Synthesis and biological evaluation of certain pyrazole derivatives derived from natural products and other synthetic analogues / Ahmed Abbass Mohamed Abdelrahman Selim ; Supervised Fatma Abdelfattah Ragab , Enas Ibrahim Mohamed , Yassin Mohammed Nissan Soliman

Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Although the majority of drugs used in clinical practice are exclusively prepared synthetically, plants have always played an important role as a source of medicines. Ammi visnaga (khella) is a widely distributed ancient egyption medicinal plant. The furochromone khellin, the major constituent of ammi visnaga seeds has been used to treat a variety of diseases including renal colic, kidney stones, coronary diseases, bronchial asthma, vitilligo and psoriasis. In addition, several semisynthetic derivatives of khellin have been semisynthesized and tested for their various medicinal properties. The present investigation described the semisynthesis of certain new pyrazolylchalcones 106a,band their corresponding pyrazolylpyrazoline derivatives 107a-d starting from khellin. Also another series of pyrazolylchalcones 108a-c and their corresponding pyrazolylpyrazoline derivatives 109a-c and 110a-f derived from hydroxyacetophenones have been synthesized. In addition synthesis of new pyrazole derivatives 113a-c, 115a-c and 117-119 derived from 5-aminopyrazoles were described. All the semisynthesized and synthesized derivatives have been tested for their anti-inflammatory activity and selectivity through in vitro enzyme inhibition assay and the most active compounds were tested in vivo for their anti-inflammatory activity and showed good activity

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