Articles written in Proceedings – Section A
Volume 13 Issue 6 June 1941 pp 566-572
With a view to study the relation between chemical constitution and physiological activity, attempts have been made chiefly to synthesise a group of sympathomimetically active amines derived from phenanthrene, chrysene, quinoline and
3∶4-Dimethoxy chrysene, 7∶8-dimethoxy-quinoline, 7∶8-dimethoxy quinaldine and 1-methyl-3∶4-dihydro-5∶6-dimethoxy-
Volume 14 Issue 2 August 1941 pp 126-132
With the object of studying the relationship between chemical constitution and physiological activity of sympathomimetically active amines, one member of the group Ar2: C (OH)·CH2NH2, belonging to the phenan-threne series has been synthesised.
A number of simple bases derived from benzene and the isoquinoline ring-systems, possessing the requisite structure for sympathomimecity, have also been prepared for purposes of a comparative pharmacological study.
Volume 15 Issue 6 June 1942 pp 432-436
With the object of studying the antibacterial effect of sulphanilamide derivatives with cyclic substituents at the sulphonamide radical, typical N1-sulphanilamido derivatives of diphenylether, phenanthrene, chrysene, dibenzofuran, carbazole, coumarin, acridine, tetrahydroquinoline and phenanthridine have been synthesised and are reported. Aminosulphonamide derivatives of naphthalene and diphenyl are also described.
Volume 16 Issue 2 August 1942 pp 163-166
The factors influencing optimum yields and purity of furyl acrylic acid by the condensation of furfural and malonic acid in the presence of pyridine have been investigated.
A rapid and elegant preparative method for β, 2-furyl acrylic acid of a high degree of purity has been worked out.
Volume 18 Issue 2 August 1943 pp 100-103
With the object of ascertaining the relative antibacterial merits of sulphonamides derived, among a few others, chiefly from heterocyclic ring systems, a series of N1-substituted sulphonamides containing the triazole, benzotriazole, indazole, indole, and indotriazine rings have been synthesised. Additional compounds reported are the sulphonamide derivatives of acetophenone and guanidine.
A few Schiff's bases derived from the sulphonamides have also been prepared for their possible therapeutic usefulness and for a study of the mode of action of the sulphonamido Schiff's bases in general.
Volume 18 Issue 2 August 1943 pp 104-107
Chiefly by the action of alkyl or aralkyl halides or the alkyl sulphates on the sulphanilamido heterocycles, a series of compounds, insoluble in alkali, has been obtained. Because of the likelihood of these not being absorbed from the intestine, which is alkaline in pH, the type of compounds synthesised are expected to prove particularly useful in infections of the intestinal tract.
Volume 18 Issue 2 August 1943 pp 108-112
On the ground that the sulphonamide group of drugs after suitable synthetic modifications of their molecules may probably be useful in mycobacterial infections, the possibility of rendering a few members, previously known to be active in coccal infections, lipophilic by the introduction of fatty acid residues in the latter has been explored. Accordingly, normal and branched chain acyl derivatives, thirty-seven in all, of sulphanilamide, sulphapyridine, sulphathiazole, sulphathiazoline, etc., have been synthesised.
Volume 19 Issue 6 June 1944 pp 343-350
With the object of exploring the group of N4, N1-diacyl sulphanilamides for practicable antibacterial agents and in view of the possibility of shedding further light on the existing theories of the mode of sulphonamide action by a study of the N4, N1-diacyl sulphanilamide type of compounds, a number of N4, N1-diacyl sulphanilamides, twenty in all, have so far been synthesised.
Volume 19 Issue 6 June 1944 pp 351-356
the synthesis of a series of phenolic azo-dyes derived from the sulphonamides with the object of exploring their therapeutic potentialities and of gaining an insight into their mode of action, has been effected and reported.
Volume 20 Issue 2 February 1944 pp 107-108
In continuation of an earlier line of work, synthesis has been effected of N,N′-trimethylene
Volume 20 Issue 4 October 1944 pp 175-186
Experiments in the group of sympathomimetics - Part V. Relation between chemical constitution and pressor activity of possible sympathomimetics derived from the benzene, naphthalene, phenanthrene and isoquinoline rings
Twenty-one selected compounds derived severally from benzene, naphthalene, acenaphthene, phenanthrene and isoquinoline have been examined for their pressor activities in the spinal cat, using tyramine as the control.
