Isatin is an endogenous compound identified in humans that possesses a wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activities and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin-N-Mannich bases of ...

3 Starting from 2-methyl-4-nitro-imidazole, new 5-(2-methyl- 4-nitro-1-imidazomethyl)-1,3,4-oxadiazole-2-thione () was synthesized and was subjected to Mannich reaction with appropriate amines to yield a new series of 3-substituted aminomethyl-5-(2-methyl-4-nitro-1-imidazomethyl)- 1,3,4-oxadiazole-2-thiones (4a-j). The structure of the title compounds was elucidated by elemental analysis and sp...

Mannich bases are generally formed by the reaction between formaldehyde, a secondary amine and a compound containing reactive hydrogen atoms. They display varied biological activities such as antimicrobial [1], cytotoxic [2,3], anticancer [2], analgesic [4], anti-inflammatory [5] and anticonvulsant [6] and DNA topoisomerase I inhibiting activities [3]. In this study, it was planned to synthesiz...

Inorganic as well as organic base catalysis was found to be effective for diastereoselective Mannich additions of malonic acid derivatives to (SS)-N-(tert-butanesulfinyl)-3,3,3-trifluoroacetaldimine. In the presence of catalytic amounts of inorganic bases, n-BuLi or DMAP, the reaction gives the corresponding (R,SS)-β-aminomalonates in good yield and with diastereoselectivity up to 9/1 dr. In co...

Disubstituted [1,3,4]-oxadaiazoles (6a-b), Mannich bases (7a-f) and S-alkylated derivatives (8a-f) have been synthesized from 4-(methylsulfonyl/sulfinyl)phenylaceticacid (3a-b) through a multi-step reaction sequence starting from (4-methylthio)phenylacetonitrile (1). The structures of new compounds were established on the basis of their elemental analysis, IR, H NMR, C NMR and mass spectral dat...

A novel, practical and efficient enantioselective synthesis of sphingoid bases, l-threo-[2S,3S]-sphinganine (safingol), l-threo-[2S,3S]-sphingosine, l-arabino-[2R,3S,4R] and l-xylo-[2R,3S,4S]-C(18)-phytosphingosine is described. The synthetic strategy features the Sharpless kinetic resolution and tethered aminohydroxylation (TA) as the key steps.

A new series of Mannich bases MK8-12 has been synthesized from 1, 2, 4thiadiazole by Mannich reaction. All the synthesized compounds of the series displayed, remarkable analgesic activity in comparison to standard drug diclofenac sodium. In the synthesized thiadiazole derivatives MK-8 & MK-10 showed activity at 20mg/kg . MK-9 & MK-11 are considered as most active compounds as they protected 60....

The starting compound 1H-indole-2,3-dione on reaction with different substituted anilines formed the Schiff bases. The corresponding NMannich bases have been prepared by the reaction of the Schiff bases with diphenyl amine in the presence of formaldehyde. The chemical structures of the title compounds have been confirmed and elucidated by means of their physical and spectral data respectively. ...