Javid Zaidi

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Novel neurotensin (NT) (8-13) (Arg(8)-Arg(9)-Pro(10)-Tyr(11)-Ile(12)-Leu(13)) mimetics 3, 4 were designed by adopting all intrinsic functional groups of the native neurotensin(8-13) and using a substituted indole as a template to mimic the pharmacophore of NT(8-13). Biological studies at subtype 1 of the NT receptor showed that 3 has a 55 and 580 nM binding(More)
We report the development of two novel neurotensin mimetics (mimics 1 and 2). These compounds were rationally designed and synthesized according to the multiple template approach. We present results of experiments designed to define their pharmacological profiles. In radioligand binding assays with murine neuroblastoma clone N1E-115, we determined the(More)
A convenient and novel method of cyclisation of 4-(4-substituted-phenylsulfonamido)-butanoic acids to their corresponding p-substituted 1-arylsulfonyl-pyrrolidin-2-ones was achieved by using polyphosphate ester (PPE). The reaction times were considerably reduced, with an increase in yields, when PPE was used in combination with a catalytic amount of(More)
A series of new benzenesulfonamides, most of which are chiral, incorporating 1, 3, 4-oxadiazole and amino acid moieties have been synthesized. Some of these compounds were screened for antimalarial activity and also evaluated for their ability to inhibit hem polymerization. The electrophoretic analysis indicated that one compound was effective in inhibiting(More)
In the enanti-omerically pure title compound, C(11)H(19)N(3)O(3)S, the chain C-N-C(O)-O-C-C (from the asymmetric carbon to a methyl of the tert-butyl group) displays an extended conformation. In the crystal, mol-ecules are linked into chains parallel to the c axis by classical N-H⋯O(diazo-carbon-yl) hydrogen bonding and an unusual inter-molecular(More)
In the enanti-omerically pure title compound, C(15)H(15)NO(6), the five-membered ring displays a twist conformation with the local axis through the N atom. The acetyl groups are perpendicular to the ring [dihedral angles 80.3 (1) and 89.3 (1)°] and project to opposite sides. The packing is governed by two weak C-H⋯O inter-actions, forming layers of(More)
The introduction of an homologous series of cyclic amines at position 2 of 5-methylfurane and its isoster 5-methylthiophene induced a weak antagonist behaviour, probably depending on the steric hindrance of the substituents at the nitrogen, in the case of the cardiac tissue. Surprisingly, when evaluated on guinea-pig ileum preparatons, these compounds(More)
Chiral 4-[(2-isopropyl-5-methylcyclohexyl)oxo]-4oxobutanoic acid reacts with substituted anilines to produce amides 1-6 in high yields. Resulted amides 1-6 were investigated for their antifungal and antibacterial activities. Compounds 2 (96.5%) against Aspergillus fumigatus and 6 (93.7%) against Helminthosporium sativum demonstrated excellent activities.(More)
We report the rational design of novel neurotensin mimetics through use of the Multiple Template Approach. This approach is based on our notion that a flexible peptide can be replaced by a partially flexible molecule, identified through testing a comparatively small number of molecules possessing a different intrinsic availability of conformations of the(More)