The α-naphthyl methylamines resemble benzylamine in exhibiting feeble activities. Fair degrees of activity are shown by the ω-amino aceto-naphthones, the β-naphthyl ethanolamines and the β-naphthyl ethylamines. The rules governing the qualitative and quantitative relation between structure and pressor action of benzenoid sympathomimetics seem to apply to members of the naphthalene series only to a limited extent. The substitution of the benzene nucleus of pressor bases by the naphthalene ring generally results in considerable increased activity, but this has an exception. Consequently, the generalisation of Madinaveitia that such substitution augments the activity by over forty times receives only limited support. The postulate of von Braun that methyl amino hydrindene owed its intense activity to its being doubly a β-phenyl ethylamine appears inadequate in view of the low activity evinced by a number of bases which may be considered as β-phenyl ethylamines many times over. While the naphthalane and acenaphthene nuclei are equal and about seven times as effective as the benzene ring the phenanthrene ring is only twice as effective. New potent pressors appear unlikely to be encountered in the benzene, phenanthrene and isoquinoline ring systems, but the naphthalene series seems to be promising.
Volume 22 Issue 3 September 1945 pp 143-147
The latex of
Volume 23 Issue 2 February 1946 pp 60-66
Kanugin C19H16O7 yields myristicic acid and
Volume 23 Issue 2 February 1946 pp 97-101
The synthesis of 3∶5∶ 6∶3′∶ 4′-pentahydroxy-flavone was already reported. The lower members of this group of 5∶ 6-hydroxy flavonols with one and no hydroxyl group in the side-phenyl nucleus have now been prepared by Kostanecki’s method. The characteristic properties are described.
Volume 25 Issue 5 May 1947 pp 432-437
The difficulty of the demethylation of synthetic primetin dimethyl ether into primetin has been solved by the use of anhydrous aluminium chloride in benzene medium. The possibility of the formation of primetin in the Primula through the intermediate stage of 5-hydroxy-flavone is suggested. This is supported by a new synthesis of primetin in which the nuclear oxidation of 5-hydroxy-flavone is effected by means of persulphate. 5-Hydroxy-flavone required for these experiments has been prepared by independent methods.
Volume 26 Issue 1 July 1947 pp 18-21
It is shown that 5:6:7:8-hydroxy-flavonols (Calycopterein series) can be made from 5:6:7-hydroxy-flavonols (quercetagetin series) by the nuclear oxidation of the 8-position. Quercetagetin and nor-tangeretin have thus been converted into 6:8-dihydroxy-quercetin and calycopteretin in good yields.
Volume 27 Issue 2 March 1948 pp 85-90
It is shown that the nuclear oxidation of hydroxy-chalkones can be successfully effected thereby introducing a fresh hydroxyl in the 5-position which corresponds to the 6-position in flavanones and flavones. 2-Hydroxy-4-methoxy-chalkone and 2-hydroxy-4∶6-dimethoxy-chalkone have thus been oxidised to the 2∶5-dihydroxy compounds. In the first case the product is shown to be 2∶5-dihydroxy-4-methoxy-chalkone by complete methylation and identification of the derivative as 2∶4∶5-trimethoxy-chalkone. In the second case it is proved to be 2∶5-dihydroxy-4∶6-dimethoxy-chalkone by partial methylation and conversion into 5∶6∶7-trimethoxy-flavanone.
