazolyl polyhydroacridine-1,8-diones from dimedone, aromatic aldehyde and isoxazolyl amine in the presence of ionic liquid [bmim]+BF4- as an efficient recyclable medium.

 

 

 

 

E Rajanarendar*, M Nagi Reddy & Firoz Pasha Shaik

 

Department of Chemistry, Kakatiya University, Warangal 506 009, India

 

 

 

 

 

 

 

253

Synthesis and antimicrobial activity of bis-[2-imino-3-[5-(3-methylbenzo[b]furan-7-yl)-1,3,4-thia­diazol-2-yl]-5-(arylidene)-1,3-thiazolan-4-one]me­thanes

 

A series of novel bis-[2-imino-3-[5-(3-methylbenzo[b]furan-7-yl)-1,3,4-thiadiazol-2-yl]-5-(arylidene)-1,3-thiazolan-4-one]­­me­thanes 6a-j have been synthesized and their structures confirmed by IR, NMR, MS and elemental analyses. All the synthesized compounds have been tested for their antimicrobial activity against Gram-positive and Gram-negative bacteria, and fungi. Among the synthesized compounds, 6c, 6e, 6f and 6g are found to be the most active against Bacillus subtilis, Bacillus sphaericus, Staphylococcus aureus, Klebsiella aerogenes and Chromobacterium violaceum. Similarly, these compounds show potent antifungal effect against Candida albicans, Aspergillus fumigatus, Trichophyton rubrum and Trichophyton mentagrophytes.

 

 

 

 

 

Ch Sanjeeva Reddy*, D Chandrashekar Rao, V Yakub & A Nagaraj

 

Department of Chemistry, Kakatiya University, Warangal 506 009, India

 

 

 

 

 

 

 

260

Additions and Corrections

 

 

 

 

 

Authors for correspondence are indicated by (*)