TY - BOOK AU - Essam Eldin Abdelfattah Osman AU - Mohamed Mahmoud Hussein , AU - Sahar Mahmoud AbouSeri , AU - Samir Mohamed Elmoghazy , TI - Design and synthesis of some rimonabant congeners of anticipated pharmacological activity as cannabinoid receptor modulators / PY - 2014/// CY - Cairo : PB - Essam Eldin Abdelfattah Osman , KW - Cannabinoid receptors KW - Molecular modeling KW - Rimonabant N1 - Thesis (Ph.D.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry; Issued also as CD N2 - In this thesis, novel series of cannabinoid receptor modulators were designed. Molecular modeling techniques were used to support the design. Semicarbazone derivatives IIIa-d and thiosemicarbazone IVa- d, Va and Vb and VIIa- e, triazole derivatives XIIIa- q, XIV and XVa and XVb and furan- 3- carbonitrile derivatives XVIIIa- i, XXa- i and XXIIa- c were synthesized. Seventeen target compounds were evaluated in an in vitro functional assay for their agonist and antagonist activities at hCB1 and hCB2 receptors. Fourteen target compounds were evaluated in an affinity binding assay in vitro towards CB1 and CB2 receptors. Compounds IIIb and IVb were CB2 agonists while IIId and IVd were CB2 antagonists. Triazole derivatives XIII were active as CB1 antagonists. Furan -3- carbonitrile XVIII and XX were variably binding to both receptor subtypes ER -