73120-67-9Relevant articles and documents
Palladium-Catalyzed Intramolecular Cross-Coupling of Unactivated C(sp3)-H and C(sp2)-H Bonds
Wu, Zhuo,Wu, Zechen,Sun, Xueliang,Qi, Weixin,Zhang, Zhengyang,Zhang, Yanghui
supporting information, p. 7161 - 7165 (2021/09/18)
Direct C-H/C-H coupling represents an appealing method for the construction of C-C bonds, and the cross-coupling of unactivated C(sp3)-H and C(sp2)-H bonds is challenging and remains to be investigated. We have developed the Pd-catalyzed intramolecular coupling of inert C(sp3)-H and C(sp2)-H bonds. The reaction proceeded by o-methyl oxime-directed aryl C(sp2)-H activation and subsequent alkyl C(sp3)-H cleavage, generating C(sp2),C(sp3)-palladacycles as the key intermediates. Dihydrobenzofurans and indanes were formed as the final products.
Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents
Partap, Sangh,Yar, Mohammad Shahar,Hassan, Md. Zaheen,Akhtar, Md. Jawaid,Siddiqui, Anees A.
, (2017/10/06)
A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABAA receptor.
Design, synthesis and antihypertensive screening of novel pyridazine substituted s-triazin-2-imine/one/thione derivatives
Mishra, Ravinesh,Siddiqui, Anees A.,Husain, Asif,Rashid, Mohd.,Goda, Chirag
, p. 552 - 559 (2015/02/19)
Some new 7-substituted-phenyl-3,4,8,9-tetrahydro-2H-pyridazino[1,6-a][1,3,5]triazin-2-imine/one/thione derivatives were synthesized by a sequence of reactions starting from appropriate aryl hydrocarbons. The final compounds were screened for antihypertensive activities by non-invasive method using Tail Cuff method. All the test compounds showed significant antihypertensive activity; 7-(biphenyl-4-yl)-3,4,8,9-tetrahydro-2H-pyridazino[1,6-a][1,3,5]triazin-2-imine (4p) exhibited antihypertensive activity more than the reference standard drugs.