- Synthesis and Identification of of Some New Heterocyclic Compounds for Mesalazin Drug Derivatives with Evaluating of Their Biological Efficiency and Anti-oxidant Activity
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In this research work new heterocyclic derivatives containing triazolidine have been prepared. The most available (mesalazine) has been used with benzaldehyde to get the starting material to prepare the alkyl triazolidine. All the synthesized compounds have been identified using FT-IR and 1H-NMR spectrum. (Scheme 1) shows that, from simple and available material mesalazine with benzaldehyde in basic media compound (H1) containing Schiff base prepared. A ring closer reaction has been made to compound W using ethylene glycol and hydrazine to get (H2) compound. The nitrogen atom of compound (H2) also alkylated by chloroacetic acid to give (H4) compound then H4 compound reacted with thionyl chloride to get acetyl chloride (H5compound). Compound H5 treated with amino acid (glycine) to get (H6) compound. (H7) Compound has been synthesis by reacting (H6) compound with aromatic aldehyde in the presence of acetic anhydride to get Oxazole ring (H7 compound). Also, (H2) compound reacted with malic anhydride to prepare triazolidine diacetic acid derivative H3 compound. These synthesized compounds had also been assessed by (DPPH) method, the compounds (H1-H7) evaluated for their antimicrobial activity and antioxidant activity, the compounds have strong antioxidant activity comparable to that of the well known (ascorbic acid) (IC50=31.95 μg/mL) used.
- Lihumis, Hala Shkyair,Hashim, Dhekra Jawad
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p. 6761 - 6770
(2021/11/01)
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- Benzoic acid derivatives and use thereof
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A pharmaceutical composition for use in the treatment of psoriasis comprises 4-aminosalicylic acid (4-ASA) or 5-aminosalicylic acid (5-ASA) or a functional derivative thereof, said pharmaceutical composition being in a form suitable for topical administration. Furthermore, 4- or 5-ASA or a functional derivative thereof are used for the manufacture of pharmaceutical compositions for treating psoriasis, atopic dermatitis, allergic dermatitis, contact dermatitis, seborrhoic dermatitis, or acne diseases. The derivatives have the formulae: STR1 where W is COOX, wherein X is H, Li, Na, K, Mg0.5, Ca0.5, Zn0.5, Al0.33, Fe(II)0.5, Fe(III)0.33, NH4, NH3 R1, NH2 R12, NHR13, NR14, or R1, where R1 is substituted or unsubstituted C1-6 -alkyl, aryl-C1-4 -alkyl, or heteroaryl-C1-4 -alkyl; or COX, where X is NR1 R1', where R1' has the same meaning as R1 defined above and R1 and R1' may be identical or different; Y is H or R1 CO, where R1 is defined as above; Z1 and Z2, which may be identical or non-identical are H, R1 or R1 CO, where R1 is defined as above, or Z1 and Z2 represent R2, where R2 is substituted or unsubstituted C1-6 -alkylidene or aryl-C1-6 -alkylidene, or heteroaryl-C1-6 -alkylidene, or Z1, Z2 together with the nitrogen atom to which they are attached may represent a 3 to 7 membered saturated or unsaturated heterocyclic ring, or may represent a group of the formula --N=N--R3 where R3 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.
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