A seriea of 33 oxime N-methylcarbamates R 1 R2C=N O CONHCHa (R 1 and R2 = � • alkyl, cycloalkyl, haloalkyl, subatituted aryl, or groupsJike (CHa)2C=CH, CFaCOCH2] was synthes � and tested for potentiel anticholinesteraae activity. Some of thoee compounds 11uch as the a,a,a-tritluoroacetopben oxime derivativea were atudied for their in vitro and in vivo activity; other structures are nove) ones. The configuration of thoee compou nds was 888igned by s � pic methods (NMR, � • lf':>: The meaaure of the reeidual activity of the acetylcholinest erase (boVllle erythrocyte) after � e inhibition by thoee moleculea allowed the detennination of the diaaociation conatant � d and the . bimolecular � bamoylation rate conatant k•. To take isomeriam into account, the group � 18 always CIS to the carbamic moiety. The structure-acti�ty relationsbip studies were performed with the usual stru ctura! parame � rs and includedcom mercial compoundssuch as aldicarb, methomyl, and ommyl The correlation equation obtained is log ki • 0.4652:174' + 0.474174'R2 + 0.4072:T + 2.247 (n = � • r • 0.862,, • 0.74), � here � e electronic effect of the grouP6 R 1 and� is depicted by the Taft indu �y e constant . U: and � � po p bilic contribution by the Hansch parameter T, S P_eC � c . correlationa exhi . b1t th � prev � partiel ��� of the group � in the formation of the enzyme-inhib1tor complex and m the mteractiona of the inhib1tor with the trimethyl site. C sHs CFa 84 2a 4-FCsH• CFa oilb 3a CFs 4-ClCsH4 oilb 4a 4-CHsCsH. CF3 62 5a 4-CHaOCsH. CFa 105 6a CFs 4-C2HsOCsH. 70 7a CFa 4-CeH&OCsH. 105-8 8a CFa 4-CF 3 Csli. oilb 9a 3-FCsH. CFs 91/l.5mmHg 10a 3-CICsH. CFs 130/1 mmHg lla 3-CHaC&lic CFa oi!b 12a CFs 3-CHaOCsH. 120/0.5 mmHg 13& 2-FCsH, CFa oilb lu 2-CICsH. CFs 79/SmmHg 15a 2-CH 3 Csli. CFa oilb 16a 2-CHsOCsli. CFa 75 17a CFs 2-CHaOCsH.

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