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• Aboul-Fadl, T
• Abdel-Aziz, H
• Kadi, A
• Ahmad, P
• Elsaman, T
• Attwa, M
• Darwish, I
• [+] on Google Scholar
• Aboul-Fadl, T
• Abdel-Aziz, H
• Kadi, A
• Ahmad, P
• Elsaman, T
• Attwa, M
• Darwish, I
• [+] on PubMed
• Aboul-Fadl, T
• Abdel-Aziz, H
• Kadi, A
• Ahmad, P
• Elsaman, T
• Attwa, M
• Darwish, I

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Molecules 2011, 16(6), 5194-5206; doi:10.3390/molecules16065194

Article

Microwave-Assisted Solution-Phase Synthesis and DART-Mass Spectrometric Monitoring of a Combinatorial Library of Indolin-2,3-dione Schiff Bases with Potential Antimycobacterial Activity

Tarek Aboul-Fadl* , Hatem A. Abdel-Aziz, Adnan Kadi, Pervez Ahmad, Tilal Elsaman, Mohamed W. Attwa and Ibrahim A. Darwish

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia

* Author to whom correspondence should be addressed.

Received: 9 May 2011; in revised form: 12 June 2011 / Accepted: 21 June 2011 / Published: 22 June 2011

(This article belongs to the Section Medicinal Chemistry)

Download PDF Full-Text [307 KB, uploaded 22 June 2011 13:51 CEST]

Abstract: A combinatorial library composed of eleven hydrazides A-K and eleven indolin-1,2-dione derivatives 1-11 has been designed to formally generate sublibraries of 22 mixtures, M₁-M₂₂ comprising of 121 Schiff bases, A-K(1-11). The designed library has been synthesized by the solution-phase method and microwave-assisted synthetic techniques. The formation of individual compounds of each mixture was confirmed by Direct Analysis in Real Time (DART) as ionization technique connected to an Ion Trap as a mass detector. The synthesized mixtures were evaluated for their antimycobacterial activity against four Mycobacterium strains; M. intercellulari, M. xenopi, M. cheleneoi and M. smegmatis. Variable antimycobacterial activity was revealed with the investigated mixtures and maximum activity was shown by M₈, M₁₀, M₁₁, and M₁₅ with MIC values of 1.5, 3.1, 6.2 and 0.09 μg/mL, respectively. Application of the indexed method of analysis on these active mixtures revealed that compounds D₈, D₁₀ and D₁₁ may contribute to the activity of the tested mixtures.

Keywords: combinatorial library; Schiff bases; solution-phase synthesis; microwave irradiation; indolin-2,3-dione; DART; antimycobacterial activity

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