Volume 28 Issue 2 August 1948 pp 31-39
Synthetic confirmation for the constitution of quercetagitrin is provided. The pentamethyl-quercetagetin obtained by the complete methylation and hydrolysis of the glucoside is finally ethylated and the product shown to be identical with a synthetic sample of 7-ethoxy-3∶5∶6∶3′∶4′-pentamethoxy flavone (V) made from 2-hydroxy-4-ethoxy-ω: 6-dimethoxy-acetophenone (VI) using oxidation with persulphate, Allan-Robinson condensation and final methylation as stages. The ketone (VI) is conveniently made by the alkali fission of
Volume 28 Issue 3 September 1948 pp 94-95
Volume 29 Issue 1 January 1949 pp 9-15
The following three partial methyl ethers of flavonols which are derivatives of naturally occurring monoglucosides having only one free hydroxyl group have been conveniently synthesised by using the method of partial benzylation: (1) 3 ∶ 5 ∶ 4′-O-trimethyl-kæmpferol derived from populnin and related glycosides, (2) 3 ∶ 5 ∶ 3′ ∶ 4′-O-tetramethyl quercetin derived from quercimeritrin and (3) 3 ∶ 5 ∶ 7 ∶ 3′ ∶ 4′-O-pentamethyl gossypetin derived from gossypin.
Volume 30 Issue 5 November 1949 pp 265-270
Asaronic acid is conveniently prepared from 4-O-methyl-β-resorcylic acid and isovanillic acid by oxidatron with alkaline persulphate and subsequent methylation. Useful partial methyl ethers and mixed methyl-ethyl ethers are also made by adopting this method. Similarly asarylic aldehyde is obtained from 4-O-methyl-β-resorcylic aldehyde and isovanillin.
Volume 31 Issue 1 January 1950 pp 21-25
Twenty-three compounds have been synthesised as possible lipophilic chemotherapeuticals of the sulphonamide and sulphone series. Among such compounds are the hydnocarpic acid derivatives of N4-
Volume 31 Issue 1 January 1950 pp 26-30
An attempt has been made to explore the little investigated but chemically and biologically interesting group of 2-sulphanilamidothiazolones, mostly carrying lipophilic alkyl radicals in the 5-position, for members likely to prove useful in the treatment of tuberculosis and leprosy. In the synthesis of the candidate compounds, emphasis has been laid on the N4-
A preparative method for the intermediate 2-amino-5-substituted thiazolones, starting with the corresponding mono- and dibasic fatty acids, has been worked out. New 5-substituted pseudothiohydantoins, derived from monobasic acids, are 5-
The following sulphonamidothiazolones have been synthesised: N4-
2-Sulphanilamido-5-ethylthiazolone, prepared in the course of this study, differs in its physical characteristics from that of sulphaethylthiazolone as reported by the earlier workers. However, the present sample affords good analytical values and is markedly active in some acute bacterial infections.
Volume 31 Issue 1 January 1950 pp 31-34
For the synthesis of 5∶6∶8-trihydroxy flavone (6-hydroxy primetin), the two stage ortho-oxidation process is applied to primetin monomethyl ether. A good yield of the 6-aldehyde is obtained, which undergoes oxidation to 5∶6-dihydroxy-8-methoxy flavone. Subsequent demethylation yields 6-hydroxy primetin. Its properties and reactions and derivatives are described.
Volume 31 Issue 2 February 1950 pp 107-116
The highly favourable first reports about the antibacterial merits of 5∶5′-dihalogenated salicils and the essentially sulphonamide-like nature of their action on bacteria, led to an improved method of preparation of 5∶5′-dichlorosalicil or “chlorosalicil” for ascertaining its usefulness in human tuberculosis.
The ineffectiveness of chlorosalicil on
A total of twenty-eight heterocyclic compounds have been synthesised in this connection. Synthesis of these furnished interesting information regarding the chemistry of imidazoles.
A few representative heterocyclics, now prepared, have been subjected to examination for efficacy
Volume 31 Issue 2 February 1950 pp 117-123
In order to fit the sulphonamides and sulphones out better for use in the chemotherapy of tuberculosis and leprosy, synthesis has been effected of a series of
The twenty-six compounds synthesised include
Volume 31 Issue 3 March 1950 pp 183-186
A series of sulphanilamides derived from N-carbo and heterocyclic hydroxamides have been synthesised, since a number of N4-acyl sulphanilhydroxamides have been favourably reported on in preliminary experimental bacterial infections. Among the latter was
Volume 31 Issue 5 May 1950 pp 358-358 Erratum
Volume 34 Issue 5 November 1951 pp 319-323
Volume 50 Issue 3 September 1959 pp 219-222
The synthesis of 6:7:3′:4′-tetramethoxy isoflavone is described.