Synthesis, Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives

被引:12
作者
Gorle, Sridevi [1 ]
Maddila, Suresh [2 ]
Chokkakula, Santosh [3 ]
Lavanya, Palakondu [4 ]
Singh, Moganavelli [1 ]
Jonnalagadda, Sreekanth B. [2 ]
机构
[1] Univ KwaZulu Natal, Sch Life Sci, Discipline Biochem, Westville Campus,Chiltern Hills, ZA-4000 Durban, South Africa
[2] Univ KwaZulu Natal, Sch Chem & Phys, Westville Campus,Chilten Hills,Private Bag 54001, ZA-4000 Durban, South Africa
[3] Adikavi Nannaya Univ, Sch Life & Hlth Sci, Rajahmundry 533296, India
[4] JNT Univ, Annamacharya Inst Technol & Sci, Dept Chem, Tirupati 517502, Andhra Pradesh, India
关键词
STRUCTURE-BASED DESIGN; ANTICONVULSANT ACTIVITY; INHIBITORS; AGENTS; DISCOVERY; SYNTHASE; POTENT; L;
D O I
10.1002/jhet.2498
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new series of 5-fluoro-N-4-(3-(4-substitutedbenzylamino)phenyl)-N-2-(4-morpholinophenyl)pyrimidine-2,4-diamine derivatives (7a-j) are prepared from using an intermediate compound 5-fluoro-N-4-(3-(aminophenyl)-N-2-(4-morpholinophenyl) pyrimidine-2,4-diamine (5). The structures of the newly synthesized products are established from their spectral H-1-NMR, C-13-NMR, F-19-NMR, ESI-MS, and analytical data. Here we report the synthesized compounds and larvicidal activity. All the compounds are screened for their significant larvicidal activity against third instar larvae at 24, 48, and 78-h time exposure, and values were compared with standard drug Malathion. The Compounds 7i, 7a, 7c, 7f, and 7j exhibited significant activity. However the compounds 7b, 7e, 7d, and 7h showed excellent activity when compared to the above compounds and to standard drug malathion too because of the presence of mild electron withdrawing groups such as trifluoro, fluorine, hydroxy, nitro, and methoxy derivatives which are attached to the benzyl ring.
引用
收藏
页码:1852 / 1858
页数:7
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