Browsing by Author "Supervisor By: Dr. Mohammad Arfan"

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    19_Evaluation of Antibacterial, Antifungal, Antioxidant Activities and Phytochemistry fo Selected Species Belonging to Families Pinaceae, Solanaceae and Guttiferae
    (INSTITUTE OF CHEMICAL SCIENCES, 2009) Mumtaz Ali; Supervisor By: Dr. Mohammad Arfan
    All praises to Almighty Allah, the creator of universe Who created human beings as the best of the creatures. Many thanks to Him, who blessed us with knowledge to differentiate between right and wrong. Many thanks to Him as He blessed us with the Holy Prophet Hazrat Muhammad (Peace be upon Him) for Whom the whole universe was created. The Prophet (Peace be upon Him) enabled us to worship only one Allah. He (PBUH) brought us out of darkness and enlightened the ways to the Heaven. I feel great pleasure in expressing my ineffable thanks to my ever encouraging, inspirational, cool minded and learned supervisor Prof.Dr. Mohammad Arfan (Director, Institute of Chemical Science), whose personal interest, thought provoking guidance, valuable suggestions and discussions enabled me to complete this tedious work. He really encouraged me in all my attempts during this research work. Deep senses of gratitude and heartfelt thanks are owed to Dr. Raza Shah (HEJRIC University of Karachi) and Dr. Derek (University of Bradford UK) for their thoughts provoking discussions, valuable suggestions and their assistance in spectral and biological studies throughout my research in their research laboratories. I am thankful to Prof.Dr. Rasool Jan (Ex-Director, Institute of Chemical Science) in facilitating my research by taking bold steps for the proper utilization of indigenous fellowship funds. Thanks to all the faculty members, especially to all teachers of organic chemistry section for their morale boosting and encouraging behavior. I am highly indebted to the HEC Pakistan, for financial support through its Indigenous PhD Scheme and also for sponsoring my research visit to University of Bradford UK under the commendable scheme (IRSIP).
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    Functionalization and Heteroannulation of Quinazolone Nucleus-Synthesis, Structure Elucidation and Bioactivity Evaluation
    (INSTITUTE OF CHEMICAL SCIENCES, 2008) RASOOL KHAN; Supervisor By: Dr. Mohammad Arfan
    The research work documented in this dissertation presents the synthesis and bioactivity evaluation of some quinazolin-4(3.H)-one based heterocyclic compounds. Part first is concerned with the synthesis and synthetic methods both reported and newly designed and developed, while the second part is about the bioassays evaluation of the synthesized quinazolin-4(3H)-ones. 2-Aryl -4H-3,1-benzoxazin-4-one and methyl-Nacylanthranilates were prepared as starting materials for further transformations into a series of various 2,3-disubstituted quinazolin-4(3H)-ones. Keeping in view the extensive applications of 2-aryl -4H-3,1-benzoxazin-4-one as precursor in the quinazolin-4(3H)-ones chemistry, a new, cheaper andfacile one-pot method for the synthesis of 2-aryl -4H-3,1-benzoxazin-4-one was developed making use of readily available substituted benzoic acids. A faster and high- yielding microwaveassisted, solvent free method was also developed for the synthesis of methyl-2- [(trifluoroacetyl) amino] benzoate. Both the 2-aryl -4H-3,1-benzoxazin-4-one and methyl-N-acylanthranilates synthesized were then utilized for the synthesis of 3-amino, 2-alkyl/aryl quinazolin- 4(3H)-ones and 2,3-disubstituted quinazolin-4(3H)-ones. Consequently, a series of fifteen (19-33) 3-amino- 2-alkyl/aryl substituted quinazolin-4(3H)-ones anda series of twenty seven (46-62) 2,3-disubstituted quinazolin-4(3 H)-ones were synthesized. The necessity of development of new, cheaper and faster methods was realised and as a result, a simpler and less tedious three component one-pot method for the synthesis of ten ( 22-31) 3-amino, 2-aryl quinazolin-4(3H)-ones was developed starting from the available substituted benzoic acid. As a consequenceof the effect of substituents on the reactivity of 2-aryl -4H-3,1- benzoxazin-4-ones, three structurally novel quinazolin-4(3H)-ones (34-36) were synthesized from substituted 2-phenyl-4H-3,1-benzoxazin-4-ones. It was found that phenyl group substituted at position 2 failed to give any product. Reasons for the observed effect onthe reactivity are proposed. Keepingin view the importance of the nature and position of substituents in drug discovery, a series of (37-62) 2, 3-disubstituted quinazolin-4(3H)-ones were synthesized employing three different methods. The effect of substituents on the reactivity and the